Ontology highlight
ABSTRACT:
SUBMITTER: Caboni L
PROVIDER: S-EPMC3295204 | biostudies-literature | 2012 Feb
REPOSITORIES: biostudies-literature
Caboni Laura L Kinsella Gemma K GK Blanco Fernando F Fayne Darren D Jagoe William N WN Carr Miriam M Williams D Clive DC Meegan Mary J MJ Lloyd David G DG
Journal of medicinal chemistry 20120210 4
Prostate cancer (PCa) therapy typically involves administration of "classical" antiandrogens, competitive inhibitors of androgen receptor (AR) ligands, dihydrotestosterone (DHT) and testosterone (tes), for the ligand-binding pocket (LBP) in the ligand-binding domain (LBD) of AR. Prolonged LBP-targeting leads to resistance, and alternative therapies are urgently required. We report the identification and characterization of a novel series of diarylhydrazides as selective disruptors of AR interact ...[more]