Perspectives on designs of antiandrogens for prostate cancer

摘要: The androgen receptor (AR) regulates gene transcription in many tissues and is profoundly important prostate cancer. Antiandrogens compete with the natural hormone are front line therapeutics to treat However, antiandrogens frequently become ineffective after prolonged treatment because of development tumor resistance. This paper reviews design principles for new generations antiandrogens: super antagonists surface allosteric modulators. Super compounds higher binding affinity than agonists that contain precisely engineered hydrophobic groups disrupt AR function. also an attractive alternative target. Surface inhibitors small molecules directly block receptor–co-activator interface, preventing co-activator recruitment. challenges designing these significant but so potential disease.