A structural mechanism for directing corepressor-selective inverse agonism of PPARγ

A structural mechanism for directing corepressor-selective inverse agonism of PPARγ

Peroxisome proliferator-activated receptor gamma (PPARγ) is a target for insulin sensitizing drugs. Here the authors combine NMR, X-ray crystallography and MD simulations and report a structural mechanism for eliciting PPARγ inverse agonism, where coactivator binding is inhibited and corepressor bin...

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Detalles Bibliográficos
Autores principales: Richard Brust, Jinsai Shang, Jakob Fuhrmann, Sarah A. Mosure, Jared Bass, Andrew Cano, Zahra Heidari, Ian M. Chrisman, Michelle D. Nemetchek, Anne-Laure Blayo, Patrick R. Griffin, Theodore M. Kamenecka, Travis S. Hughes, Douglas J. Kojetin
Formato: article
Lenguaje:EN
Publicado: Nature Portfolio 2018
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Science
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Acceso en línea:https://doaj.org/article/83045b413545471dafc949ec4db32b64
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Sumario:Peroxisome proliferator-activated receptor gamma (PPARγ) is a target for insulin sensitizing drugs. Here the authors combine NMR, X-ray crystallography and MD simulations and report a structural mechanism for eliciting PPARγ inverse agonism, where coactivator binding is inhibited and corepressor binding promoted, which causes PPARγ repression.

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