Inhibiting androgen receptor nuclear entry in castration-resistant prostate cancer

Julie A. Pollock,Suzanne E. Wardell,A.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

Inhibiting androgen receptor nuclear entry in castration-resistant prostate cancer

2016

Julie A. Pollock
Suzanne E. Wardell
A.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

A 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.

Keywords:

Small molecule
Prostate cancer
Androgen receptor
Molecular biology
Biology
Cell signaling
Cyclobutane
Transcription (biology)
Receptor
castration resistant
Internal medicine
Cancer research
Endocrinology

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