Article
Overcoming mutation-based resistance to antiandrogens with rational drug design.
eLife - 9 Apr 2013
Balbas Minna D, Evans Michael J, Hosfield David J, Wongvipat John, Arora Vivek K, Watson Philip A, Chen Yu, Greene Geoffrey L, Shen Yang, Sawyers Charles L
Abstract excerpt
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-based mutagenesis...
Topics
- Androgen Antagonists
- Cell Line
- Drug Design
- Drug Resistance, Neoplasm
- Humans
- Male
- Molecular Dynamics Simulation
- Mutation
- Prostatic Neoplasms