abstract |
Modified androgen receptor polypeptides that exhibit resistance to inhibition by androgen receptor inhibitors are described herein. Compositions, combinations and kits comprising the modified androgen receptor polypeptide, and methods of using the modified androgen receptor polypeptide are described herein. Methods of using modified androgen receptor polypeptides as screening agents for the identification and design of third generation androgen receptor modulators are also described herein. A third generation androgen receptor modulator that inhibits the activity of a modified androgen receptor polypeptide is also described herein. Pharmaceutical compositions and medicaments comprising the compounds described herein, and these androgen receptor modulators alone, with other compounds for the treatment of diseases or conditions, including cancers, such as castration resistant prostate cancer, mediated or dependent on androgen receptors. The method of using it in combination is also described. |