.. Currently available AR antagonists such as bicalutamide have limited activity in castration-resistant prostate cancer (CRPC). Mechanistic studies have shown that the bicalutamide liganded AR can accumulate in the nucleus and bind to chromatin, but that it does not effectively recruit coactivator proteins and instead can recruit the corepressor proteins NCoR and SMRT. This ability to mediate chromatin binding may be an
The likely FDA approval of MDV3100 will arm oncologists with two new agents (abiraterone and MDV3100) that can suppress AR activity in CRPC, but patients invariably relapse and resistance mechanisms are unknown. Tis proposal will determine in detail the mechanisms of action for MDV3100 and functionally related AR antagonists under development, and identify mechanisms of .intrinsic and acquired resistance.
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