Discovery of JNJ-63576253: A Clinical Stage Androgen Receptor Antagonist for F877L Mutant and Wild-Type Castration-Resistant Prostate Cancer (mCRPC).

doi:10.1021/acs.jmedchem.0c01563

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Article

Discovery of JNJ-63576253: A Clinical Stage Androgen Receptor Antagonist for F877L Mutant and Wild-Type Castration-Resistant Prostate Cancer (mCRPC).

Journal of medicinal chemistry - 28 Jan 2021

Zhang Zhuming, Connolly Peter J, Lim Heng Keang, Pande Vineet, Meerpoel Lieven, Teleha Christopher, Branch Jonathan R, Ondrus Janine, Hickson Ian, Bush Tammy, Luistro Leopoldo, Packman Kathryn, Bischoff James R, Ibrahim Salam, Parrett Christopher, Chong Yolanda, Gottardis Marco M, Bignan Gilles

Abstract excerpt

Persistent androgen receptor (AR) activation drives therapeutic resistance to second-generation AR pathway inhibitors and contributes to the progression of advanced prostate cancer. One resistance mechanism is point mutations in the ligand binding domain of AR that can transform antagonists into agonists. The AR F877L mutation, identified in patients treated with enzalutamide or apalutamide, confers resistance to...

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PMID: 33470111
DOI: 10.1021/acs.jmedchem.0c01563

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