Article
Orally Bioavailable Androgen Receptor Degrader, Potential Next-Generation Therapeutic for Enzalutamide-Resistant Prostate Cancer.
Clinical cancer research : an official journal of the American Association for Cancer Research - 15 Nov 2019
Ponnusamy Suriyan, He Yali, Hwang Dong-Jin, Thiyagarajan Thirumagal, Houtman Rene, Bocharova Vera, Sumpter Bobby G, Fernandez Elias, Johnson Daniel, Du Ziyun, Pfeffer Lawrence M, Getzenberg Robert H, McEwan Iain J, Miller Duane D, Narayanan Ramesh
Abstract excerpt
PURPOSE: Androgen receptor (AR)-targeting prostate cancer drugs, which are predominantly competitive ligand-binding domain (LBD)-binding antagonists, are inactivated by common resistance mechanisms. It is important to develop next-generation mechanistically distinct drugs to treat castration- and drug-resistant prostate cancers. EXPERIMENTAL DESIGN: Second-generation AR pan antagonist UT-34 was selected from a...
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