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Page 1
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: bignan g. 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: bignan g. 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: bignan g. 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: bignan g. 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
A vascular endothelial growth factor receptor-2 kinase inhibitor potentiates the activity of the conventional chemotherapeutic agents paclitaxel and doxorubicin in tumor xenograft models.
Emanuel S, Gruninger RH, Fuentes-Pesquera A, Connolly PJ, Seamon JA, Hazel S, Tominovich R, Hollister B, Napier C, D'Andrea MR, Reuman M, Bignan G, Tuman R, Johnson D, Moffatt D, Batchelor M, Foley A, O'Connell J, Allen R, Perry M, Jolliffe L, Middleton SA. Emanuel S, et al. Among authors: bignan g. Mol Pharmacol. 2004 Sep;66(3):635-47. doi: 10.1124/mol.104.000638. Mol Pharmacol. 2004. PMID: 15322256
Modulating Androgen Receptor-Driven Transcription in Prostate Cancer with Selective CDK9 Inhibitors.
Richters A, Doyle SK, Freeman DB, Lee C, Leifer BS, Jagannathan S, Kabinger F, Koren JV, Struntz NB, Urgiles J, Stagg RA, Curtin BH, Chatterjee D, Mathea S, Mikochik PJ, Hopkins TD, Gao H, Branch JR, Xin H, Westover L, Bignan GC, Rupnow BA, Karlin KL, Olson CM, Westbrook TF, Vacca J, Wilfong CM, Trotter BW, Saffran DC, Bischofberger N, Knapp S, Russo JW, Hickson I, Bischoff JR, Gottardis MM, Balk SP, Lin CY, Pop MS, Koehler AN. Richters A, et al. Among authors: bignan gc. Cell Chem Biol. 2021 Feb 18;28(2):134-147.e14. doi: 10.1016/j.chembiol.2020.10.001. Epub 2020 Oct 20. Cell Chem Biol. 2021. PMID: 33086052 Free article.
14 results