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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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
Materias:	Science Q
Acceso en línea:	https://doaj.org/article/83045b413545471dafc949ec4db32b64
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spelling	oai:doaj.org-article:83045b413545471dafc949ec4db32b642021-12-02T16:50:07ZA structural mechanism for directing corepressor-selective inverse agonism of PPARγ10.1038/s41467-018-07133-w2041-1723https://doaj.org/article/83045b413545471dafc949ec4db32b642018-11-01T00:00:00Zhttps://doi.org/10.1038/s41467-018-07133-whttps://doaj.org/toc/2041-1723Peroxisome 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.Richard BrustJinsai ShangJakob FuhrmannSarah A. MosureJared BassAndrew CanoZahra HeidariIan M. ChrismanMichelle D. NemetchekAnne-Laure BlayoPatrick R. GriffinTheodore M. KameneckaTravis S. HughesDouglas J. KojetinNature PortfolioarticleScienceQENNature Communications, Vol 9, Iss 1, Pp 1-14 (2018)
institution	DOAJ
collection	DOAJ
language	EN
topic	Science Q
spellingShingle	Science Q 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 A structural mechanism for directing corepressor-selective inverse agonism of PPARγ
description	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.
format	article
author	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
author_facet	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
author_sort	Richard Brust
title	A structural mechanism for directing corepressor-selective inverse agonism of PPARγ
title_short	A structural mechanism for directing corepressor-selective inverse agonism of PPARγ
title_full	A structural mechanism for directing corepressor-selective inverse agonism of PPARγ
title_fullStr	A structural mechanism for directing corepressor-selective inverse agonism of PPARγ
title_full_unstemmed	A structural mechanism for directing corepressor-selective inverse agonism of PPARγ
title_sort	structural mechanism for directing corepressor-selective inverse agonism of pparγ
publisher	Nature Portfolio
publishDate	2018
url	https://doaj.org/article/83045b413545471dafc949ec4db32b64
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A structural mechanism for directing corepressor-selective inverse agonism of PPARγ

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