Article
An F876L mutation in androgen receptor confers genetic and phenotypic resistance to MDV3100 (enzalutamide).
Cancer discovery - 1 Sept 2013
Korpal Manav, Korn Joshua M, Gao Xueliang, Rakiec Daniel P, Ruddy David A, Doshi Shivang, Yuan Jing, Kovats Steve G, Kim Sunkyu, Cooke Vesselina G, Monahan John E, Stegmeier Frank, Roberts Thomas M, Sellers William R, Zhou Wenlai, Zhu Ping
Abstract excerpt
UNLABELLED: Castration-resistant prostate cancer (CRPC) is the most aggressive, incurable form of prostate cancer. MDV3100 (enzalutamide), an antagonist of the androgen receptor (AR), was approved for clinical use in men with metastatic CRPC. Although this compound showed clinical efficacy, many initial responders later developed resistance. To uncover relevant resistant mechanisms, we developed a model of...
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