Ibetazol, a novel inhibitor of importin b1-mediated nuclear import.
Vercruysse T, Vanstreels E, Jacquemyn M, Boland S, Kilonda A, Allasia A, Vandecaetsbeek I, Klaassen H, Versele M, Chaltin P, Marchand A, Daelemans D. Nature Communications Biology. 2024 Nov 23. 7(1):1560. doi: 10.1038/s42003-024-07237-8.
Synthesis of novel imino-coumarin and acrylonitrile 2-benzoale hybrids as potent anticancer agents targeting tubulin
Pavlinak I, Persoons L, Bec A, Vrban L, Daelemans D, Vianello R, Hranjec M,
Bioorg Chem. 2024 Nov 22. 154:107991. doi: 10.1016/j.bioorg.2024.107991.
3-nitropyridine analogues as novel microtubule-targeting agents.
Herman J, Vanstreels E, Bardiot D, Prota A, Gaillard N, Gao L, Vercruysse T, Persoons L, Daems T, Waer M, Herdewijn P, Louat T, Steinmetz M, De Jonghe S, Sprangers B, Daelemans D.
PLoS One. 2024 Nov 7. 19(11):e0307153. doi: 10.1371/journal.pone.0307153. eCollection 2024.
Allosteric degraders induce CRL5 -ASB8 mediated degradation of XPO1.
Hudman-Wing C, Fung H, Cagatay T, Kwanten B, Niesman A, Gharghabi M, Permentier B, Shakya B, Schacham S, Landesman Y, Lapalombella R, Daelemans D, Chook Y.
bioRxiv [preprint]. 2024 Oct 11. 2024.10.07.617049. doi: 10.1101/2024.10.07.617049.
Biological evaluation of novel amidino substituted coumarin-benzazole hybrids as promising therapeutic agents.
Beč A, Racané L, Žonja L, Persoons L, Daelemans D, Starčević K, Vianello R, Hranjec M. RSC Med Chem. 2023 Apr 4. 14(5):957-968. doi: 10.1039/d3md00055a.
Polyketide Synthase-Mediated O-Methyloxime Formation in the Biosynthesis of the Oximidine Anticancer Agents.
Vriens E, De Ruysscher D, Weir ANM, Dekimpe S, Steurs G, Shemy A, Persoons L, Santos AR, Williams C, Daelemans D, Crump MP, Voet A, De Borggraeve W, Lescrinier E, Masschelein J.
Angew Chem Int Ed Engl. 2023 Aug 21. 62(34):e202304476. doi: 10.1002/anie.202304476.
Novel Biologically Active N-Substituted Benzimidazole Derived Schiff Bases: Design, Synthesis, and Biological Evaluation.
Beč A, Cindrić M, Persoons L, Banjanac M, Radovanović V, Daelemans D, Hranjec M. Molecules. 2023 Apr 25. 28(9):3720. doi: 10.3390/molecules28093720.
E3 ubiquitin ligase ASB8 promotes selinexor-induced proteasomal degradation of XPO1.
Kwanten B, Deconick T, Walker C, Wang F, Landesman Y, Daelemans D. Biomed Pharmacother. 2023 Apr. 160:114305. doi: 10.1016/j.biopha.2023.114305.
Intrinsic temperature increases drivers of lipid metabolism towards ferroptosis evasion and chemotherapy resistance in pancreatic cancer.
de Laat V, Topal H, Spotbeen X, Talebi A, Dehairs J, Idkowiak J, Vanderhoydonc F, Ostyn T, Zhao P, Jacquemyn M, Wolk M, Sablina A, Augustyns K, Vanden Berghe T, Roskams T, Daelemans D, Fedorova M, Topal B, Swinnen JV.
Nature Communications. 2024 Oct 2 15(1):8540. doi: 10.1038/s41467-024-52978-z.
Tankyrase1/2 inhibitor XAV-939 reverts EMT and suggests that PARylation partially regulates aerobic activities in human hepatocytes and HepG2 cells.
De Vos K, Mavrogiannis A, Wolters JC, Schlenner S, Wierda K, Cortes Calabuig A, Chinnaraj R, Dermesrobian V, Armoudjian Y, Jacqueymyn M, Corthout N, Daelemans D, Annaerts P.
Biochem. Pharmacol. 2024 Sep. 227:116445. doi: 10.1016/j.bcp.2024.116445. Epub 2024 Jul 23.
The Role of TIM-1 and CD300a in Zika Virus Infection Investigated with Cell-Based Electrical Impedance.
Oeyen M, Heymann CJF, Jacquemyn M, Daelemans D, Schols D.
Biosensors (Basel). 2024 Jul 25. 14(8):362. doi: 10.3390/bios14080362.
Targeting conserved TIM3+VISTA+ tumor-associated macrophages overcomes resistance to cancer immunotherapy.
Vanmeerbeek I, Naulaerts S, Sprooten J, Laureano RS, Govaerts J, Trotta R, Pretto S, Zhao S, Cafarello ST, Verelst J , Jacquemyn M, Pociupany M, Boon L, Schlenner SM, Tejpar S, Daelemans D, Mazzone M, Garg AD.
Sci Adv. 2024 Jul 19; 10(29):eadm8660. doi: 10.1126/sciadv.adm8660. Epub 2024 Jul 19.
IL-10 predicts incident neuroinflammatory disease and proviral load synamics in a large brazilian cohort of people living with human T-lymphotropic virus type 1.
Assone T, Menezes SM, Goncalves FT, Folgosi VA, Braz M, Smid J, Haziot ME, Marcusso RMN, Dahy FE, de Oliviera ACP, Vanderlinden E, Claes S, Daelemans D, Vercauteren J, Schols D, Casseb J, Van Weyenbergh J.
Front Immunol. 2024 Jun 19;15:1416476. doi: 10.3389/fimmu.2024.1416476. eCollection 2024.
Biological activity and computational analysis of novel acrylonitrile derived benzazoles as potent antiproliferative agents for pancreatic adenocarcinoma with antioxidative properties.
Bec A, Persoons L, Daelemans D, Starcevic K, Vianello R, Hranjec M.
Bioorg Chem. 2024 Jun;147:107326. doi: 10.1016/j.bioorg.2024.107326. Epub 2024 Apr 6.
Novel acrylonitrile derived imidazo[4,5-b]pyridines as antioxidants and potent antiproliferative agents for pancreatic adenocarcinoma.
Bocek Pavlinac I, Persoons L, Daelemans D, Starcevic K, Vianello R, Hranjec M.
Int J Biol Macromol. 2024 May;266(Pt 2): 131239. doi: 10.1016/j.ijbiomac.2024.131239. Epub 2024 Apr 1.
Synthesis and Biological Evaluation of Novel Amino and Amido Substituted Pentacyclic Benzimidazole Derivatives as Antiproliferative Agents.
Perin N, Gulin M, Kos M, Persoons L, Daelemans D, Fabijanic I, Stojkovic MR, Hranjec M.
Int J Mol Sci. 2024 Feb 14;25(4):2288. doi: 10.3390/ijms25042288.
4-Octyl itaconate reduces influenza A replication by targeting the nuclear export protein CRM1.
Ribo-Molina P, Weiss HJ, Susma B, van Nieuwkoop S, Persoons L, Zheng Y, Ruzek M, Daelemans D, Fouchier RAM, O’Neill LAJ, van den Hoogen BG.
J Virol. 2023 Oct 31;97(10):e0132523. doi: 10.1128/jvi.01325-23. Epub 2023 Oct 12.
Synthesis and Antiproliferative Activity of 2,6-Disubstituted Imidazo[4,5-b]pyridines Prepared by Suzuki Cross Coupling.
Boček Pavlinac I, Dragić M, Persoons L, Daelemans D, Hranjec M.
Molecules. 2023 Oct 21. 28(20):7208. doi: 10.3390/molecules28207208
4-Octyl itaconate reduces influenza A replication by targeting the nuclear export protein CRM1.
Ribó-Molina P, Weiss HJ, Susma B, van Nieuwkoop S, Persoons L, Zheng Y, Ruzek M, Daelemans D, Fouchier RAM, O’Neill LAJ, van den Hoogen BG.
J Virol. 2023 Oct 31. 97(10):e0132523. doi: 10.1128/jvi.01325-23.
Novel hydroxy- and amidino-substituted benzimidazoles and benzothiazoles as antibacterial and antiproliferative agents.
Beč A, Racané L, Tomić T, Persoons L, Daelemans D, Banjanac M, Radovanović V, Hranjec M.
Future Med Chem. 2023 Jul. 15(14):1251-1272. doi: 10.4155/fmc-2023-0154.
TMEM106B is a receptor mediating ACE2-independent SARS-CoV-2 cell entry.
Baggen J, Jacquemyn M, Persoons L, Vanstreels E, Pye VE, Wrobel AG, Calvaresi V, Martin SR, Roustan C, Cronin NB, Reading E, Thibaut HJ, Vercruysse T, Maes P, De Smet F, Yee A, Nivitchanyong T, Roell M, Franco-Hernandez N, Rhinn H, Mamchak AA, Ah Young-Chapon M, Brown E, Cherepanov P, Daelemans D. Cell. 2023 Aug 3. 186(16):3427-3442.e22. doi: 10.1016/j.cell.2023.06.005.
Biological evaluation of novel amidino substituted coumarin-benzazole hybrids as promising therapeutic agents.
Beč A, Racané L, Žonja L, Persoons L, Daelemans D, Starčević K, Vianello R, Hranjec M. RSC Med Chem. 2023 Apr 4. 14(5):957-968. doi: 10.1039/d3md00055a.
Polyketide Synthase-Mediated O-Methyloxime Formation in the Biosynthesis of the Oximidine Anticancer Agents.
Vriens E, De Ruysscher D, Weir ANM, Dekimpe S, Steurs G, Shemy A, Persoons L, Santos AR, Williams C, Daelemans D, Crump MP, Voet A, De Borggraeve W, Lescrinier E, Masschelein J.
Angew Chem Int Ed Engl. 2023 Aug 21. 62(34):e202304476. doi: 10.1002/anie.202304476.
Novel Biologically Active N-Substituted Benzimidazole Derived Schiff Bases: Design, Synthesis, and Biological Evaluation.
Beč A, Cindrić M, Persoons L, Banjanac M, Radovanović V, Daelemans D, Hranjec M. Molecules. 2023 Apr 25. 28(9):3720. doi: 10.3390/molecules28093720.
E3 ubiquitin ligase ASB8 promotes selinexor-induced proteasomal degradation of XPO1.
Kwanten B, Deconick T, Walker C, Wang F, Landesman Y, Daelemans D. Biomed Pharmacother. 2023 Apr. 160:114305. doi: 10.1016/j.biopha.2023.114305.
Biological evaluation of novel amidino substituted coumarin-benzazole hybrids as promising therapeutic agents.
Beč A, Racané L, Žonja L, Persoons L, Daelemans D, Starčević K, Vianello R, Hranjec M. RSC Med Chem. 2023 Apr 4. 14(5):957-968. doi: 10.1039/d3md00055a.
Polyketide Synthase-Mediated O-Methyloxime Formation in the Biosynthesis of the Oximidine Anticancer Agents.
Vriens E, De Ruysscher D, Weir ANM, Dekimpe S, Steurs G, Shemy A, Persoons L, Santos AR, Williams C, Daelemans D, Crump MP, Voet A, De Borggraeve W, Lescrinier E, Masschelein J.
Angew Chem Int Ed Engl. 2023 Aug 21. 62(34):e202304476. doi: 10.1002/anie.202304476.
Novel Biologically Active N-Substituted Benzimidazole Derived Schiff Bases: Design, Synthesis, and Biological Evaluation.
Beč A, Cindrić M, Persoons L, Banjanac M, Radovanović V, Daelemans D, Hranjec M. Molecules. 2023 Apr 25. 28(9):3720. doi: 10.3390/molecules28093720.
E3 ubiquitin ligase ASB8 promotes selinexor-induced proteasomal degradation of XPO1.
Kwanten B, Deconick T, Walker C, Wang F, Landesman Y, Daelemans D. Biomed Pharmacother. 2023 Apr. 160:114305. doi: 10.1016/j.biopha.2023.114305.
CRISPR-Cas9 recognition of enzymatically synthesized base-modified nucleic acids.
Yang H, Eremeeva E, Abramov M, Jacquemyn M, Groaz E, Daelemans D, Herdewijn P. Nucleic Acids Res. 2023 Feb 28. 51(4):1501-1511. doi: 10.1093/nar/gkac1147.
Biological Activity of Amidino-Substituted Imidazo [4,5-b]pyridines.
Pavlinac IB, Zlatić K, Persoons L, Daelemans D, Banjanac M, Radovanović V, Butković K, Kralj M, Hranjec M. Molecules. 2022 Dec 21. 28(1):34. doi: 10.3390/molecules28010034.
Systemic cytokines and GlycA discriminate disease status and predict corticosteroid response in HTLV-1-associated neuroinflammation.
Assone T, Menezes SM, de Toledo Gonçalves F, Folgosi VA, da Silva Prates G, Dierckx T, Braz M, Smid J, Haziot ME, Marcusso RMN, Dahy FE, Vanderlinden E, Claes S, Schols D, Bruhn R, Murphy EL, Penalva de Oliveira AC, Daelemans D, Vercauteren J, Casseb J, Van Weyenbergh J. J Neuroinflammation. 2022 Dec 8. 19(1):293. doi: 10.1186/s12974-022-02658-w.
The material properties of a bacterial-derived biomolecular condensate tune biological function in natural and synthetic systems.
Lasker K, Boeynaems S, Lam V, Scholl D, Stainton E, Briner A, Jacquemyn M, Daelemans D, Deniz A, Villa E, Holehouse AS, Gitler AD, Shapiro L.
Nat Commun. 2022 Sep 26. 13(1):5643. doi: 10.1038/s41467-022-33221-z.
CRISPR/Cas9 screen in human iPSC-derived cortical neurons identifies NEK6 as a novel disease modifier of C9orf72 poly(PR) toxicity.
