Cancer therapy articles
- 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
- 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.
- 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.
- 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.
- 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.
- 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
- Intermedilysin cytolytic activity depends on heparan sulfates and membrane composition.
Drabavicius G, Daelemans D. PLoS Genet. 2021 doi: 10.1371/journal.pgen.1009387.
- 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
- Quantitative Nucelocytoplasmic 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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
- 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
- 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
- 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.
- 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.
- 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.
- 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.
- Synthesis, Computational Analysis, and Antiproliferative Activity of Novel Benzimidazole Acrylonitriles as Tubulin Polymerization Inhibitors: Part 2.
Beč A, Hok L, Persoons L, Vanstreels E, Daelemans D, Vianello R, Hranjec M. Pharmaceuticals (Basel). 2021 Oct 17. 14(10):1052. doi: 10.3390/ph14101052.
- 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.
- 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.
- 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 Nitroxoline Analogs with Potent Cathepsin B Exopeptidase Inhibitory Activity.
Van de Walle T, Briand M, Mitrović A, Sosič 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.
- 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.
- Design and Synthesis of New 6-Nitro and 6-Amino-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, Pérez-Pérez MJ.
Molecules. 2019 Nov 21. 24(23):4236. doi: 10.3390/molecules24234236.
- Xylo-C-nucleosides with a pyrrolo[2,1-f][1,2,4]triazin-4-amine heterocyclic 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.
- 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.
- 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..
- 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.
- 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.
- 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
- 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.
- 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
- 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.
- 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.
- 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.