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ID: ALA4823312
Journal: Bioorg Med Chem
Title: Virtual screening and biological evaluation of PPARγ antagonists as potential anti-prostate cancer agents.
Authors: Almahmoud S, Elix CC, Jones JO, Hopkins CR, Vennerstrom JL, Zhong HA.
Abstract: The peroxisome proliferator-activated receptor gamma (PPARγ) was identified as an oncogene and it plays a key role in prostate cancer (PC) development and progression. PPARγ antagonists have been shown to inhibit PC cell growth. Herein, we describe a virtual screening-based approach that led to the discovery of novel PPARγ antagonist chemotypes that bind at the allosteric pocket. Arg288, Lys367, and His449 appear to be important for PPARγ antagonist binding.
CiteXplore: 34433102