Article
Selectively targeting the dimerization interface of human androgen receptor with small-molecules to treat castration-resistant prostate cancer.
Cancer letters - 28 Nov 2018
Dalal Kush, Ban Fuqiang, Li Huifang, Morin Hélène, Roshan-Moniri Mani, Tam Kevin J, Shepherd Ashley, Sharma Aishwariya, Peacock James, Carlson Michael L, LeBlanc Eric, Perez Carl, Duong Franck, Ong Christopher J, Rennie Paul S, Cherkasov Artem
Abstract excerpt
Prostate cancer (PCa) is a leading cause of death for men in North America. The androgen receptor (AR) - a hormone inducible transcription factor - drives expression of tumor promoting genes and represents an important therapeutic target in PCa. The AR is activated by steroid recruitment to its ligand binding domain (LBD), followed by receptor nuclear translocation and dimerization via the DNA binding domain...
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