Two steps, one ligand: How PPARγ binds small-molecule agonists

James J Siclari; Kevin H Gardner

doi:10.1016/j.str.2021.08.005

Two steps, one ligand: How PPARγ binds small-molecule agonists

Structure. 2021 Sep 2;29(9):935-936. doi: 10.1016/j.str.2021.08.005.

Authors

James J Siclari¹, Kevin H Gardner²

Affiliations

¹ Structural Biology Initiative, CUNY Advanced Science Research Center, New York, NY 10031, USA; Ph.D. Program in Biology, Graduate Center, City University of New York, NY 10016, USA.
² Structural Biology Initiative, CUNY Advanced Science Research Center, New York, NY 10031, USA; Department of Chemistry and Biochemistry, City College of New York, NY 10031, USA; Ph.D. Programs in Biology, Biochemistry, and Chemistry, Graduate Center, City University of New York, NY 10016, USA. Electronic address: kgardner@gc.cuny.edu.

Abstract

In this issue of Structure,Shang and Kojetin (2021) present insights into the binding mechanism of artificial agonists to the PPARγ nuclear receptor. These data support a two-step model with induced fit and conformational selection aspects. This mechanism may exist in related receptors, providing new opportunities for drug development.

Publication types

Research Support, N.I.H., Extramural
Research Support, U.S. Gov't, Non-P.H.S.
Comment

MeSH terms

Ligands
PPAR gamma*
Thiazolidinediones*

Substances

Ligands
PPAR gamma
Thiazolidinediones

Grants and funding

R01 GM106239/GM/NIGMS NIH HHS/United States