Guo W, Wang H, Kumar Tharkeshwar A, Couthouis J, Braems E, Masrori P, Van Schoor E, Fan Y, Ahuja K, Moisse M, Jacquemyn M, Furtado Madeiro da Costa R, Gajjar M, Balusu S, Tricot T, Fumagalli L, Hersmus N, Janky R, Impens F, Vanden Berghe P, Ho R, Thal DR, Vandenberghe R, Hegde ML, Chandran S, De Strooper B, Daelemans D, Van Damme P, Van Den Bosch L, Verfaillie C.
Alzheimers Dement. 2023 Apr. 19(4):1245-1259. doi: 10.1002/alz.12760.
CRISPR/Cas9 screen in human iPSC-derived cortical neurons identifies NEK6 as a novel disease modifier of C9orf72 poly(PR) toxicity.
Guo W, Wang H, Kumar Tharkeshwar A, Couthouis J, Braems E, Masrori P, Van Schoor E, Fan Y, Ahuja K, Moisse M, Jacquemyn M, Furtado Madeiro da Costa R, Gajjar M, Balusu S, Tricot T, Fumagalli L, Hersmus N, Janky R, Impens F, Vanden Berghe P, Ho R, Thal DR, Vandenberghe R, Hegde ML, Chandran S, De Strooper B, Daelemans D, Van Damme P, Van Den Bosch L, Verfaillie C.
Alzheimers Dement. 2023 Apr. 19(4):1245-1259. doi: 10.1002/alz.12760.
Hybridization Approach to Identify Salicylanilides as Inhibitors of Tubulin Polymerization and Signal Transducers and Activators of Transcription 3 (STAT3).
Gargantilla M, Persoons L, Kauerová T, Del Río N, Daelemans D, Priego EM, Kollar P, Pérez-Pérez MJ. Pharmaceuticals (Basel). 2022 Jul 6. 15(7):835. doi: 10.3390/ph15070835.
Imidazo[4,5-b]pyridine derived tubulin polymerization inhibitors: Design, synthesis, biological activity in vitro and computational analysis.
Boček I, Hok L, Persoons L, Daelemans D, Vianello R, Hranjec M. Bioorg Chem. 2022 Oct. 127:106032. doi: 10.1016/j.bioorg.2022.106032.
Cellular Stress Induces Nucleocytoplasmic Transport Deficits Independent of Stress Granules.
Vanneste J, Vercruysse T, Boeynaems S, Van Damme P, Daelemans D, Van Den Bosch L. Biomedicines. 2022 May 3. 10(5):1057. doi: 10.3390/biomedicines10051057.
The T850D Phosphomimetic Mutation in the Androgen Receptor Ligand Binding Domain Enhances Recruitment at Activation Function 2.
Helsen C, Nguyen T, Vercruysse T, Wouters S, Daelemans D, Voet A, Claessens F. Int J Mol Sci. 2022 Jan 29. 23(3):1557. doi: 10.3390/ijms23031557.
Anthranilamides with quinoline and β-carboline scaffolds: design, synthesis, and biological activity.
Beus M, Persoons L, Daelemans D, Schols D, Savijoki K, Varmanen P, Yli-Kauhaluoma J, Pavić K, Zorc B.
Mol Divers. 2022 Oct. 26(5):2595-2612. doi: 10.1007/s11030-021-10347-8.
Inhibition of XPO-1 Mediated Nuclear Export through the Michael-Acceptor Character of Chalcones.
Gargantilla M, López-Fernández J, Camarasa MJ, Persoons L, Daelemans D, Priego EM, Pérez-Pérez MJ. Pharmaceuticals (Basel). 2021 Nov 6. 14(11):1131. doi: 10.3390/ph14111131.
Target Identification of Small Molecules Using Large-Scale CRISPR-Cas Mutagenesis Scanning of Essential Genes.
Kwanten B, Neggers JE, Daelemans D. Methods Mol Biol. 2022. 2377:43-67. doi: 10.1007/978-1-0716-1720-5_3.
Hybridization Approach to Identify Salicylanilides as Inhibitors of Tubulin Polymerization and Signal Transducers and Activators of Transcription 3 (STAT3).
Gargantilla M, Persoons L, Kauerová T, Del Río N, Daelemans D, Priego EM, Kollar P, Pérez-Pérez MJ. Pharmaceuticals (Basel). 2022 Jul 6. 15(7):835. doi: 10.3390/ph15070835.
Imidazo[4,5-b]pyridine derived tubulin polymerization inhibitors: Design, synthesis, biological activity in vitro and computational analysis.
Boček I, Hok L, Persoons L, Daelemans D, Vianello R, Hranjec M. Bioorg Chem. 2022 Oct. 127:106032. doi: 10.1016/j.bioorg.2022.106032.
Cellular Stress Induces Nucleocytoplasmic Transport Deficits Independent of Stress Granules.
Vanneste J, Vercruysse T, Boeynaems S, Van Damme P, Daelemans D, Van Den Bosch L. Biomedicines. 2022 May 3. 10(5):1057. doi: 10.3390/biomedicines10051057.
The T850D Phosphomimetic Mutation in the Androgen Receptor Ligand Binding Domain Enhances Recruitment at Activation Function 2.
Helsen C, Nguyen T, Vercruysse T, Wouters S, Daelemans D, Voet A, Claessens F. Int J Mol Sci. 2022 Jan 29. 23(3):1557. doi: 10.3390/ijms23031557.
Anthranilamides with quinoline and β-carboline scaffolds: design, synthesis, and biological activity.
Beus M, Persoons L, Daelemans D, Schols D, Savijoki K, Varmanen P, Yli-Kauhaluoma J, Pavić K, Zorc B.
Mol Divers. 2022 Oct. 26(5):2595-2612. doi: 10.1007/s11030-021-10347-8.
Inhibition of XPO-1 Mediated Nuclear Export through the Michael-Acceptor Character of Chalcones.
Gargantilla M, López-Fernández J, Camarasa MJ, Persoons L, Daelemans D, Priego EM, Pérez-Pérez MJ. Pharmaceuticals (Basel). 2021 Nov 6. 14(11):1131. doi: 10.3390/ph14111131.
Target Identification of Small Molecules Using Large-Scale CRISPR-Cas Mutagenesis Scanning of Essential Genes.
Kwanten B, Neggers JE, Daelemans D. Methods Mol Biol. 2022. 2377:43-67. doi: 10.1007/978-1-0716-1720-5_3.
Synthesis, Computational Analysis and Antiproliferative Activity of Novel Benzimidazole Acrylonitriles as Tubulin Polymerization Inhibitors: Part 2.
Bec A, Hok L, Persoons L, Vanstreels E, Daelemans D, Vianello R, Hranjec M. Pharmaceuticals (BaseI). 2021 Oct 17. 14(10):1052. doi: 10.3390/ph14101052.
Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, And Molecular Modeling Studies.
Huang B, Ginex T, Luque FJ, Jiang X, Gao P, Zhang J, Kang D, Daelemans D, De Clerq E, Pannecouque C, Zhan P, Liu X.
J Med Chem. 2021 Sep 23. 64(18):13604-13621. doi: 10.1021/acs.jmedchem.1c00987.
Cellular host factors for SARS-CoV-2 infection.
Baggen J, Vanstreels E, Jansen S, Daelemans D. Nat Microbiol. 2021 Oct;6(10):1219-1232. doi: 10.1038/s41564-021-00958-0. PMID: 34471255 Review.
Preparation of Antiproliferative Terpene-Alkaloid Hybrids by Free Radical-Mediated Modification of ent-Kauranic Derivatives.
Pruteanu E, Gîrbu V, Ungur N, Persoons L, Daelemans D, Renaud P, Kulcițki V. Molecules. 2021 Jul 28. 26(15):4549. doi: 10.3390/molecules26154549.
Antibacterial and antitumoral properties of 1,2,3-triazolo fused triterpenes and their mechanism of inhibiting the proliferation of HL-60 cells.
Wang R, Li Y, Hu H, Persoons L, Daelemans D, De Jonghe S, Luyten W, Krasniqi B, Dehaen W.
Eur J Med Chem. 2021 Nov 15. 224:113727. doi: 10.1016/j.ejmech.2021.113727.
Discovery of ( ±)-3-(1H-pyrazol-1-yl)-6,7-dihydro-5H-[1,2,4]triazolo[3,4-b][1,3,4] thiadiazine derivatives with promising in vitro anticoronavirus and antitumoral activity.
Jilloju PC, Persoons L, Kurapati SK, Schols D, De Jonghe S, Daelemans D, Vedula RR. Mol Divers. 2022 Jun. 26(3):1357-1371. doi: 10.1007/s11030-021-10258-8.
Benzofuranyl-2-imidazoles as imidazoline I(2) receptor ligands for Alzheimer’s disease.
Rodriguez-Arévalo S, Bagán A, Griñán-Ferré C, Vasilopoulou F, Pallàs M, Brocos-Mosquera I, Callado LF, Loza MI, Martínez AL, Brea J, Pérez B, Molins E, De Jonghe S, Daelemans D, Radan M, Djikic T, Nikolic K, Hernández-Hernández E, García-Fuster MJ, García-Sevilla JA, Escolano C.
Eur J Med Chem. 2021 Oct 15. 222:113540. doi: 10.1016/j.ejmech.2021.113540.
Genome-wide CRISPR screening identifies TMEM106B as a proviral host factor for SARS-CoV-2.
Baggen J, Persoons L, Vanstreels E, Jansen S, Van Looveren D, Boeckx B, Geudens V, De Man J, Jochmans D, Wauters J, Wauters E, Vanaudenaerde BM, Lambrechts D, Neyts J, Dallmeier K, Thibaut HJ, Jacquemyn M, Maes P, Daelemans D. Nat Genet. 2021 doi: 10.1038/s41588-021-00805-2
Quantitative Nucleocytoplasmic Transport Assays in Cellular Models of Neurodegeneration.
Vanneste J, Vercruysse T, Van Damme P, Van Den Bosch L, Daelemans D. Bio Protoc. 2020 Jun 20. 10(12):e3659. doi: 10.21769/BioProtoc.3659.
Intermedilysin cytolytic activity depends on heparan sulfates and membrane composition.
Drabavicius G, Daelemans D. PLoS Genet. 2021 doi: 10.1371/journal.pgen.1009387
XPO1 inhibitors represent a novel therapeutic option in Adult T-cell Leukemia, triggering p53-mediated caspase-dependent apoptosis.
Boons E, Nogueira TC, Dierckx T, Menezes SM, Jacquemyn M, Tamir S, Landesman Y, Farré L, Bittencourt A, Kataoka K, Ogawa S, Snoeck R, Andrei G, Van Weyenbergh J, Daelemans D. Blood Cancer J. 2021 doi: 10.1038/s41408-021-00409-3.
Synthesis, in silico ADME, molecular docking and in vitro cytotoxicity evaluation of stilbene linked 1,2,3-triazoles.
Das A, Kumar S, Persoons L, Daelemans D, Schols D, Alici H, Tahtaci H, Karki SS. Heliyon. 2021 Jan 30. 7(1):e05893. doi: 10.1016/j.heliyon.2020.e05893.
Loss of tRNA-modifying enzyme Elp3 activates a p53-dependent antitumor checkpoint in hematopoiesis.
Rosu A, El Hachem N, Rapino F, Rouault-Pierre K, Jorssen J, Somja J, Ramery E, Thiry M, Nguyen L, Jacquemyn M, Daelemans D, Adams CM, Bonnet D, Chariot A, Close P, Bureau F, Desmet CJ. J Exp Med. 2021 Mar 1. 218(3):e20200662. doi: 10.1084/jem.20200662.
Neggers JE, Jacquemyn M, Dierckx T, Kleinstiver BP, Thibaut HJ, Daelemans D. Mol Ther. 2021 doi: 10.1016/j.ymthe.2020.09.025
Antibacterial and antitumoral properties of 1,2,3-triazolo fused triterpenes and their mechanism of inhibiting the proliferation of HL-60 cells.
Wang R, Li Y, Hu H, Persoons L, Daelemans D, De Jonghe S, Luyten W, Krasniqi B, Dehaen W.
Eur J Med Chem. 2021 Nov 15. 224:113727. doi: 10.1016/j.ejmech.2021.113727.
Discovery of ( ±)-3-(1H-pyrazol-1-yl)-6,7-dihydro-5H-[1,2,4]triazolo[3,4-b][1,3,4] thiadiazine derivatives with promising in vitro anticoronavirus and antitumoral activity.
Jilloju PC, Persoons L, Kurapati SK, Schols D, De Jonghe S, Daelemans D, Vedula RR. Mol Divers. 2022 Jun. 26(3):1357-1371. doi: 10.1007/s11030-021-10258-8.
Benzofuranyl-2-imidazoles as imidazoline I(2) receptor ligands for Alzheimer’s disease.
Rodriguez-Arévalo S, Bagán A, Griñán-Ferré C, Vasilopoulou F, Pallàs M, Brocos-Mosquera I, Callado LF, Loza MI, Martínez AL, Brea J, Pérez B, Molins E, De Jonghe S, Daelemans D, Radan M, Djikic T, Nikolic K, Hernández-Hernández E, García-Fuster MJ, García-Sevilla JA, Escolano C.
Eur J Med Chem. 2021 Oct 15. 222:113540. doi: 10.1016/j.ejmech.2021.113540.
Genome-wide CRISPR screening identifies TMEM106B as a proviral host factor for SARS-CoV-2.
Baggen J, Persoons L, Vanstreels E, Jansen S, Van Looveren D, Boeckx B, Geudens V, De Man J, Jochmans D, Wauters J, Wauters E, Vanaudenaerde BM, Lambrechts D, Neyts J, Dallmeier K, Thibaut HJ, Jacquemyn M, Maes P, Daelemans D. Nat Genet. 2021 doi: 10.1038/s41588-021-00805-2
Quantitative Nucleocytoplasmic Transport Assays in Cellular Models of Neurodegeneration.
