INT131: a selective modulator of PPAR gamma.

  title={INT131: a selective modulator of PPAR gamma.},
  author={Alykhan Motani and Zhulun Wang and Jennifer V Weiszmann and Lawrence R. McGee and Gary P Lee and Qingxiang Liu and Jocelyn Staunton and Zexu Fang and Helen Fuentes and Michelle Lindstrom and Jinsong Liu and Donna H T Biermann and Juan A. Ja{\'e}n and Nigel P. C. Walker and R. Marc Learned and Jin-long Chen and Yang Li},
  journal={Journal of molecular biology},
  volume={386 5},
The nuclear hormone receptor peroxisome proliferator-activated receptor gamma (PPAR gamma; NR1C3) plays a central role in adipogenesis and is the molecular target of the thiazolidinedione class of antidiabetic drugs. To overcome the well-known shortcomings of thiazolidinediones, we have identified INT131 (formerly T131 and AMG131) as a potent selective ligand for PPAR gamma that is structurally and pharmacologically distinct from glitazone agonists. In vitro biochemical and cell-based… CONTINUE READING
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