abstract |
Described herein are mutant androgen receptor polypeptides that are resistant to inhibition by androgen receptor inhibitors. Described herein are compositions, combinations, and kits that include mutant androgen receptor polypeptides, and methods of using mutant androgen receptor polypeptides. Further described herein are methods that use mutant androgen receptor polypeptides as screening agents for the identification and design of third generation androgen receptor modulators. Further described herein are third generation androgen receptor modulators that inhibit the activity of mutant androgen receptor polypeptides. Further described are pharmaceutical compositions and agents comprising the compounds described herein, and the treatment of diseases or conditions such as androgen receptor mediated or dependent cancers such as gonadectomy resistant prostate cancer. Therefore, such androgen receptor modulators are used alone and in combination with other compounds. |