Article
Small molecule-induced degradation of the full length and V7 truncated variant forms of human androgen receptor.
European journal of medicinal chemistry - 5 Sept 2018
Dalal Kush, Morin Helene, Ban Fuqiang, Shepherd Ashley, Fernandez Michael, Tam Kevin J, Li Huifang, LeBlanc Eric, Lack Nathan, Prinz Helge, Rennie Paul S, Cherkasov Artem
Abstract excerpt
The androgen receptor (AR) is a hormone-activated transcription factor that regulates the development and progression of prostate cancer (PCa) and represents one of the most well-established drug targets. Currently clinically approved small molecule inhibitors of AR, such as enzalutamide, are built upon a common chemical scaffold that interacts with the AR by the same mechanism of action. These inhibitors...
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