IN THE SPOTLIGHT Resistance Emerges to Second-Generation Antiandrogens in Prostate Cancer

نویسندگان

  • William G. Nelson
  • Srinivasan Yegnasubramanian
چکیده

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 Research. Summary: The appearance of a mutant androgen receptor, ARF876L, 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. Cancer Discov; 3(9); 971–4. ©2013 AACR.

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

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 کامل

Resistance emerges to second-generation antiandrogens in prostate cancer.

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.

متن کامل

Progress in antiandrogen design targeting hormone binding pocket to circumvent mutation based resistance

Androgen receptor (AR) plays a critical role in the development and progression of prostate cancer (PCa). Current clinically used antiandrogens such as flutamide, bicalutamide, and newly approved enzalutamide mainly target the hormone binding pocket (HBP) of AR. However, over time, drug resistance invariably develops and switches these antiandrogens from antagonist to agonist of the AR. Accumul...

متن کامل

Discovery of ODM-201, a new-generation androgen receptor inhibitor targeting resistance mechanisms to androgen signaling-directed prostate cancer therapies

Activation of androgen receptor (AR) is crucial for prostate cancer growth. Remarkably, also castration-resistant prostate cancer (CRPC) is dependent on functional AR, and several mechanisms have been proposed to explain the addiction. Known causes of CRPC include gene amplification and overexpression as well as point mutations of AR. We report here the pharmacological profile of ODM-201, a nov...

متن کامل

The Effects of Ten Weeks Resistance Training on Resting Levels of Some Angiogenesis Factors Among Men with Prostate Cancer

Background: Prostate cancer is the second most prevalent canceramong men and the eighth leading cause of death in Iran. In pathological conditions, angiogenesis increases the chance of metastasis and thus spreads cancer. The aim of the present study was to examine the effects of 10 weeks of resistance training on some angiogenesis factors among men affected by prostate cancer. Materials and Me...

متن کامل

ذخیره در منابع من


  با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

عنوان ژورنال:

دوره   شماره 

صفحات  -

تاریخ انتشار 2013