Vanneste J, Vercruysse T, Van Damme P, Van Den Bosch L, Daelemans D. Bio Protoc. 2020 Jun 20. 10(12):e3659. doi: 10.21769/BioProtoc.3659.
Intermedilysin cytolytic activity depends on heparan sulfates and membrane composition.
Drabavicius G, Daelemans D. PLoS Genet. 2021 doi: 10.1371/journal.pgen.1009387
XPO1 inhibitors represent a novel therapeutic option in Adult T-cell Leukemia, triggering p53-mediated caspase-dependent apoptosis.
Boons E, Nogueira TC, Dierckx T, Menezes SM, Jacquemyn M, Tamir S, Landesman Y, Farré L, Bittencourt A, Kataoka K, Ogawa S, Snoeck R, Andrei G, Van Weyenbergh J, Daelemans D. Blood Cancer J. 2021 doi: 10.1038/s41408-021-00409-3.
Synthesis, in silico ADME, molecular docking and in vitro cytotoxicity evaluation of stilbene linked 1,2,3-triazoles.
Das A, Kumar S, Persoons L, Daelemans D, Schols D, Alici H, Tahtaci H, Karki SS. Heliyon. 2021 Jan 30. 7(1):e05893. doi: 10.1016/j.heliyon.2020.e05893.
Loss of tRNA-modifying enzyme Elp3 activates a p53-dependent antitumor checkpoint in hematopoiesis.
Rosu A, El Hachem N, Rapino F, Rouault-Pierre K, Jorssen J, Somja J, Ramery E, Thiry M, Nguyen L, Jacquemyn M, Daelemans D, Adams CM, Bonnet D, Chariot A, Close P, Bureau F, Desmet CJ. J Exp Med. 2021 Mar 1. 218(3):e20200662. doi: 10.1084/jem.20200662.
enAsCas12a Enables CRISPR-Directed Evolution to Screen for Functional Drug Resistance Mutations in Sequences Inaccessible to SpCas9.
Neggers JE, Jacquemyn M, Dierckx T, Kleinstiver BP, Thibaut HJ, Daelemans D. Mol Ther. 2021 doi: 10.1016/j.ymthe.2020.09.025
Correction to Bicyclic a-Iminophosphonates as High Affinity Imidazoline I(2) Receptor Ligands for Alzheimer’s Disease.
Abas S, Rodriguez-Arevalo S, Bagan A, Grinan-Ferré C, Vasilopoulou F, Brocos-Mosquera I, Muguruza C, Pérez B, Molins E, Luque FJ, Pérez Lozano, De Jonghe S, Daelemans D, Naesens L, Brea J, Loza MI, Hernandez-Hernandez E, Garcia-Sevilla JA, Garcia-Fuster MJ, Radan M, Djikic T, Nikolic K, Pallas M, Callado LF, Escolano C.
J Med Chem. 2020 Sep 24. 63(18)10529. doi: 10.1021/acs.jmedchem.0c01324.
Design, synthesis and biological evaluation of pyrazolo[3,4-d]pyrimidine-based protein kinase D inhibitors.
Gilles P, Kashyap RS, Freitas MJ, Ceusters S, Van Asch K, Janssens A, de Jonghe S, Persoons L, Cobbaut M, Daelemans D, Van Lint J, Voet ARD, De Borggraeve WM.
Eur J Med Chem. 2020 Nov 1. 11(8):1605-1610. doi: 10.1021/acsmedchemlett.0c00269.
Synthesis of Novel Nitroxoloine Analogs with Potent Cathepsin B Exopeptidase Inhibitory Activity.
Van de Walle T, Briand M, Mitrovic A, Sosic I, Gobec S, Kos J, Persoons L, Daelemans D, de Jonghe S, Ubiparip Z, Desmet T, Van Hecke K, Mangelinckx S, D’hooghe M.
ChemMedChem. 2020 Dec 15. 15(24):2477-2490.doi: 10.1002/cmdc.202000402.
Design, synthesis, and biological evaluation of piperidinyl-substituted [1,2,4]triazolo[1,5-a]pyrimidine derivatives as potential anti-HIV-1 agents with reduced cytotoxicity.
Huang B, Kang D, Tian Y, Daelemans D, De Clerc E, Pannecouque C, Zhan P, Liu X, Chem Biol Drug Des. 2021 Jan. 97(1):67-76. doi: 10.1111/cbdd.13760.
Drug repurposing: phosphate prodrugs of anticancer and antiviral FDA-approved nucleosides as novel antimicrobials.
Pertusati F, Pileggi E, Richards J, Wootton M, Van Leemputte T, Persoons L, De Coster D, Villanueva X, Daelemans D, Steenackers H, McGuigan C, Serpi M.
J Antimicrob Chemother. 2020 Oct 1. 75(10):2864-2878. doi: 10.1093/jac/dkaa268.
Discovery of potential dual-target prodrugs of HIV-1 reverse transcriptase and nucleocapsid protein 7.
Sun S, Huang B, Li Z, Wang Z, Sun L, Gao P, Kang D, Chen CH, Lee KH, Daelemans D, De Clercq E, Pannecouque C, Zhan P, Liu X.
Bioorg Med Chem Lett. 2020 Aug 15. 30(16):127287. doi: 10.1016/j.bmcl.2020.127287.
Bicyclic α-Iminophosphonates as High Affinity Imidazoline I(2) Receptor Ligands for Alzheimer’s Disease.
Abás S, Rodríguez-Arévalo S, Bagán A, Griñán-Ferré C, Vasilopoulou F, Brocos-Mosquera I, Muguruza C, Pérez B, Molins E, Luque FJ, Pérez-Lozano P, de Jonghe S, Daelemans D, Naesens L, Brea J, Loza MI, Hernández-Hernández E, García-Sevilla JA, García-Fuster MJ, Radan M, Djikic T, Nikolic K, Pallàs M, Callado LF, Escolano C.
J Med Chem. 2020 Apr 9. 63(7):3610-3633. doi: 10.1021/acs.jmedchem.9b02080.
Iron/Copper Co-Catalyzed Cross-Coupling Reaction for the Synthesis of 6-Substituted 7-Deazapurines and the Corresponding Nucleosides.
Li Q, Persoons L, Daelemans D, Herdewijn P. J Org Chem. 2020 Jan 17. 85(2):403-418. doi: 10.1021/acs.joc.9b02414.
Preclinical Assessment with Clinical Validation of Selinexor with Gemcitabine and Nab-Paclitaxel for the Treatment of Pancreatic Ductal Adenocarcinoma.
Azmi AS, Khan HY, Muqbil I, Aboukameel A, Neggers JE, Daelemans D, Mahipal A, Dyson G, Kamgar M, Al-Hallak MN, Tesfaye A, Kim S, Shidham V, M Mohammad R, Philip PA. Clin Cancer Res. 2020 Mar 15. 26(6):1338-1348. doi: 10.1158/1078-0432.CCR-19-1728.
Drug repurposing: phosphate prodrugs of anticancer and antiviral FDA-approved nucleosides as novel antimicrobials.
Pertusati F, Pileggi E, Richards J, Wootton M, Van Leemputte T, Persoons L, De Coster D, Villanueva X, Daelemans D, Steenackers H, McGuigan C, Seri M.
J Antimicrob Chemother. 2020 Oct 1. 75(10):2864-2878. doi:10.1093/jac/dkaa268.
ATXN1 repeat expansions confer risk for amyotrophic lateral sclerosis and contribute to TDP-43 mislocalization.
Tazelaar GHP, Boeynaems S, De Decker M, van Vugt JJFA, Kool L, Goedee HS, McLaughlin RL, Sproviero W, Iacoangeli A, Moisse M, Jacquemyn M, Daelemans D, Dekker AM, van der Spek RA, Westeneng HJ, Kenna KP, Assialioui A, Da Silva N; Project MinE ALS Sequencing Consortium; Povedano M, Pardina JSM, Hardiman O, Salachas F, Millecamps S, Vourc’h P, Corcia P, Couratier P, Morrison KE, Shaw PJ, Shaw CE, Pasterkamp RJ, Landers JE, Van Den Bosch L, Robberecht W, Al-Chalabi A, van den Berg LH, Van Damme P, Veldink JH, van Es MA. Brain Commun. 2020 May 19;2(2):fcaa064. doi: 10.1093/braincomms/fcaa064.
Discovery of potential dual-target prodrugs of HIV-1 reverse transcriptase and nucleocapsid protein 7.
Sun S, Huang B, Li Z, Wang Z, Sun L, Gao P, Kang D, Chen CH, Lee KH, Daelemans D, De Clercq E, Pannecouque C, Zhan P, Liu X.
Bioorg Med Chem Lett. 2020 Aug 15. 30(16):127287. doi:10.1016/j.bmcl.2020.127287.
Bicyclic a-Iminophosphonates as High Affinity Imidazoline I(2) Receptor Ligands for Alzheimer’s Disease.
Abas S, Rodriguez-Arevalo S, Bagan A, Grinan-Ferre C, Vasilopoulou F, Brocos-Mosequera I, Muguruza C, Perez B, Molins E, Luque FJ, Perez-Lozano P, de Jonghe S, Daelemans D, Naesens L, Brea J, Loza MI, Hernandez-Hernandez E, Garcia-Sevilla JA, Garcia-Fuster MJ, Radan M, Djikic T, Nikolic K, Pallas M, Callado LF, Escolano C.
J Med Chem. 2020 Apr 9.63(7)3610-3633. doi:10.1021/acs.jmedchem.9b02080.
Iron/Copper Co-Catalyzed Cross-Coupling Reaction for the Synthesis of 6-Substituted 7-Deazapurines and the Corresponding Nucleosides.
Li Q, Persoons L, Daelemans D, Herdewijn P.
J Org Chem. 2020 Jan 17. 85(2):403-418. doi:10.1021/acs.joc.9b02414.
Quantitative Nucleocytoplasmic Transport Assays in Cellular Models of Neurodegeneration.
Vanneste J, Vercruysse T, Van Damme P, Van Den Bosch L, Daelemans D.
Bio Proto. 2020 Jun 20. 10(12):e3659. doi:10.21769/BioProtoc.3659.
Preclinical Assessment with Clinival Validation of Selinexor with Gemcitabine and Nab-Paclitaxel for the Treatmet of Pancreatic Ductal Adenocarcinoma.
Azmi AS, Khan HY, Muqbil I, Aboukameel A, Negger JE, Daelemans D, Mahipal A, Dyson G, Kamgar M, AI-Hallak MN, Tefaye A, Kim S, Shidham V, M Mohammad R, Philip PA.
Clin Cancer Res. 2020 Mar 15. 26(6):1338-1348. doi:10.1158/1078-0432.CCR-19-1728.
Design and Synthesis of New 6-Nitro and 6-Amina-3,3a,4,5-Tetrahydro-2H-Benzo[g]indazole Derivatives: Antiproliferative and Antibacterial Activity.
Cuartas V, Crespo MDP, Priego EM, Persoons L, Daelemans D, Camarasa MJ, Insuasty B, Perez-Perez MJ.
Molecules 2019 Nov 21. 24(23):4236. doi:10.3390/moleculs24234236.
C9orf72-generated poly-GR and poly-PR do not directly interfere with nucleocytoplasmic transport.
Vanneste J, Vercruysse T, Boeynaems S, Sicart A, Van Damme P, Daelemans D, Van Den Bosch L.
Sci Rep. 2019 Oct 31. 9(1):15728. doi:10.1038/s41598-019-52035-6.
STK38 kinase acts as XPO1 gatekeeper regulating the nuclear export of autophagy proteins and other cargoes.
Martin AP, Jacquemyn M, Lipecka J, Chhuon C, Aushev VN, Meunier B, Singh MK, Carpi N, Piel M, Codogno P, Hergovich A, Parrini MC, Zalcman G, Guerrera IC, Daelemans D, Camonis JH.
EMBO Rep. 2019 Nov 5. 20(11):e48150. doi:10.15252/embr.201948150.
Xylo-C-nucleosides with a pyrrolo[2,1-f][1,2,4]triazin-4-amine hetrocyclic base: Synthesis and antiproliferative properties.
Nie P, Groaz E, Daelemans D, Herdewijn P.
Bioorg Med Chem Lett. 2019 Jun 15. 29(12):1450-1453. doi:10.1016/j.bmcl.2019.04.023.
Exploiting the Tolerant Region I of the Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI) Binding Pocket: Discovery of Potent Diarylpyrimidine-Typed HIV-1 NNRTIs against Wild-Type and E138K Mutant Virus with Significantly Improved Water Solubility and Favorable Safety Profiles.
Huang B, Chen W, Zhao T, Li Z, Jiang X, Ginex T, Vílchez D, Luque FJ, Kang D, Gao P, Zhang J, Tian Y, Daelemans D, De Clercq E, Pannecouque C, Zhan P, Liu X.
J Med Chem. 2019 Feb 28. 62(4):2083-2098. doi: 10.1021/acs.jmedchem.8b01729.
Design, synthesis and biological evaluation of novel acetamide-substituted doravirine and its prodrugs as potent HIV-1 NNRTIs.
Wang Z, Yu Z, Kang D, Zhang J, Tian Y, Daelemans D, De Clercq E, Pannecouque C, Zhan P, Liu X.
Bioorg Med Chem. 2019 Feb 1. 27(3):447-456. doi: 10.1016/j.bmc.2018.12.039.
Down-regulation of AR splice variants through XPO1 suppression contributes to the inhibition of prostate cancer progression.
Aboukameel A, Muqbil I, Baloglu E, Senapedis W, Landesman Y, Argueta C, Kauffman M, Chang H, Kashyap T, Shacham S, Neggers JE, Daelemans D, Heath EI, Azmi AS. Oncotarget. 2018 Oct 19. 9(82):35327-35342. doi: 10.18632/oncotarget.26239.
