Article
Discovery of small-molecule inhibitors selectively targeting the DNA-binding domain of the human androgen receptor.
Journal of medicinal chemistry - 14 Aug 2014
Li Huifang, Ban Fuqiang, Dalal Kush, Leblanc Eric, Frewin Kate, Ma Dennis, Adomat Hans, Rennie Paul S, Cherkasov Artem
Abstract excerpt
The human androgen receptor (AR) is considered as a master regulator in the development and progression of prostate cancer (PCa). As resistance to clinically used anti-AR drugs remains a major challenge for the treatment of advanced PCa, there is a pressing need for new anti-AR therapeutic avenues. In this study, we identified a binding site on the DNA binding domain (DBD) of the receptor and utilized virtual...
Topics
- Androgen Receptor Antagonists
- Animals
- Antineoplastic Agents
- Benzamides
- Binding Sites
- Cell Line, Tumor
- Cell Survival
- Computer Simulation
- DNA
- Databases, Chemical
- Drug Resistance, Neoplasm
- Humans
- Imidazoles