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.

Fragment-Based Covalent Targeting of Lysines at the Allosteric Latch Site of SHP2.

  Vincenzo Di Lorenzo , Noémi Csorba , Renáta Szabó , Levente Kollár , Yvette Roske , Ivan Rand̵elović , Krisztina Balázs , Tibor Vikt...