Sunday, September 22, 2024

Nuclear Receptors: A new mode of inhibition

  1. Andrew D Huber, 
  1. Taosheng Chen
  2.  
eLife 2024, 13:e101446.

https://doi.org/10.7554/eLife.101446

The article presents the discussion on interaction of covalent inhibitors GW9662 and T0070907 with the peroxisome proliferator-activated receptor gamma (PPARγ), revealing new insights into how these compounds influence receptor activity. Topics include the role of PPARγ in regulating fatty tissue and glucose levels; and the effects of covalent inhibitors on PPARγ's ligand-binding site and its interaction with co-activators and co-repressors.

Dual-Site Covalent Targeting Enables BD2-Selective BET Inhibition With Potent Antitumor Activity in Mice

Jibo Kang, Xuan Wang, Hong Zhang, Jieying Lin, Peng Chen, Zuqin Wang, Zengjun Hao, Fengfei Miao, Fengcai Zhang, Tao Li, Yusheng Xie, Junjian...