Discovery of potent HIV-1 non-nucleoside reverse transcriptase inhibitors by exploring the structure-activity relationship of solvent-exposed regions I.
Kang D, Wang Z, Chen M, Feng D, Wu G, Zhou Z, Jing L, Zuo X, Jiang X, Daelemans D, De Clercq E, Pannecouque C, Zhan P, Liu X.
Chem Biol Drug Des. 2019 Apr. 93(4):430-437. doi: 10.1111/cbdd.13429.
Exploiting the Tolerant Region I of the Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI) Binding Pocket: Discovery of Potent Diarylpyrimidine-Typed HIV-1 NNRTIs against Wild-Type and E138K Mutant Virus with Significantly Improved Water Solubility and Favorable Safety Profiles.
Huang B, Chen W, Zhao T, Li Z, Jiang X, Ginex T, Vílchez D, Luque FJ, Kang D, Gao P, Zhang J, Tian Y, Daelemans D, De Clercq E, Pannecouque C, Zhan P, Liu X.
J Med Chem. 2019 Feb 28. 62(4):2083-2098. doi: 10.1021/acs.jmedchem.8b01729.
Design, synthesis and biological evaluation of novel acetamide-substituted doravirine and its prodrugs as potent HIV-1 NNRTIs.
Wang Z, Yu Z, Kang D, Zhang J, Tian Y, Daelemans D, De Clercq E, Pannecouque C, Zhan P, Liu X.
Bioorg Med Chem. 2019 Feb 1. 27(3):447-456. doi: 10.1016/j.bmc.2018.12.039.
Down-regulation of AR splice variants through XPO1 suppression contributes to the inhibition of prostate cancer progression.
Aboukameel A, Muqbil I, Baloglu E, Senapedis W, Landesman Y, Argueta C, Kauffman M, Chang H, Kashyap T, Shacham S, Neggers JE, Daelemans D, Heath EI, Azmi AS. Oncotarget. 2018 Oct 19. 9(82):35327-35342. doi: 10.18632/oncotarget.26239.
Discovery of potent HIV-1 non-nucleoside reverse transcriptase inhibitors by exploring the structure-activity relationship of solvent-exposed regions I.
Kang D, Wang Z, Chen M, Feng D, Wu G, Zhou Z, Jing L, Zuo X, Jiang X, Daelemans D, De Clercq E, Pannecouque C, Zhan P, Liu X.
Chem Biol Drug Des. 2019 Apr. 93(4):430-437. doi: 10.1111/cbdd.13429.
Design, synthesis and antiviral evaluation of novel hydrazone-substituted thiophene[3,2-d]pyrimidine derivatives as potent human immunodeficiency virus-1 inhibitors.
Wang Z, Kang D, Chen M, Wu G, Feng D, Zhao T, Zhou Z, Huo Z, Jing L, Zuo X, Daelemans D, De Clercq E, Pannecouque C, Zhan P, Liu X.
Chem Biol Drug Des. 2018 Dec. 92(6):2009-2021. doi:10.1111/cbdd.13373.
Targeting the XPO1-dependent nuclear export of E2F7 reverses anthracycline resistance in head and neck squamous cell carcinomas.
Saenz-Ponce N, Pillay R, de Long LM, Kashyap T, Argueta C, Landesman Y, Hazar-Rethinam M, Boros S, Panizza B, Jacquemyn M, Daelemans D, Gannon OM, Saunders NA.
Sci Transl Med. 2018 Jun 27. 10(447):eaar7223. doi: 10.1126/scitranslmed.aar7223.
Targeting the XPO1-dependent nuclear export of E2F7 reverses anthracycline resistance in head and neck squamous cell carcinomas.
Saenz-Ponce N, Pillay R, de Long LM, Kashyap T, Argueta C, Landesman Y, Hazar-Rethinam M, Boros S, Panizza B, Jacquemyn M, Daelemans D, Gannon OM, Saunders NA.
Sci Transl Med. 2018 Jun 27. 10(447):eaar7223. doi: 10.1126/scitranslmed.aar7223.
5-Hydroxypyrido[2,3-b]pyrazin-6(5H)-one derivatives as novel dual inhibitors of HIV-1 reverse transcriptase-associated ribonuclease H and integrase.
Sun L, Gao P, Dong G, Zhang X, Cheng X, Ding X, Wang X, Daelemans D, De Clercq E, Pannecouque C, Menéndez-Arias L, Zhan P, Liu X.
Eur J Med Chem. 2018 Jul 15. 155:714-724. doi: 10.1016/j.ejmech.2018.06.036.
Further Exploring Solvent-Exposed Tolerant Regions of Allosteric Binding Pocket for Novel HIV-1 NNRTIs Discovery.
Kang D, Wang Z, Zhang H, Wu G, Zhao T, Zhou Z, Huo Z, Huang B, Feng D, Ding X, Zhang J, Zuo X, Jing L, Luo W, Guma S, Daelemans D, Clercq E, Pannecouque C, Zhan P, Liu X.
ACS Med Chem Lett. 2018 Mar 1. 9(4):370-375. doi: 10.1021/acsmedchemlett.8b00054.
Discovery of Novel Diarylpyrimidine Derivatives as Potent HIV-1 NNRTIs Targeting the “”NNRTI Adjacent”” Binding Site.
Huo Z, Zhang H, Kang D, Zhou Z, Wu G, Desta S, Zuo X, Wang Z, Jing L, Ding X, Daelemans D, De Clercq E, Pannecouque C, Zhan P, Liu X.
ACS Med Chem Lett. 2018 Feb 27. 9(4):334-338. doi: 10.1021/acsmedchemlett.7b00524.
Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
Tian Y, Liu Z, Liu J, Huang B, Kang D, Zhang H, De Clercq E, Daelemans D, Pannecouque C, Lee KH, Chen CH, Zhan P, Liu X.
Eur J Med Chem. 2018 May 10. 151:339-350. doi: 10.1016/j.ejmech.2018.03.059.
Near-native, site-specific and purification-free protein labeling for quantitative protein interaction analysis by MicroScale Thermophoresis.
Bartoschik T, Galinec S, Kleusch C, Walkiewicz K, Breitsprecher D, Weigert S, Muller YA, You C, Piehler J, Vercruysse T, Daelemans D, Tschammer N.
Sci Rep. 2018 Mar 21. 8(1):4977. doi: 10.1038/s41598-018-23154-3.
The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2.
Lu X, Yang J, Kang D, Gao P, Daelemans D, De Clercq E, Pannecouque C, Zhan P, Liu X. Bioorg Med Chem. 2018 May 1. 26(8):2051-2060. doi: 10.1016/j.bmc.2018.03.003.
First discovery of a potential carbonate prodrug of NNRTI drug candidate RDEA427 with submicromolar inhibitory activity against HIV-1 K103N/Y181C double mutant strain.
Huang B, Liu X, Tian Y, Kang D, Zhou Z, Daelemans D, De Clercq E, Pannecouque C, Zhan P, Liu X.
Bioorg Med Chem Lett. 2018 May 1. 28(8):1348-1351. doi: 10.1016/j.bmcl.2018.03.012.
Target identification of small molecules using large-scale CRISPR-Cas mutagenesis scanning of essential genes.
Neggers JE, Kwanten B, Dierckx T, Noguchi H, Voet A, Bral L, Minner K, Massant B, Kint N, Delforge M, Vercruysse T, Baloglu E, Senapedis W, Jacquemyn M, Daelemans D. Nat Comm. 2018
Discovery of novel diarylpyrimidines as potent HIV-1 NNRTIs by investigating the chemical space of a less explored “hydrophobic channel”.
Zhou Z, Liu T, Kang D, Huo Z, Wu G, Daelemans D, De Clercq E, Pannecouque C, Zhan P, Liu X. Org Biomol Chem. 2018 Feb 7. 16(6):1014-1028. doi: 10.1039/c7ob02828h.
To disinfect or not to disinfect in postharvest research on the fungal decay of apple?
Naets M, van Dael M, Vanstreels E, Daelemans D, Verboven P, Nicolaï B, Keulemans W, Geeraerd A.
Int J Food Microbiol. 2018 Feb 2. 266:190-199. doi: 10.1016/j.ijfoodmicro.2017.12.003.
Synthesis and Biological Evaluation of Pyrrolo[2,1-f][1,2,4]triazine C-Nucleosides with a Ribose, 2′-Deoxyribose, and 2′,3′-Dideoxyribose Sugar Moiety.
Li Q, Lescrinier E, Groaz E, Persoons L, Daelemans D, Herdewijn P, De Jonghe S. ChemMedChem. 2018 Jan 8. 13(1):97-104. doi: 10.1002/cmdc.201700657.
Discovery of Novel Diarylpyrimidine Derivatives as Potent HIV-1 NNRTIs Targeting the “”NNRTI Adjacent”” Binding Site.
Huo Z, Zhang H, Kang D, Zhou Z, Wu G, Desta S, Zuo X, Wang Z, Jing L, Ding X, Daelemans D, De Clercq E, Pannecouque C, Zhan P, Liu X.
ACS Med Chem Lett. 2018 Feb 27. 9(4):334-338. doi: 10.1021/acsmedchemlett.7b00524.
Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
Tian Y, Liu Z, Liu J, Huang B, Kang D, Zhang H, De Clercq E, Daelemans D, Pannecouque C, Lee KH, Chen CH, Zhan P, Liu X.
Eur J Med Chem. 2018 May 10. 151:339-350. doi: 10.1016/j.ejmech.2018.03.059.
Near-native, site-specific and purification-free protein labeling for quantitative protein interaction analysis by MicroScale Thermophoresis.
Bartoschik T, Galinec S, Kleusch C, Walkiewicz K, Breitsprecher D, Weigert S, Muller YA, You C, Piehler J, Vercruysse T, Daelemans D, Tschammer N.
Sci Rep. 2018 Mar 21. 8(1):4977. doi: 10.1038/s41598-018-23154-3.
The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2.
Lu X, Yang J, Kang D, Gao P, Daelemans D, De Clercq E, Pannecouque C, Zhan P, Liu X. Bioorg Med Chem. 2018 May 1. 26(8):2051-2060. doi: 10.1016/j.bmc.2018.03.003.
First discovery of a potential carbonate prodrug of NNRTI drug candidate RDEA427 with submicromolar inhibitory activity against HIV-1 K103N/Y181C double mutant strain.
Huang B, Liu X, Tian Y, Kang D, Zhou Z, Daelemans D, De Clercq E, Pannecouque C, Zhan P, Liu X.
Bioorg Med Chem Lett. 2018 May 1. 28(8):1348-1351. doi: 10.1016/j.bmcl.2018.03.012.
Target identification of small molecules using large-scale CRISPR-Cas mutagenesis scanning of essential genes.
Neggers JE, Kwanten B, Dierckx T, Noguchi H, Voet A, Bral L, Minner K, Massant B, Kint N, Delforge M, Vercruysse T, Baloglu E, Senapedis W, Jacquemyn M, Daelemans D. Nat Comm. 2018
Discovery of novel diarylpyrimidines as potent HIV-1 NNRTIs by investigating the chemical space of a less explored “hydrophobic channel”.
Zhou Z, Liu T, Kang D, Huo Z, Wu G, Daelemans D, De Clercq E, Pannecouque C, Zhan P, Liu X. Org Biomol Chem. 2018 Feb 7. 16(6):1014-1028. doi: 10.1039/c7ob02828h.
To disinfect or not to disinfect in postharvest research on the fungal decay of apple?
Naets M, van Dael M, Vanstreels E, Daelemans D, Verboven P, Nicolaï B, Keulemans W, Geeraerd A.
Int J Food Microbiol. 2018 Feb 2. 266:190-199. doi: 10.1016/j.ijfoodmicro.2017.12.003.
Synthesis and Biological Evaluation of Pyrrolo[2,1-f][1,2,4]triazine C-Nucleosides with a Ribose, 2′-Deoxyribose, and 2′,3′-Dideoxyribose Sugar Moiety.
Li Q, Lescrinier E, Groaz E, Persoons L, Daelemans D, Herdewijn P, De Jonghe S. ChemMedChem. 2018 Jan 8. 13(1):97-104. doi: 10.1002/cmdc.201700657.
Discovery of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 NNRTIs Targeting the Tolerant Region I of NNIBP.
Kang D, Ding X, Wu G, Huo Z, Zhou Z, Zhao T, Feng D, Wang Z, Tian Y, Daelemans D, De Clercq E, Pannecouque C, Zhan P, Liu X.
ACS Med Chem Lett. 2017 Oct 19. 8(11):1188-1193. doi: 10.1021/acsmedchemlett.7b00361.
Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives as potent HIV-1 NNRTIs.
Liu Z, Tian Y, Liu J, Huang B, Kang D, De Clercq E, Daelemans D, Pannecouque C, Zhan P, Liu X.
Eur J Med Chem. 2017 Nov 10. 140:383-391. doi: 10.1016/j.ejmech.2017.07.012.
Comparative study of the organisation and phenotypes of bladder interstitial cells in human, mouse and rat.
Gevaert T, Neuhaus J, Vanstreels E, Daelemans D, Everaerts W, Der Aa FV, Timmermans JP, Roskams T, Steiner C, Pintelon I, De Ridder D.
Cell Tissue Res. 2017 Dec. 370(3):403-416. doi: 10.1007/s00441-017-2694-9.
Discovery of novel DAPY-IAS hybrid derivatives as potential HIV-1 inhibitors using molecular hybridization based on crystallographic overlays.
Huang B, Wang X, Liu X, Chen Z, Li W, Sun S, Liu H, Daelemans D, De Clercq E, Pannecouque C, Zhan P, Liu X.
Bioorg Med Chem. 2017 Aug 15. 25(16):4397-4406. doi: 10.1016/j.bmc.2017.06.022.
Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
Kang D, Fang Z, Huang B, Lu X, Zhang H, Xu H, Huo Z, Zhou Z, Yu Z, Meng Q, Wu G, Ding X, Tian Y, Daelemans D, De Clercq E, Pannecouque C, Zhan P, Liu X.
