Literature DB >> 34478635

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

James J Siclari1, Kevin H Gardner2.   

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.
Copyright © 2021 Elsevier Ltd. All rights reserved.

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Year:  2021        PMID： 34478635      PMCID： PMC8819882          DOI： 10.1016/j.str.2021.08.005

Source DB:  PubMed          Journal:  Structure        ISSN： 0969-2126            Impact factor:   5.006


  10 in total

1.  Ligand-escape pathways from the ligand-binding domain of PPARgamma receptor as probed by molecular dynamics simulations.

Authors:  D Genest; N Garnier; A Arrault; C Marot; L Morin-Allory; M Genest
Journal:  Eur Biophys J       Date:  2007-10-11       Impact factor: 1.733

Review 2.  Small molecule modulation of nuclear receptor conformational dynamics: implications for function and drug discovery.

Authors:  Douglas J Kojetin; Thomas P Burris
Journal:  Mol Pharmacol       Date:  2012-08-06       Impact factor: 4.436

Review 3.  The multifaceted factor peroxisome proliferator-activated receptor γ (PPARγ) in metabolism, immunity, and cancer.

Authors:  Jung-Hoon Kim; Jaewhan Song; Kye Won Park
Journal:  Arch Pharm Res       Date:  2015-01-13       Impact factor: 4.946

4.  New PPARG mutation leads to lipodystrophy and loss of protein function that is partially restored by a synthetic ligand.

Authors:  Angelika Lüdtke; Janine Buettner; Hartmut H-J Schmidt; Howard J Worman
Journal:  J Med Genet       Date:  2007-09       Impact factor: 6.318

5.  Coupling of receptor conformation and ligand orientation determine graded activity.

Authors:  John B Bruning; Alexander A Parent; German Gil; Min Zhao; Jason Nowak; Margaret C Pace; Carolyn L Smith; Pavel V Afonine; Paul D Adams; John A Katzenellenbogen; Kendall W Nettles
Journal:  Nat Chem Biol       Date:  2010-10-10       Impact factor: 15.040

6.  An antidiabetic thiazolidinedione is a high affinity ligand for peroxisome proliferator-activated receptor gamma (PPAR gamma).

Authors:  J M Lehmann; L B Moore; T A Smith-Oliver; W O Wilkison; T M Willson; S A Kliewer
Journal:  J Biol Chem       Date:  1995-06-02       Impact factor: 5.157

7.  A Pharmacogenetic Approach to the Treatment of Patients With PPARG Mutations.

Authors:  Maura Agostini; Erik Schoenmakers; Junaid Beig; Louise Fairall; Istvan Szatmari; Odelia Rajanayagam; Frederick W Muskett; Claire Adams; A David Marais; Stephen O'Rahilly; Robert K Semple; Laszlo Nagy; Amit R Majithia; John W R Schwabe; Dirk J Blom; Rinki Murphy; Krishna Chatterjee; David B Savage
Journal:  Diabetes       Date:  2018-04-05       Impact factor: 9.461

8.  Structural mechanism underlying ligand binding and activation of PPARγ.

Authors:  Jinsai Shang; Douglas J Kojetin
Journal:  Structure       Date:  2021-03-12       Impact factor: 5.871

9.  A molecular switch regulating transcriptional repression and activation of PPARγ.

Authors:  Jinsai Shang; Sarah A Mosure; Jie Zheng; Richard Brust; Jared Bass; Ashley Nichols; Laura A Solt; Patrick R Griffin; Douglas J Kojetin
Journal:  Nat Commun       Date:  2020-02-19       Impact factor: 14.919

Review 10.  PPARγ in Ischemia-Reperfusion Injury: Overview of the Biology and Therapy.

Authors:  Ruizhen Huang; Chiyu Zhang; Xing Wang; Honglin Hu
Journal:  Front Pharmacol       Date:  2021-04-28       Impact factor: 5.810
  10 in total

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