Inhibiting androgen receptor nuclear entry in castration-resistant prostate cancer

Julie A Pollock, Suzanne E Wardell,Alexander A Parent,David B Stagg, Stephanie J Ellison,Holly M Alley,Christina A Chao,Scott A Lawrence,James P Stice, Ivan Spasojevic,Jennifer G Baker, Sung Hoon Kim,Donald P McDonnell,John A Katzenellenbogen,John D Norris

Nature Chemical Biology（2016）

引用 16|浏览43

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摘要

cyclobutane compound competitively inhibits the activity of androgen receptors (AR) containing antiandrogen-resistant mutations through stabilization of the receptor in an apo-like conformation and preventing AR nuclear entry.

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关键词

Cancer therapy,Cell signalling,Small molecules,Transcription,Chemistry/Food Science,general,Biochemical Engineering,Biochemistry,Cell Biology,Bioorganic Chemistry

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