J Med Chem. 2017 May 25. 60(10):4424-4443. doi: 10.1021/acs.jmedchem.7b00332.
Phase Separation of C9orf72 Dipeptide Repeats Perturbs Stress Granule Dynamics.
Boeynaems S, Bogaert E, Kovacs D, Konijnenberg A, Timmerman E, Volkov A, Guharoy M, De Decker M, Jaspers T, Ryan VH, Janke AM, Baatsen P, Vercruysse T, Kolaitis RM, Daelemans D, Taylor JP, Kedersha N, Anderson P, Impens F, Sobott F, Schymkowitz J, Rousseau F, Fawzi NL, Robberecht W, Van Damme P, Tompa P, Van Den Bosch L.
Mol Cell. 2017 Mar 16. 65(6):1044-1055.e5. doi: 10.1016/j.molcel.2017.02.013.
The stem cell growth factor receptor KIT is not expressed on interstitial cells in bladder.
Gevaert T, Ridder D, Vanstreels E, Daelemans D, Everaerts W, Aa FV, Pintelon I, Timmermans JP, Roskams T, Steiner C, Neuhaus J.
J Cell Mol Med. 2017 Jun. 21(6):1206-1216. doi: 10.1111/jcmm.13054.
Structural Modifications of Diarylpyrimidine-quinolone Hybrids as Potent HIV-1 NNRTIs with an Improved Drug Resistance Profile.
Mao TQ, He QQ, Chen WX, Tang GF, Chen FE, De Clercq E, Daelemans D, Pannecouque C.
Curr Pharm Des. 2016. 22(46):6982-6987. doi: 10.2174/1381612823666161122125657.
The second-generation exportin-1 inhibitor KPT-8602 demonstrates potent activity against acute lymphoblastic leukemia.
Vercruysse T, De Bie J, Neggers J, Jacquemyn M, Vanstreels E, Schmid-Burgk JL, Hornung V, Baloglu E, Landesman Y, Senapedis W, Shacham S, Dagklis A, Cools J, Daelemans D. Clin Cancer Res. 2016 Oct 25.
Discovery of novel piperidine-substituted indolylarylsulfones as potent HIV NNRTIs via structure-guided scaffold morphing and fragment rearrangement.
Li X, Gao P, Huang B, Zhou Z, Yu Z, Yuan Z, Liu H, Pannecouque C, Daelemans D, De Clercq E, Zhan P, Liu X.
Eur J Med Chem. 2017 Jan 27. 126:190-201. doi: 10.1016/j.ejmech.2016.10.009.
XPO1-dependent nuclear export is a druggable vulnerability in KRAS-mutant lung cancer.
Kim J, McMillan E, Kim HS, Venkateswaran N, Makkar G, Rodriguez-Canales J, Villalobos P, Neggers JE, Mendiratta S, Wei S, Landesman Y, Senapedis W, Baloglu E, Chow CB, Frink RE, Gao B, Roth M, Minna JD, Daelemans D, Wistuba II, Posner BA, Scaglioni PP, White MA. Nature. 2016 Oct 6;538(7623):114-117
Heterozygous mutation of cysteine528 in XPO1 is sufficient for resistance to selective inhibitors of nuclear export.
Neggers JE, Vanstreels E, Baloglu E, Shacham S, Landesman Y, Daelemans D. Oncotarget. 2016 Oct 18;7(42):68842-68850.
Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.
Kang D, Fang Z, Li Z, Huang B, Zhang H, Lu X, Xu H, Zhou Z, Ding X, Daelemans D, De Clercq E, Pannecouque C, Zhan P, Liu X.
J Med Chem. 2016 Sep 8. 59(17):7991-8007. doi: 10.1021/acs.jmedchem.6b00738.
Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach.
Lu X, Li X, Yang J, Huang B, Kang D, Zhao F, Zhou Z, De Clercq E, Daelemans D, Pannecouque C, Zhan P, Liu X.
Bioorg Med Chem. 2016 Sep 15. 24(18):4424-4433. doi: 10.1016/j.bmc.2016.07.041.
Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket.
Chen W, Zhan P, Daelemans D, Yang J, Huang B, De Clercq E, Pannecouque C, Liu X. Eur J Med Chem. 2016 Oct 4. 121:352-363. doi: 10.1016/j.ejmech.2016.05.054.
Design, synthesis, and biological evaluation of novel 5-Alkyl-6-Adamantylmethylpyrimidin-4(3H)-ones as HIV-1 non-nucleoside reverse-transcriptase inhibitors.
Li W, Huang B, Kang D, De Clercq E, Daelemans D, Pannecouque C, Zhan P, Liu X. Chem Biol Drug Des. 2016 Sep. 88(3):380-5. doi: 10.1111/cbdd.12765.
L-Aspartic and l-glutamic acid ester-based ProTides of anticancer nucleosides: Synthesis and antitumoral evaluation.
Gao LJ, De Jonghe S, Daelemans D, Herdewijn P. Bioorg Med Chem Lett. 2016 May 1. 26(9):2142-6. doi: 10.1016/j.bmcl.2016.03.076.
Design, synthesis and evaluation of novel HIV-1 NNRTIs with dual structural conformations targeting the entrance channel of the NNRTI binding pocket.
Meng Q, Chen X, Kang D, Huang B, Li W, Zhan P, Daelemans D, De Clercq E, Pannecouque C, Liu X.
Eur J Med Chem. 2016 Jun 10. 115:53-62. doi: 10.1016/j.ejmech.2016.02.068.
The Oxygen Sensor PHD2 Controls Dendritic Spines and Synapses via Modification of Filamin A.
Segura I, Lange C, Knevels E, Moskalyuk A, Pulizzi R, Eelen G, Chaze T, Tudor C, Boulegue C, Holt M, Daelemans D, Matondo M, Ghesquière B, Giugliano M, Ruiz de Almodovar C, Dewerchin M, Carmeliet P.
Cell Rep. 2016 Mar 22. 14(11):2653-67. doi: 10.1016/j.celrep.2016.02.047.
Arylazolyl(azinyl)thioacetanilides: Part 19: Discovery of Novel Substituted Imidazo[4,5-b]pyridin-2-ylthioacetanilides as Potent HIV NNRTIs Via a Structure-based Bioisosterism Approach.
Li X, Huang B, Zhou Z, Gao P, Pannecouque C, Daelemans D, De Clercq E, Zhan P, Liu X. Chem Biol Drug Des. 2016 Aug. 88(2):241-53. doi: 10.1111/cbdd.12751.
Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket.
Yang J, Chen W, Kang D, Lu X, Li X, Liu Z, Huang B, Daelemans D, Pannecouque C, De Clercq E, Zhan P, Liu X.
Eur J Med Chem. 2016 Feb 15. 109:294-304. doi: 10.1016/j.ejmech.2015.11.039.
Human exportin-1 is a target for combined therapy of HIV and AIDS related lymphoma.
Boons E, Vanstreels E, Jacquemyn M, Nogueira TC, Neggers JE, Vercruysse T, van den Oord J, Tamir S, Shacahm S, Landesman Y, Snoeck R, Pannecouque C, Andrei G, Daelemans D. EBioMedicine. 2015 2:1102-1113
Design, Synthesis, and Biological Evaluation of Novel 2-(Pyridin-3-yloxy)acetamide Derivatives as Potential Anti-HIV-1 Agents.
Huang B, Li X, Zhan P, De Clercq E, Daelemans D, Pannecouque C, Liu X. Chem Biol Drug Des. 2016 Feb. 87(2):283-9. doi: 10.1111/cbdd.12657.
Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue.
Wan ZY, Yao J, Mao TQ, Wang XL, Wang HF, Chen WX, Yin H, Chen FE, De Clercq E, Daelemans D, Pannecouque C.
Eur J Med Chem. 2015 Sep 18. 102:215-22. doi: 10.1016/j.ejmech.2015.08.007.
Hybrid chemistry. Part 4: Discovery of etravirine-VRX-480773 hybrids as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
Wan ZY, Tao Y, Wang YF, Mao TQ, Yin H, Chen FE, Piao HR, De Clercq E, Daelemans D, Pannecouque C.
Bioorg Med Chem. 2015 Aug 1. 23(15):4248-4255. doi: 10.1016/j.bmc.2015.06.048.
Understanding the molecular mechanism of host-based statin resistance in hepatitis C virus replicon containing cells.
Delang L, Scheers E, Grabner M, Verpaalen B, Helsen N, Vanstreels E, Daelemans D, Verfaillie C, Neyts J.
Biochem Pharmacol. 2015 Aug 1. 96(3):190-201. doi: 10.1016/j.bcp.2015.06.003.
Discovery of piperidin-4-yl-aminopyrimidine derivatives as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
Wan ZY, Yao J, Tao Y, Mao TQ, Wang XL, Lu YP, Wang HF, Yin H, Wu Y, Chen FE, De Clercq E, Daelemans D, Pannecouque C.
Eur J Med Chem. 2015 Jun 5. 97:1-9. doi: 10.1016/j.ejmech.2015.04.050.
Anti-HIV diarylpyrimidine-quinolone hybrids and their mode of action.
Mao TQ, He QQ, Wan ZY, Chen WX, Chen FE, Tang GF, De Clercq E, Daelemans D, Pannecouque C.
Bioorg Med Chem. 2015 Jul 1. 23(13):3860-8. doi: 10.1016/j.bmc.2015.03.037.
Scaffold hopping: exploration of acetanilide-containing uracil analogues as potential NNRTIs.
Babkov DA, Valuev-Elliston VT, Paramonova MP, Ozerov AA, Ivanov AV, Chizhov AO, Khandazhinskaya AL, Kochetkov SN, Balzarini J, Daelemans D, Pannecouque C, Seley-Radtke KL, Novikov MS. Bioorg Med Chem. 2015 Mar 1. 23(5):1069-81. doi: 10.1016/j.bmc.2015.01.002.
Identifying Drug-Target Selectivity of Small-Molecule CRM1/XPO1 Inhibitors by CRISPR/Cas9 Genome Editing.
Neggers JE, Vercruysse T, Jacquemyn M, Vanstreels E, Baloglu E, Shacham S, Crochiere M, Landesman Y, Daelemans D. Chem Biol. 2015 Jan 8. pii: S1074-5521(14)00425-6.
Synthesis and biological evaluation of DAPY-DPEs hybrids as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
Wu HQ, Yao J, He QQ, Chen WX, Chen FE, Pannecouque C, De Clercq E, Daelemans D. Bioorg Med Chem. 2015 Feb 1. 23(3):624-31. doi: 10.1016/j.bmc.2014.11.032.
A stably expressed llama single-domain intrabody targeting Rev displays broad-spectrum anti-HIV activity.
Boons E, Li G, Vanstreels E, Vercruysse T, Pannecouque C, Vandamme AM, Daelemans D. Antiviral Res. 2014 Dec;112:91-102.
Exploiting the anti-HIV 6-desfluoroquinolones to design multiple ligands.
Sancineto L, Iraci N, Barreca ML, Massari S, Manfroni G, Corazza G, Cecchetti V, Marcello A, Daelemans D, Pannecouque C, Tabarrini O.
Bioorg Med Chem. 2014 Sep 1. 22(17):4658-66. doi: 10.1016/j.bmc.2014.07.018.
Anti-HIV-1 activity of the G-quadruplex ligand BRACO-19.
Perrone R, Butovskaya E, Daelemans D, Palù G, Pannecouque C, Richter SN. J Antimicrob Chemother. 2014 Dec. 69(12):3248-58. doi: 10.1093/jac/dku280.
Identification of different phenotypes of interstitial cells in the upper and deep lamina propria of the human bladder dome.
Gevaert T, Vanstreels E, Daelemans D, Franken J, Van Der Aa F, Roskams T, De Ridder D. J Urol. 2014 Nov. 192(5):1555-63. doi: 10.1016/j.juro.2014.05.096.
Dynamics of the ternary complex formed by c-Myc interactor JPO2, transcriptional co-activator LEDGF/p75, and chromatin.
Hendrix J, van Heertum B, Vanstreels E, Daelemans D, De Rijck J. J Biol Chem. 2014 May 2. 289(18):12494-506. doi: 10.1074/jbc.M113.525964.
HIV-1 Rev multimerization: mechanism and insights.
Vercruysse T, Daelemans D. Curr HIV Res. 2013 Dec;11(8):623-34.
Towards new C6-rigid S-DABO HIV-1 reverse transcriptase inhibitors: synthesis, biological investigation and molecular modeling studies.
Wu HQ, Yan ZH, Chen WX, He QQ, Chen FE, De Clercq E, Balzarini J, Daelemans D, Pannecouque C.
Bioorg Med Chem. 2013 Nov 1. 21(21):6477-83. doi: 10.1016/j.bmc.2013.08.040.
Role of PFKFB3-driven glycolysis in vessel sprouting.
De Bock K, Georgiadou M, Schoors S, Kuchnio A, Wong BW, Cantelmo AR, Quaegebeur A, Ghesquière B, Cauwenberghs S, Eelen G, Phng LK, Betz I, Tembuyser B, Brepoels K, Welti J, Geudens I, Segura I, Cruys B, Bifari F, Decimo I, Blanco R, Wyns S, Vangindertael J, Rocha S, Collins RT, Munck S, Daelemans D, Imamura H, Devlieger R, Rider M, Van Veldhoven PP, Schuit F, Bartrons R, Hofkens J, Fraisl P, Telang S, Deberardinis RJ, Schoonjans L, Vinckier S, Chesney J, Gerhardt H, Dewerchin M, Carmeliet P.
Cell. 2013 Aug 1. 154(3):651-63. doi: 10.1016/j.cell.2013.06.037.
Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors.
Yang S, Pannecouque C, Daelemans D, Ma XD, Liu Y, Chen FE, De Clercq E. Eur J Med Chem. 2013 Jul. 65:134-43. doi: 10.1016/j.ejmech.2013.04.052.
