Resistance emerges to second-generation antiandrogens in prostate cancer.
نویسندگان
چکیده
The appearance of a mutant androgen receptor, AR(F876L), in prostate cancer cells chronically exposed to enzalutamide or ARN-509 promotes a switch from antagonist to agonist receptor function, undermining the potential long-term effectiveness of these second-generation antiandrogen drugs.
منابع مشابه
A clinically relevant androgen receptor mutation confers resistance to second-generation antiandrogens enzalutamide and ARN-509.
UNLABELLED Despite the impressive clinical activity of the second-generation antiandrogens enzalutamide and ARN-509 in patients with prostate cancer, acquired resistance invariably emerges. To identify the molecular mechanisms underlying acquired resistance, we developed and characterized cell lines resistant to ARN-509 and enzalutamide. In a subset of cell lines, ARN-509 and enzalutamide exhib...
متن کاملIN THE SPOTLIGHT Resistance Emerges to Second-Generation Antiandrogens in Prostate Cancer
Authors’ Affi liation: Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins, Baltimore, Maryland Corresponding Author: William G. Nelson, Sidney Kimmel Comprehensive Cancer Center, Suite 1100, Weinberg Building, 401 North Broadway, Baltimore, MD 21231. Phone: 410-955-8822; Fax: 410-955-6787; E-mail: [email protected] doi: 10.1158/2159-8290.CD-13-0405 ©2013 American Association for Cancer R...
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The second-generation antiandrogen enzalutamide was recently approved for patients with castration-resistant prostate cancer. Despite its success, the duration of response is often limited. For previous antiandrogens, one mechanism of resistance is mutation of the androgen receptor (AR). To prospectively identify AR mutations that might confer resistance to enzalutamide, we performed a reporter...
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ورودعنوان ژورنال:
- Cancer discovery
دوره 3 9 شماره
صفحات -
تاریخ انتشار 2013