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.

Rapid, potent, and persistent covalent chemical probes to deconvolute PI3Kα signaling

Lukas Bissegger,  Theodora A. Constantin,  Erhan Keles,  Luka Raguž,   Isobel Barlow-Busch,  Clara Orbegozo,   Thorsten Schaefer,  Valentina...