Mapping the binding interface between an HIV-1 inhibiting intrabody and the viral protein Rev.
Vercruysse T, Boons E, Venken T, Vanstreels E, Voet A, Steyaert J, De Maeyer M, Daelemans D. PLoS One. 2013;8(4)
Hemozoin induces lung inflammation and correlates with malaria-associated acute respiratory distress syndrome.
Deroost K, Tyberghein A, Lays N, Noppen S, Schwarzer E, Vanstreels E, Komuta M, Prato M, Lin JW, Pamplona A, Janse CJ, Arese P, Roskams T, Daelemans D, Opdenakker G, Van den Steen PE. Am J Respir Cell Mol Biol. 2013 May. 48(5):589-600. doi: 10.1165/rcmb.2012-0450OC.
Some hydrazones of 2-aroylamino-3-methylbutanohydrazide: synthesis, molecular modeling studies, and identification as stereoselective inhibitors of HIV-1.
Tatar E, Küçükgüzel I, Daelemans D, Talele TT, Kaushik-Basu N, De Clercq E, Pannecouque C.
Arch Pharm (Weinheim). 2013 Feb. 346(2):140-53. doi: 10.1002/ardp.201200311.
Synthesis, biological evaluation and molecular modeling of 4,6-diarylpyrimidines and diarylbenzenes as novel non-nucleosides HIV-1 reverse transcriptase inhibitors.
Ribone SR, Leen V, Madrid M, Dehaen W, Daelemans D, Pannecouque C, Briñón MC. Eur J Med Chem. 2012 Dec. 58:485-92. doi: 10.1016/j.ejmech.2012.10.036.
A phenyl-thiadiazolylidene-amine derivative ejects zinc from retroviral nucleocapsid zinc fingers and inactivates HIV virions.
Vercruysse T, Basta B, Dehaen W, Humbert N, Balzarini J, Debaene F, Sanglier-Cianférani S, Pannecouque C, Mély Y, Daelemans. Retrovirology. 2012 Nov 12;9:95.
Selective inhibitors of nuclear export show that CRM1/XPO1 is a target in chronic lymphocytic leukemia.
Lapalombella R, Sun Q, Williams K, Tangeman L, Jha S, Zhong Y, Goettl V, Mahoney E, Berglund C, Gupta S, Farmer A, Mani R, Johnson AJ, Lucas D, Mo X, Daelemans D, Sandanayaka V, Shechter S, McCauley D, Shacham S, Kauffman M, Chook YM, Byrd JC. Blood. 2012 Nov 29;120(23):4621-34.
CXCR4 chemokine receptor antagonists: nickel(II) complexes of configurationally restricted macrocycles.
Smith R, Huskens D, Daelemans D, Mewis RE, Garcia CD, Cain AN, Freeman TN, Pannecouque C, De Clercq E, Schols D, Hubin TJ, Archibald SJ.
Dalton Trans. 2012 Oct 7. 41(37):11369-77. doi: 10.1039/c2dt31137b.
Intracytoplasmic trapping of influenza virus by a lipophilic derivative of aglycoristocetin.
Vanderlinden E, Vanstreels E, Boons E, ter Veer W, Huckriede A, Daelemans D, Van Lommel A, Rőth E, Sztaricskai F, Herczegh P, Naesens L.
J Virol. 2012 Sep. 86(17):9416-31. doi: 10.1128/JVI.07032-11.
Computational investigation ofthe HIV-1 Rev multimerization using molecular dynamics simulations and binding free energy calculations.
Venken T, Daelemans D, De Maeyer M, Voet A. Proteins. 2012 Jun;80(6):1633-46.
A time-of-drug addition approach to target identification of antiviral compounds.
Daelemans D, Pauwels R, De Clercq E, Pannecouque C. Nat Protoc. 2011 Jun;6(6):925-33.
Selective inhibition of Human Immunodeficiency Virus type 1 (HIV-1) by a novel family of tricyclic nucleosides.
Bonache MC, Cordeiro A, Quesada E, Vanstreels E, Daelemans D, Camarasa MJ, Balzarini J, San-Félix A.
Antiviral Res. 2011 Oct. 92(1):37-44. doi: 10.1016/j.antiviral.2011.05.002.
Structural investigation of the naphthyridone scaffold: identification of a 1,6-naphthyridone derivative with potent and selective anti-HIV activity.
Tabarrini O, Massari S, Sancineto L, Daelemans D, Sabatini S, Manfroni G, Cecchetti V, Pannecouque C.
ChemMedChem. 2011 Jul 4. 6(7):1249-57. doi: 10.1002/cmdc.201100073.
Measuring cooperative Rev protein-protein interactions on Rev responsive RNA by fluorescence resonance energy transfer.
Vercruysse T, Pawar S, De Borggraeve W, Pardon E, Pavlakis GN, Pannecouque C, Steyaert J, Balzarini J, Daelemans D. RNA Biol. 2011 Mar-Apr;8(2):316-24.
Studies of anti-HIV transcription inhibitor quinolones: identification of potent N1-vinyl derivatives.
Tabarrini O, Massari S, Daelemans D, Meschini F, Manfroni G, Bottega L, Gatto B, Palumbo M, Pannecouque C, Cecchetti V.
ChemMedChem. 2010 Nov 8. 5(11):1880-92. doi: 10.1002/cmdc.201000267.
An intrabody based on a llama single-domain antibody targeting the N-terminal alpha-helical multimerization domain of HIV-1 rev prevents viral production.
Vercruysse T, Pardon E, Vanstreels E, Steyaert J, Daelemans D. J Biol Chem. 2010 Jul 9;285(28):21768-80.
Inhibition of HIV-1 replication by a bis-thiadiazolbenzene-1,2-diamine that chelates zinc ions from retroviral nucleocapsid zinc fingers.
Pannecouque C, Szafarowicz B, Volkova N, Bakulev V, Dehaen W, Mély Y, Daelemans D. Antimicrob Agents Chemother. 2010 Apr;54(4):1461-8.
A 1,8-naphthyridone derivative targets the HIV-1 Tat-mediated transcription and potently inhibits the HIV-1 replication.
Massari S, Daelemans D, Barreca ML, Knezevich A, Sabatini S, Cecchetti V, Marcello A, Pannecouque C, Tabarrini O.
J Med Chem. 2010 Jan 28. 53(2):641-8. doi: 10.1021/jm901211d.
Debio-025 inhibits HIV-1 by interfering with an early event in the replication cycle.
Daelemans D, Dumont JM, Rosenwirth B, De Clercq E, Pannecouque C. Antiviral Res. 2010 Feb;85(2):418-21.
Capture and transmission of HIV-1 by the C-type lectin L-SIGN (DC-SIGNR) is inhibited by carbohydrate-binding agents and polyanions.
Auwerx J, François KO, Vanstreels E, Van Laethem K, Daelemans D, Schols D, Balzarini J. Antiviral Res. 2009 Jul. 83(1):61-70. doi: 10.1016/j.antiviral.2009.03.011.
Specific targeting of the F13L protein by ST-246 affects orthopoxvirus production differently.
Duraffour S, Vigne S, Vermeire K, Garcel A, Vanstreels E, Daelemans D, Yang G, Jordan R, Hruby DE, Crance JM, Garin D, Andrei G, Snoeck R.
Antivir Ther. 2008. 13(8):977-90.
Studies on anti-HIV quinolones: new insights on the C-6 position.
Massari S, Daelemans D, Manfroni G, Sabatini S, Tabarrini O, Pannecouque C, Cecchetti V. Bioorg Med Chem. 2009 Jan 15. 17(2):667-74. doi: 10.1016/j.bmc.2008.11.056.
Inhibition of the CRM1-mediated nucleocytoplasmic transport by N-azolylacrylates: structure-activity relationship and mechanism of action.
Van Neck T, Pannecouque C, Vanstreels E, Stevens M, Dehaen W, Daelemans D. Bioorg Med Chem. 2008 Nov 1;16(21):9487-97.
Structure-activity relationship study on anti-HIV 6-desfluoroquinolones.
Tabarrini O, Massari S, Daelemans D, Stevens M, Manfroni G, Sabatini S, Balzarini J, Cecchetti V, Pannecouque C, Fravolini A.
J Med Chem. 2008 Sep 11. 51(17):5454-8. doi: 10.1021/jm701585h.
Fluorescence-based antiviral assay for the evaluation of compounds against vaccinia virus, varicella zoster virus and human cytomegalovirus.
Dal Pozzo F, Andrei G, Daelemans D, Winkler M, Piette J, De Clercq E, Snoeck R. J Virol Methods. 2008 Jul. 151(1):66-73. doi: 10.1016/j.jviromet.2008.03.025.
Tetrazolium-based colorimetric assay for the detection of HIV replication inhibitors: revisited 20 years later.
Pannecouque C, Daelemans D, De Clercq E. Nat Protoc. 2008;3(3):427-34.
Deletion of the transient receptor potential cation channel TRPV4 impairs murine bladder voiding.
Gevaert T, Vriens J, Segal A, Everaerts W, Roskams T, Talavera K, Owsianik G, Liedtke W, Daelemans D, Dewachter I, Van Leuven F, Voets T, De Ridder D, Nilius B.
J Clin Invest. 2007 Nov. 117(11):3453-62. doi: 10.1172/JCI31766.
Entry of hepatitis C virus and human immunodeficiency virus is selectively inhibited by carbohydrate-binding agents but not by polyanions.
Bertaux C, Daelemans D, Meertens L, Cormier EG, Reinus JF, Peumans WJ, Van Damme EJ, Igarashi Y, Oki T, Schols D, Dragic T, Balzarini J.
Virology. 2007 Sep 15. 366(1):40-50. doi: 10.1016/j.virol.2007.04.008.
Characterization of a replication-competent, integrase-defective human immunodeficiency virus (HIV)/simian virus 40 chimera as a powerful tool for the discovery and validation of HIV integrase inhibitors.
Daelemans D, Lu R, De Clercq E, Engelman A. J Virol. 2007 Apr;81(8):4381-5.
The nucleotide analog cidofovir suppresses basic fibroblast growth factor (FGF2) expression and signaling and induces apoptosis in FGF2-overexpressing endothelial cells.
Liekens S, Gijsbers S, Vanstreels E, Daelemans D, De Clercq E, Hatse S. Mol Pharmacol. 2007 Mar. 71(3):695-703. doi: 10.1124/mol.106.026559.
Pradimicin A, a carbohydrate-binding nonpeptidic lead compound for treatment of infections with viruses with highly glycosylated envelopes, such as human immunodeficiency virus.
Balzarini J, Van Laethem K, Daelemans D, Hatse S, Bugatti A, Rusnati M, Igarashi Y, Oki T, Schols D. J Virol. 2007 Jan. 81(1):362-73. doi: 10.1128/JVI.01404-06.
HIV-1 Rev function as target for antiretroviral drug development.
Daelemans D, Pannecouque C. HIV-1 Rev function as target for antiretroviral drug development. Curr Opin HIV AIDS. 2006 Sep;1(5):388-97.
A novel and efficient approach to discriminate between pre- and post-transcription HIV inhibitors.
Daelemans D, Pannecouque C, Pavlakis GN, Tabarrini O, De Clercq E. Mol Pharmacol. 2005 May;67(5):1574-80.
Kinetic and molecular analysis of nuclear export factor CRM1 association with its cargo in vivo.
Daelemans D, Costes SV, Lockett S, Pavlakis GN. Mol Cell Biol. 2005 Jan;25(2):728-39.
In vivo HIV-1 Rev multimerization in the nucleolus and cytoplasm identified by fluorescence resonance energy transfer.
Daelemans D, Costes SV, Cho EH, Erwin-Cohen RA, Lockett S, Pavlakis GN. J Biol Chem. 2004 Nov 26;279(48):50167-75.
Automatic and quantitative measurement of protein-protein colocalization in live cells.
Costes SV, Daelemans D, Cho EH, Dobbin Z, Pavlakis G, Lockett S. Biophys J. 2004 Jun;86(6):3993-4003.
A synthetic HIV-1 Rev inhibitor interfering with the CRM1-mediated nuclear export.
Daelemans D, Afonina E, Nilsson J, Werner G, Kjems J, De Clercq E, Pavlakis GN, Vandamme AM. Proc Natl Acad Sci U S A. 2002 Oct 29;99(22):14440-5.
A quantitative GFP-based bioassay for the detection of HIV-1 Tat transactivation inhibitors.
Daelemans D, De Clercq E, Vandamme AM. J Virol Methods. 2001 Aug;96(2):183-8.
A second target for the peptoid Tat/transactivation response element inhibitor CGP64222: inhibition of human immunodeficiency virus replication by blocking CXC-chemokine receptor 4-mediated virus entry.
Daelemans D, Schols D, Witvrouw M, Pannecouque C, Hatse S, van Dooren S, Hamy F, Klimkait T, de Clercq E, VanDamme AM. Mol Pharmacol. 2000 Jan;57(1):116-24.
Human immunodeficiency virus gene regulation as a target for antiviral chemotherapy.
Daelemans D, Vandamme AM, De Clercq E. Antivir Chem Chemother. 1999 Jan;10(1):1-14. Review.
Stereospecificity of 6′-C-neplanocin A analogues as inhibitors of S-adenosylhomocysteine hydrolase activity and human immunodeficiency virus replication.
Daelemans D, Vandamme AM, Shuto S, Matsuda A, De Clercq E. Nucleosides Nucleotides. 1998 Jan-Mar;17(1-3):479-86.
S-adenosylhomocysteine hydrolase inhibitors interfere with the replication of human immunodeficiency virus type 1 through inhibition of the LTR transactivation.
Daelemans D, Esté JA, Witvrouw M, Pannecouque C, Jonckheere H, Aquaro S, Perno CF, De Clercq E, Vandamme AM. Mol Pharmacol. 1997 Dec;52(6):1157-63.
Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
Kang D, Fang Z, Huang B, Lu X, Zhang H, Xu H, Huo Z, Zhou Z, Yu Z, Meng Q, Wu G, Ding X, Tian Y, Daelemans D, De Clercq E, Pannecouque C, Zhan P, Liu X.
J Med Chem. 2017 May 25. 60(10):4424-4443. doi: 10.1021/acs.jmedchem.7b00332.
Phase Separation of C9orf72 Dipeptide Repeats Perturbs Stress Granule Dynamics.
Boeynaems S, Bogaert E, Kovacs D, Konijnenberg A, Timmerman E, Volkov A, Guharoy M, De Decker M, Jaspers T, Ryan VH, Janke AM, Baatsen P, Vercruysse T, Kolaitis RM, Daelemans D, Taylor JP, Kedersha N, Anderson P, Impens F, Sobott F, Schymkowitz J, Rousseau F, Fawzi NL, Robberecht W, Van Damme P, Tompa P, Van Den Bosch L.
Mol Cell. 2017 Mar 16. 65(6):1044-1055.e5. doi: 10.1016/j.molcel.2017.02.013.
The stem cell growth factor receptor KIT is not expressed on interstitial cells in bladder.
Gevaert T, Ridder D, Vanstreels E, Daelemans D, Everaerts W, Aa FV, Pintelon I, Timmermans JP, Roskams T, Steiner C, Neuhaus J.
J Cell Mol Med. 2017 Jun. 21(6):1206-1216. doi: 10.1111/jcmm.13054.
Structural Modifications of Diarylpyrimidine-quinolone Hybrids as Potent HIV-1 NNRTIs with an Improved Drug Resistance Profile.
Mao TQ, He QQ, Chen WX, Tang GF, Chen FE, De Clercq E, Daelemans D, Pannecouque C.
Curr Pharm Des. 2016. 22(46):6982-6987. doi: 10.2174/1381612823666161122125657.
The second-generation exportin-1 inhibitor KPT-8602 demonstrates potent activity against acute lymphoblastic leukemia.
Vercruysse T, De Bie J, Neggers J, Jacquemyn M, Vanstreels E, Schmid-Burgk JL, Hornung V, Baloglu E, Landesman Y, Senapedis W, Shacham S, Dagklis A, Cools J, Daelemans D. Clin Cancer Res. 2016 Oct 25.
Discovery of novel piperidine-substituted indolylarylsulfones as potent HIV NNRTIs via structure-guided scaffold morphing and fragment rearrangement.
Li X, Gao P, Huang B, Zhou Z, Yu Z, Yuan Z, Liu H, Pannecouque C, Daelemans D, De Clercq E, Zhan P, Liu X.
Eur J Med Chem. 2017 Jan 27. 126:190-201. doi: 10.1016/j.ejmech.2016.10.009.
XPO1-dependent nuclear export is a druggable vulnerability in KRAS-mutant lung cancer.
Kim J, McMillan E, Kim HS, Venkateswaran N, Makkar G, Rodriguez-Canales J, Villalobos P, Neggers JE, Mendiratta S, Wei S, Landesman Y, Senapedis W, Baloglu E, Chow CB, Frink RE, Gao B, Roth M, Minna JD, Daelemans D, Wistuba II, Posner BA, Scaglioni PP, White MA. Nature. 2016 Oct 6;538(7623):114-117
Heterozygous mutation of cysteine528 in XPO1 is sufficient for resistance to selective inhibitors of nuclear export.
Neggers JE, Vanstreels E, Baloglu E, Shacham S, Landesman Y, Daelemans D. Oncotarget. 2016 Oct 18;7(42):68842-68850.
Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.
Kang D, Fang Z, Li Z, Huang B, Zhang H, Lu X, Xu H, Zhou Z, Ding X, Daelemans D, De Clercq E, Pannecouque C, Zhan P, Liu X.
J Med Chem. 2016 Sep 8. 59(17):7991-8007. doi: 10.1021/acs.jmedchem.6b00738.
Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach.
Lu X, Li X, Yang J, Huang B, Kang D, Zhao F, Zhou Z, De Clercq E, Daelemans D, Pannecouque C, Zhan P, Liu X.
Bioorg Med Chem. 2016 Sep 15. 24(18):4424-4433. doi: 10.1016/j.bmc.2016.07.041.
Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket.
Chen W, Zhan P, Daelemans D, Yang J, Huang B, De Clercq E, Pannecouque C, Liu X. Eur J Med Chem. 2016 Oct 4. 121:352-363. doi: 10.1016/j.ejmech.2016.05.054.
Design, synthesis, and biological evaluation of novel 5-Alkyl-6-Adamantylmethylpyrimidin-4(3H)-ones as HIV-1 non-nucleoside reverse-transcriptase inhibitors.
Li W, Huang B, Kang D, De Clercq E, Daelemans D, Pannecouque C, Zhan P, Liu X. Chem Biol Drug Des. 2016 Sep. 88(3):380-5. doi: 10.1111/cbdd.12765.
L-Aspartic and l-glutamic acid ester-based ProTides of anticancer nucleosides: Synthesis and antitumoral evaluation.
Gao LJ, De Jonghe S, Daelemans D, Herdewijn P. Bioorg Med Chem Lett. 2016 May 1. 26(9):2142-6. doi: 10.1016/j.bmcl.2016.03.076.
Design, synthesis and evaluation of novel HIV-1 NNRTIs with dual structural conformations targeting the entrance channel of the NNRTI binding pocket.
Meng Q, Chen X, Kang D, Huang B, Li W, Zhan P, Daelemans D, De Clercq E, Pannecouque C, Liu X.
Eur J Med Chem. 2016 Jun 10. 115:53-62. doi: 10.1016/j.ejmech.2016.02.068.
The Oxygen Sensor PHD2 Controls Dendritic Spines and Synapses via Modification of Filamin A.
Segura I, Lange C, Knevels E, Moskalyuk A, Pulizzi R, Eelen G, Chaze T, Tudor C, Boulegue C, Holt M, Daelemans D, Matondo M, Ghesquière B, Giugliano M, Ruiz de Almodovar C, Dewerchin M, Carmeliet P.
Cell Rep. 2016 Mar 22. 14(11):2653-67. doi: 10.1016/j.celrep.2016.02.047.
Arylazolyl(azinyl)thioacetanilides: Part 19: Discovery of Novel Substituted Imidazo[4,5-b]pyridin-2-ylthioacetanilides as Potent HIV NNRTIs Via a Structure-based Bioisosterism Approach.
Li X, Huang B, Zhou Z, Gao P, Pannecouque C, Daelemans D, De Clercq E, Zhan P, Liu X. Chem Biol Drug Des. 2016 Aug. 88(2):241-53. doi: 10.1111/cbdd.12751.
Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket.
Yang J, Chen W, Kang D, Lu X, Li X, Liu Z, Huang B, Daelemans D, Pannecouque C, De Clercq E, Zhan P, Liu X.
Eur J Med Chem. 2016 Feb 15. 109:294-304. doi: 10.1016/j.ejmech.2015.11.039.
Human exportin-1 is a target for combined therapy of HIV and AIDS related lymphoma.
Boons E, Vanstreels E, Jacquemyn M, Nogueira TC, Neggers JE, Vercruysse T, van den Oord J, Tamir S, Shacahm S, Landesman Y, Snoeck R, Pannecouque C, Andrei G, Daelemans D. EBioMedicine. 2015 2:1102-1113
Design, Synthesis, and Biological Evaluation of Novel 2-(Pyridin-3-yloxy)acetamide Derivatives as Potential Anti-HIV-1 Agents.
Huang B, Li X, Zhan P, De Clercq E, Daelemans D, Pannecouque C, Liu X. Chem Biol Drug Des. 2016 Feb. 87(2):283-9. doi: 10.1111/cbdd.12657.
Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue.
Wan ZY, Yao J, Mao TQ, Wang XL, Wang HF, Chen WX, Yin H, Chen FE, De Clercq E, Daelemans D, Pannecouque C.
Eur J Med Chem. 2015 Sep 18. 102:215-22. doi: 10.1016/j.ejmech.2015.08.007.
Hybrid chemistry. Part 4: Discovery of etravirine-VRX-480773 hybrids as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
Wan ZY, Tao Y, Wang YF, Mao TQ, Yin H, Chen FE, Piao HR, De Clercq E, Daelemans D, Pannecouque C.
Bioorg Med Chem. 2015 Aug 1. 23(15):4248-4255. doi: 10.1016/j.bmc.2015.06.048.
Understanding the molecular mechanism of host-based statin resistance in hepatitis C virus replicon containing cells.
Delang L, Scheers E, Grabner M, Verpaalen B, Helsen N, Vanstreels E, Daelemans D, Verfaillie C, Neyts J.
Biochem Pharmacol. 2015 Aug 1. 96(3):190-201. doi: 10.1016/j.bcp.2015.06.003.
Discovery of piperidin-4-yl-aminopyrimidine derivatives as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
Wan ZY, Yao J, Tao Y, Mao TQ, Wang XL, Lu YP, Wang HF, Yin H, Wu Y, Chen FE, De Clercq E, Daelemans D, Pannecouque C.
Eur J Med Chem. 2015 Jun 5. 97:1-9. doi: 10.1016/j.ejmech.2015.04.050.
Anti-HIV diarylpyrimidine-quinolone hybrids and their mode of action.
Mao TQ, He QQ, Wan ZY, Chen WX, Chen FE, Tang GF, De Clercq E, Daelemans D, Pannecouque C.
Bioorg Med Chem. 2015 Jul 1. 23(13):3860-8. doi: 10.1016/j.bmc.2015.03.037.
Scaffold hopping: exploration of acetanilide-containing uracil analogues as potential NNRTIs.
Babkov DA, Valuev-Elliston VT, Paramonova MP, Ozerov AA, Ivanov AV, Chizhov AO, Khandazhinskaya AL, Kochetkov SN, Balzarini J, Daelemans D, Pannecouque C, Seley-Radtke KL, Novikov MS. Bioorg Med Chem. 2015 Mar 1. 23(5):1069-81. doi: 10.1016/j.bmc.2015.01.002.
Identifying Drug-Target Selectivity of Small-Molecule CRM1/XPO1 Inhibitors by CRISPR/Cas9 Genome Editing.
Neggers JE, Vercruysse T, Jacquemyn M, Vanstreels E, Baloglu E, Shacham S, Crochiere M, Landesman Y, Daelemans D. Chem Biol. 2015 Jan 8. pii: S1074-5521(14)00425-6.
Synthesis and biological evaluation of DAPY-DPEs hybrids as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
Wu HQ, Yao J, He QQ, Chen WX, Chen FE, Pannecouque C, De Clercq E, Daelemans D. Bioorg Med Chem. 2015 Feb 1. 23(3):624-31. doi: 10.1016/j.bmc.2014.11.032.
A stably expressed llama single-domain intrabody targeting Rev displays broad-spectrum anti-HIV activity.
Boons E, Li G, Vanstreels E, Vercruysse T, Pannecouque C, Vandamme AM, Daelemans D. Antiviral Res. 2014 Dec;112:91-102.
Exploiting the anti-HIV 6-desfluoroquinolones to design multiple ligands.
Sancineto L, Iraci N, Barreca ML, Massari S, Manfroni G, Corazza G, Cecchetti V, Marcello A, Daelemans D, Pannecouque C, Tabarrini O.
Bioorg Med Chem. 2014 Sep 1. 22(17):4658-66. doi: 10.1016/j.bmc.2014.07.018.
Anti-HIV-1 activity of the G-quadruplex ligand BRACO-19.
Perrone R, Butovskaya E, Daelemans D, Palù G, Pannecouque C, Richter SN. J Antimicrob Chemother. 2014 Dec. 69(12):3248-58. doi: 10.1093/jac/dku280.
Identification of different phenotypes of interstitial cells in the upper and deep lamina propria of the human bladder dome.
Gevaert T, Vanstreels E, Daelemans D, Franken J, Van Der Aa F, Roskams T, De Ridder D. J Urol. 2014 Nov. 192(5):1555-63. doi: 10.1016/j.juro.2014.05.096.
Dynamics of the ternary complex formed by c-Myc interactor JPO2, transcriptional co-activator LEDGF/p75, and chromatin.
Hendrix J, van Heertum B, Vanstreels E, Daelemans D, De Rijck J. J Biol Chem. 2014 May 2. 289(18):12494-506. doi: 10.1074/jbc.M113.525964.
HIV-1 Rev multimerization: mechanism and insights.
Vercruysse T, Daelemans D. Curr HIV Res. 2013 Dec;11(8):623-34.
Towards new C6-rigid S-DABO HIV-1 reverse transcriptase inhibitors: synthesis, biological investigation and molecular modeling studies.
Wu HQ, Yan ZH, Chen WX, He QQ, Chen FE, De Clercq E, Balzarini J, Daelemans D, Pannecouque C.
Bioorg Med Chem. 2013 Nov 1. 21(21):6477-83. doi: 10.1016/j.bmc.2013.08.040.
Role of PFKFB3-driven glycolysis in vessel sprouting.
De Bock K, Georgiadou M, Schoors S, Kuchnio A, Wong BW, Cantelmo AR, Quaegebeur A, Ghesquière B, Cauwenberghs S, Eelen G, Phng LK, Betz I, Tembuyser B, Brepoels K, Welti J, Geudens I, Segura I, Cruys B, Bifari F, Decimo I, Blanco R, Wyns S, Vangindertael J, Rocha S, Collins RT, Munck S, Daelemans D, Imamura H, Devlieger R, Rider M, Van Veldhoven PP, Schuit F, Bartrons R, Hofkens J, Fraisl P, Telang S, Deberardinis RJ, Schoonjans L, Vinckier S, Chesney J, Gerhardt H, Dewerchin M, Carmeliet P.
Cell. 2013 Aug 1. 154(3):651-63. doi: 10.1016/j.cell.2013.06.037.
Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors.
Yang S, Pannecouque C, Daelemans D, Ma XD, Liu Y, Chen FE, De Clercq E. Eur J Med Chem. 2013 Jul. 65:134-43. doi: 10.1016/j.ejmech.2013.04.052.
