Ontology highlight
ABSTRACT:
SUBMITTER: Dalal K
PROVIDER: S-EPMC5628141 | biostudies-literature | 2017 Oct
REPOSITORIES: biostudies-literature
Dalal Kush K Che Meixia M Que Nanette S NS Sharma Aishwariya A Yang Rendong R Lallous Nada N Borgmann Hendrik H Ozistanbullu Deniz D Tse Ronnie R Ban Fuqiang F Li Huifang H Tam Kevin J KJ Roshan-Moniri Mani M LeBlanc Eric E Gleave Martin E ME Gewirth Daniel T DT Dehm Scott M SM Cherkasov Artem A Rennie Paul S PS
Molecular cancer therapeutics 20170803 10
Human androgen receptor (AR) is a hormone-activated transcription factor that is an important drug target in the treatment of prostate cancer. Current small-molecule AR antagonists, such as enzalutamide, compete with androgens that bind to the steroid-binding pocket of the AR ligand-binding domain (LBD). In castration-resistant prostate cancer (CRPC), drug resistance can manifest through AR-LBD mutations that convert AR antagonists into agonists, or by expression of AR variants lacking the LBD. ...[more]