Abstract
The peroxisome proliferator-activated receptor gamma (PPAR gamma) was identified as an oncogene and it plays a key role in prostate cancer (PC) development and progression. PPAR gamma antagonists have been shown to inhibit PC cell growth. Herein, we describe a virtual screening-based approach that led to the discovery of novel PPAR gamma antagonist chemotypes that bind at the allosteric pocket. Arg288, Lys367, and His449 appear to be important for PPAR gamma antagonist binding.