Mapping the binding interface between an HIV-1 inhibiting intrabody and the viral protein Rev.
Vercruysse T, Boons E, Venken T, Vanstreels E, Voet A, Steyaert J, De Maeyer M, Daelemans D. PLoS One. 2013;8(4)
Hemozoin induces lung inflammation and correlates with malaria-associated acute respiratory distress syndrome.
Deroost K, Tyberghein A, Lays N, Noppen S, Schwarzer E, Vanstreels E, Komuta M, Prato M, Lin JW, Pamplona A, Janse CJ, Arese P, Roskams T, Daelemans D, Opdenakker G, Van den Steen PE. Am J Respir Cell Mol Biol. 2013 May. 48(5):589-600. doi: 10.1165/rcmb.2012-0450OC.
Some hydrazones of 2-aroylamino-3-methylbutanohydrazide: synthesis, molecular modeling studies, and identification as stereoselective inhibitors of HIV-1.
Tatar E, Küçükgüzel I, Daelemans D, Talele TT, Kaushik-Basu N, De Clercq E, Pannecouque C.
Arch Pharm (Weinheim). 2013 Feb. 346(2):140-53. doi: 10.1002/ardp.201200311.
Synthesis, biological evaluation and molecular modeling of 4,6-diarylpyrimidines and diarylbenzenes as novel non-nucleosides HIV-1 reverse transcriptase inhibitors.
Ribone SR, Leen V, Madrid M, Dehaen W, Daelemans D, Pannecouque C, Briñón MC. Eur J Med Chem. 2012 Dec. 58:485-92. doi: 10.1016/j.ejmech.2012.10.036.
A phenyl-thiadiazolylidene-amine derivative ejects zinc from retroviral nucleocapsid zinc fingers and inactivates HIV virions.
Vercruysse T, Basta B, Dehaen W, Humbert N, Balzarini J, Debaene F, Sanglier-Cianférani S, Pannecouque C, Mély Y, Daelemans. Retrovirology. 2012 Nov 12;9:95.
Selective inhibitors of nuclear export show that CRM1/XPO1 is a target in chronic lymphocytic leukemia.
Lapalombella R, Sun Q, Williams K, Tangeman L, Jha S, Zhong Y, Goettl V, Mahoney E, Berglund C, Gupta S, Farmer A, Mani R, Johnson AJ, Lucas D, Mo X, Daelemans D, Sandanayaka V, Shechter S, McCauley D, Shacham S, Kauffman M, Chook YM, Byrd JC. Blood. 2012 Nov 29;120(23):4621-34.
CXCR4 chemokine receptor antagonists: nickel(II) complexes of configurationally restricted macrocycles.
Smith R, Huskens D, Daelemans D, Mewis RE, Garcia CD, Cain AN, Freeman TN, Pannecouque C, De Clercq E, Schols D, Hubin TJ, Archibald SJ.
Dalton Trans. 2012 Oct 7. 41(37):11369-77. doi: 10.1039/c2dt31137b.
Intracytoplasmic trapping of influenza virus by a lipophilic derivative of aglycoristocetin.
Vanderlinden E, Vanstreels E, Boons E, ter Veer W, Huckriede A, Daelemans D, Van Lommel A, Rőth E, Sztaricskai F, Herczegh P, Naesens L.
J Virol. 2012 Sep. 86(17):9416-31. doi: 10.1128/JVI.07032-11.
Computational investigation ofthe HIV-1 Rev multimerization using molecular dynamics simulations and binding free energy calculations.
Venken T, Daelemans D, De Maeyer M, Voet A. Proteins. 2012 Jun;80(6):1633-46.
A time-of-drug addition approach to target identification of antiviral compounds.
Daelemans D, Pauwels R, De Clercq E, Pannecouque C. Nat Protoc. 2011 Jun;6(6):925-33.
Selective inhibition of Human Immunodeficiency Virus type 1 (HIV-1) by a novel family of tricyclic nucleosides.
Bonache MC, Cordeiro A, Quesada E, Vanstreels E, Daelemans D, Camarasa MJ, Balzarini J, San-Félix A.
Antiviral Res. 2011 Oct. 92(1):37-44. doi: 10.1016/j.antiviral.2011.05.002.
Structural investigation of the naphthyridone scaffold: identification of a 1,6-naphthyridone derivative with potent and selective anti-HIV activity.
Tabarrini O, Massari S, Sancineto L, Daelemans D, Sabatini S, Manfroni G, Cecchetti V, Pannecouque C.
ChemMedChem. 2011 Jul 4. 6(7):1249-57. doi: 10.1002/cmdc.201100073.
Measuring cooperative Rev protein-protein interactions on Rev responsive RNA by fluorescence resonance energy transfer.
Vercruysse T, Pawar S, De Borggraeve W, Pardon E, Pavlakis GN, Pannecouque C, Steyaert J, Balzarini J, Daelemans D. RNA Biol. 2011 Mar-Apr;8(2):316-24.
Studies of anti-HIV transcription inhibitor quinolones: identification of potent N1-vinyl derivatives.
Tabarrini O, Massari S, Daelemans D, Meschini F, Manfroni G, Bottega L, Gatto B, Palumbo M, Pannecouque C, Cecchetti V.
ChemMedChem. 2010 Nov 8. 5(11):1880-92. doi: 10.1002/cmdc.201000267.
An intrabody based on a llama single-domain antibody targeting the N-terminal alpha-helical multimerization domain of HIV-1 rev prevents viral production.
Vercruysse T, Pardon E, Vanstreels E, Steyaert J, Daelemans D. J Biol Chem. 2010 Jul 9;285(28):21768-80.
Inhibition of HIV-1 replication by a bis-thiadiazolbenzene-1,2-diamine that chelates zinc ions from retroviral nucleocapsid zinc fingers.
Pannecouque C, Szafarowicz B, Volkova N, Bakulev V, Dehaen W, Mély Y, Daelemans D. Antimicrob Agents Chemother. 2010 Apr;54(4):1461-8.
A 1,8-naphthyridone derivative targets the HIV-1 Tat-mediated transcription and potently inhibits the HIV-1 replication.
Massari S, Daelemans D, Barreca ML, Knezevich A, Sabatini S, Cecchetti V, Marcello A, Pannecouque C, Tabarrini O.
J Med Chem. 2010 Jan 28. 53(2):641-8. doi: 10.1021/jm901211d.
Debio-025 inhibits HIV-1 by interfering with an early event in the replication cycle.
Daelemans D, Dumont JM, Rosenwirth B, De Clercq E, Pannecouque C. Antiviral Res. 2010 Feb;85(2):418-21.
Capture and transmission of HIV-1 by the C-type lectin L-SIGN (DC-SIGNR) is inhibited by carbohydrate-binding agents and polyanions.
Auwerx J, François KO, Vanstreels E, Van Laethem K, Daelemans D, Schols D, Balzarini J. Antiviral Res. 2009 Jul. 83(1):61-70. doi: 10.1016/j.antiviral.2009.03.011.
Specific targeting of the F13L protein by ST-246 affects orthopoxvirus production differently.
Duraffour S, Vigne S, Vermeire K, Garcel A, Vanstreels E, Daelemans D, Yang G, Jordan R, Hruby DE, Crance JM, Garin D, Andrei G, Snoeck R.
Antivir Ther. 2008. 13(8):977-90.
Studies on anti-HIV quinolones: new insights on the C-6 position.
Massari S, Daelemans D, Manfroni G, Sabatini S, Tabarrini O, Pannecouque C, Cecchetti V. Bioorg Med Chem. 2009 Jan 15. 17(2):667-74. doi: 10.1016/j.bmc.2008.11.056.
Inhibition of the CRM1-mediated nucleocytoplasmic transport by N-azolylacrylates: structure-activity relationship and mechanism of action.
Van Neck T, Pannecouque C, Vanstreels E, Stevens M, Dehaen W, Daelemans D. Bioorg Med Chem. 2008 Nov 1;16(21):9487-97.
Structure-activity relationship study on anti-HIV 6-desfluoroquinolones.
Tabarrini O, Massari S, Daelemans D, Stevens M, Manfroni G, Sabatini S, Balzarini J, Cecchetti V, Pannecouque C, Fravolini A.
J Med Chem. 2008 Sep 11. 51(17):5454-8. doi: 10.1021/jm701585h.
Fluorescence-based antiviral assay for the evaluation of compounds against vaccinia virus, varicella zoster virus and human cytomegalovirus.
Dal Pozzo F, Andrei G, Daelemans D, Winkler M, Piette J, De Clercq E, Snoeck R. J Virol Methods. 2008 Jul. 151(1):66-73. doi: 10.1016/j.jviromet.2008.03.025.
Tetrazolium-based colorimetric assay for the detection of HIV replication inhibitors: revisited 20 years later.
Pannecouque C, Daelemans D, De Clercq E. Nat Protoc. 2008;3(3):427-34.
Deletion of the transient receptor potential cation channel TRPV4 impairs murine bladder voiding.
Gevaert T, Vriens J, Segal A, Everaerts W, Roskams T, Talavera K, Owsianik G, Liedtke W, Daelemans D, Dewachter I, Van Leuven F, Voets T, De Ridder D, Nilius B.
J Clin Invest. 2007 Nov. 117(11):3453-62. doi: 10.1172/JCI31766.
Entry of hepatitis C virus and human immunodeficiency virus is selectively inhibited by carbohydrate-binding agents but not by polyanions.
Bertaux C, Daelemans D, Meertens L, Cormier EG, Reinus JF, Peumans WJ, Van Damme EJ, Igarashi Y, Oki T, Schols D, Dragic T, Balzarini J.
Virology. 2007 Sep 15. 366(1):40-50. doi: 10.1016/j.virol.2007.04.008.
Characterization of a replication-competent, integrase-defective human immunodeficiency virus (HIV)/simian virus 40 chimera as a powerful tool for the discovery and validation of HIV integrase inhibitors.
Daelemans D, Lu R, De Clercq E, Engelman A. J Virol. 2007 Apr;81(8):4381-5.
The nucleotide analog cidofovir suppresses basic fibroblast growth factor (FGF2) expression and signaling and induces apoptosis in FGF2-overexpressing endothelial cells.
Liekens S, Gijsbers S, Vanstreels E, Daelemans D, De Clercq E, Hatse S. Mol Pharmacol. 2007 Mar. 71(3):695-703. doi: 10.1124/mol.106.026559.
Pradimicin A, a carbohydrate-binding nonpeptidic lead compound for treatment of infections with viruses with highly glycosylated envelopes, such as human immunodeficiency virus.
Balzarini J, Van Laethem K, Daelemans D, Hatse S, Bugatti A, Rusnati M, Igarashi Y, Oki T, Schols D. J Virol. 2007 Jan. 81(1):362-73. doi: 10.1128/JVI.01404-06.
HIV-1 Rev function as target for antiretroviral drug development.
Daelemans D, Pannecouque C. HIV-1 Rev function as target for antiretroviral drug development. Curr Opin HIV AIDS. 2006 Sep;1(5):388-97.
A novel and efficient approach to discriminate between pre- and post-transcription HIV inhibitors.
Daelemans D, Pannecouque C, Pavlakis GN, Tabarrini O, De Clercq E. Mol Pharmacol. 2005 May;67(5):1574-80.
Kinetic and molecular analysis of nuclear export factor CRM1 association with its cargo in vivo.
Daelemans D, Costes SV, Lockett S, Pavlakis GN. Mol Cell Biol. 2005 Jan;25(2):728-39.
In vivo HIV-1 Rev multimerization in the nucleolus and cytoplasm identified by fluorescence resonance energy transfer.
Daelemans D, Costes SV, Cho EH, Erwin-Cohen RA, Lockett S, Pavlakis GN. J Biol Chem. 2004 Nov 26;279(48):50167-75.
Automatic and quantitative measurement of protein-protein colocalization in live cells.
Costes SV, Daelemans D, Cho EH, Dobbin Z, Pavlakis G, Lockett S. Biophys J. 2004 Jun;86(6):3993-4003.
A synthetic HIV-1 Rev inhibitor interfering with the CRM1-mediated nuclear export.
Daelemans D, Afonina E, Nilsson J, Werner G, Kjems J, De Clercq E, Pavlakis GN, Vandamme AM. Proc Natl Acad Sci U S A. 2002 Oct 29;99(22):14440-5.
A quantitative GFP-based bioassay for the detection of HIV-1 Tat transactivation inhibitors.
Daelemans D, De Clercq E, Vandamme AM. J Virol Methods. 2001 Aug;96(2):183-8.
A second target for the peptoid Tat/transactivation response element inhibitor CGP64222: inhibition of human immunodeficiency virus replication by blocking CXC-chemokine receptor 4-mediated virus entry.
Daelemans D, Schols D, Witvrouw M, Pannecouque C, Hatse S, van Dooren S, Hamy F, Klimkait T, de Clercq E, VanDamme AM. Mol Pharmacol. 2000 Jan;57(1):116-24.
Human immunodeficiency virus gene regulation as a target for antiviral chemotherapy.
Daelemans D, Vandamme AM, De Clercq E. Antivir Chem Chemother. 1999 Jan;10(1):1-14. Review.
Stereospecificity of 6′-C-neplanocin A analogues as inhibitors of S-adenosylhomocysteine hydrolase activity and human immunodeficiency virus replication.
Daelemans D, Vandamme AM, Shuto S, Matsuda A, De Clercq E. Nucleosides Nucleotides. 1998 Jan-Mar;17(1-3):479-86.
S-adenosylhomocysteine hydrolase inhibitors interfere with the replication of human immunodeficiency virus type 1 through inhibition of the LTR transactivation.
Daelemans D, Esté JA, Witvrouw M, Pannecouque C, Jonckheere H, Aquaro S, Perno CF, De Clercq E, Vandamme AM. Mol Pharmacol. 1997 Dec;52(6):1157-63.