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Design and synthesis of a series of bioavailable fatty acid synthase (FASN) KR domain inhibitors for cancer therapy.
Lu T, Schubert C, Cummings MD, Bignan G, Connolly PJ, Smans K, Ludovici D, Parker MH, Meyer C, Rocaboy C, Alexander R, Grasberger B, De Breucker S, Esser N, Fraiponts E, Gilissen R, Janssens B, Peeters D, Van Nuffel L, Vermeulen P, Bischoff J, Meerpoel L. Lu T, et al. Among authors: meerpoel l. Bioorg Med Chem Lett. 2018 Jul 1;28(12):2159-2164. doi: 10.1016/j.bmcl.2018.05.014. Epub 2018 May 8. Bioorg Med Chem Lett. 2018. PMID: 29779975
Discovery of JNJ-63576253: A Clinical Stage Androgen Receptor Antagonist for F877L Mutant and Wild-Type Castration-Resistant Prostate Cancer (mCRPC).
Zhang Z, Connolly PJ, Lim HK, Pande V, Meerpoel L, Teleha C, Branch JR, Ondrus J, Hickson I, Bush T, Luistro L, Packman K, Bischoff JR, Ibrahim S, Parrett C, Chong Y, Gottardis MM, Bignan G. Zhang Z, et al. Among authors: meerpoel l. J Med Chem. 2021 Jan 28;64(2):909-924. doi: 10.1021/acs.jmedchem.0c01563. Epub 2021 Jan 20. J Med Chem. 2021. PMID: 33470111
Spirocyclic Thiohydantoin Antagonists of F877L and Wild-Type Androgen Receptor for Castration-Resistant Prostate Cancer.
Zhang Z, Connolly PJ, Trabalón Escolar L, Rocaboy C, Pande V, Meerpoel L, Lim HK, Branch JR, Ondrus J, Hickson I, Bush TL, Bischoff JR, Bignan G. Zhang Z, et al. Among authors: meerpoel l. ACS Med Chem Lett. 2021 Jun 29;12(8):1245-1252. doi: 10.1021/acsmedchemlett.1c00032. eCollection 2021 Aug 12. ACS Med Chem Lett. 2021. PMID: 34422225 Free PMC article.
Discovery of JNJ-63576253, a Next-Generation Androgen Receptor Antagonist Active Against Wild-Type and Clinically Relevant Ligand Binding Domain Mutations in Metastatic Castration-Resistant Prostate Cancer.
Branch JR, Bush TL, Pande V, Connolly PJ, Zhang Z, Hickson I, Ondrus J, Jaensch S, Bischoff JR, Habineza G, Van Hecke G, Meerpoel L, Packman K, Parrett CJ, Chong YT, Gottardis MM, Bignan G. Branch JR, et al. Among authors: meerpoel l. Mol Cancer Ther. 2021 May;20(5):763-774. doi: 10.1158/1535-7163.MCT-20-0510. Epub 2021 Mar 1. Mol Cancer Ther. 2021. PMID: 33649102
Structure-Based Design of Type II Inhibitors Applied to Maternal Embryonic Leucine Zipper Kinase.
Johnson CN, Adelinet C, Berdini V, Beke L, Bonnet P, Brehmer D, Calo F, Coyle JE, Day PJ, Frederickson M, Freyne EJ, Gilissen RA, Hamlett CC, Howard S, Meerpoel L, Mevellec L, McMenamin R, Pasquier E, Patel S, Rees DC, Linders JT. Johnson CN, et al. Among authors: meerpoel l. ACS Med Chem Lett. 2014 May 23;6(1):31-6. doi: 10.1021/ml5001273. eCollection 2015 Jan 8. ACS Med Chem Lett. 2014. PMID: 25589926 Free PMC article.
Fragment-based discovery of type I inhibitors of maternal embryonic leucine zipper kinase.
Johnson CN, Berdini V, Beke L, Bonnet P, Brehmer D, Coyle JE, Day PJ, Frederickson M, Freyne EJ, Gilissen RA, Hamlett CC, Howard S, Meerpoel L, McMenamin R, Patel S, Rees DC, Sharff A, Sommen F, Wu T, Linders JT. Johnson CN, et al. Among authors: meerpoel l. ACS Med Chem Lett. 2014 May 23;6(1):25-30. doi: 10.1021/ml5001245. eCollection 2015 Jan 8. ACS Med Chem Lett. 2014. PMID: 25589925 Free PMC article.
Synthesis and in vitro and in vivo structure-activity relationships of novel antifungal triazoles for dermatology.
Meerpoel L, Backx LJ, Van der Veken LJ, Heeres J, Corens D, De Groot A, Odds FC, Van Gerven F, Woestenborghs FA, Van Breda A, Oris M, van Dorsselaer P, Willemsens GH, Vermuyten KJ, Marichal PJ, Vanden Bossche HF, Ausma J, Borgers M. Meerpoel L, et al. J Med Chem. 2005 Mar 24;48(6):2184-93. doi: 10.1021/jm0494772. J Med Chem. 2005. PMID: 15771461
47 results