Molecular tuning of farnesoid X receptor partial agonism

The ligand-activated transcription factor farnesoid X receptor (FXR) acts as a cellular sensor for bile acids and is of interest as a drug target. Here the authors employ X-ray crystallography and NMR to characterize the molecular determinants of FXR agonists, antagonists and a partial agonist that...

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Autores principales:	Daniel Merk, Sridhar Sreeramulu, Denis Kudlinzki, Krishna Saxena, Verena Linhard, Santosh L. Gande, Fabian Hiller, Christina Lamers, Ewa Nilsson, Anna Aagaard, Lisa Wissler, Niek Dekker, Krister Bamberg, Manfred Schubert-Zsilavecz, Harald Schwalbe
Formato:	article
Lenguaje:	EN
Publicado:	Nature Portfolio 2019
Materias:	Science Q
Acceso en línea:	https://doaj.org/article/6e7a5ba2682343c4b07e17fc173490a6
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spelling	oai:doaj.org-article:6e7a5ba2682343c4b07e17fc173490a62021-12-02T15:35:47ZMolecular tuning of farnesoid X receptor partial agonism10.1038/s41467-019-10853-22041-1723https://doaj.org/article/6e7a5ba2682343c4b07e17fc173490a62019-07-01T00:00:00Zhttps://doi.org/10.1038/s41467-019-10853-2https://doaj.org/toc/2041-1723The ligand-activated transcription factor farnesoid X receptor (FXR) acts as a cellular sensor for bile acids and is of interest as a drug target. Here the authors employ X-ray crystallography and NMR to characterize the molecular determinants of FXR agonists, antagonists and a partial agonist that drive FXR activation and antagonism.Daniel MerkSridhar SreeramuluDenis KudlinzkiKrishna SaxenaVerena LinhardSantosh L. GandeFabian HillerChristina LamersEwa NilssonAnna AagaardLisa WisslerNiek DekkerKrister BambergManfred Schubert-ZsilaveczHarald SchwalbeNature PortfolioarticleScienceQENNature Communications, Vol 10, Iss 1, Pp 1-14 (2019)
institution	DOAJ
collection	DOAJ
language	EN
topic	Science Q
spellingShingle	Science Q Daniel Merk Sridhar Sreeramulu Denis Kudlinzki Krishna Saxena Verena Linhard Santosh L. Gande Fabian Hiller Christina Lamers Ewa Nilsson Anna Aagaard Lisa Wissler Niek Dekker Krister Bamberg Manfred Schubert-Zsilavecz Harald Schwalbe Molecular tuning of farnesoid X receptor partial agonism
description	The ligand-activated transcription factor farnesoid X receptor (FXR) acts as a cellular sensor for bile acids and is of interest as a drug target. Here the authors employ X-ray crystallography and NMR to characterize the molecular determinants of FXR agonists, antagonists and a partial agonist that drive FXR activation and antagonism.
format	article
author	Daniel Merk Sridhar Sreeramulu Denis Kudlinzki Krishna Saxena Verena Linhard Santosh L. Gande Fabian Hiller Christina Lamers Ewa Nilsson Anna Aagaard Lisa Wissler Niek Dekker Krister Bamberg Manfred Schubert-Zsilavecz Harald Schwalbe
author_facet	Daniel Merk Sridhar Sreeramulu Denis Kudlinzki Krishna Saxena Verena Linhard Santosh L. Gande Fabian Hiller Christina Lamers Ewa Nilsson Anna Aagaard Lisa Wissler Niek Dekker Krister Bamberg Manfred Schubert-Zsilavecz Harald Schwalbe
author_sort	Daniel Merk
title	Molecular tuning of farnesoid X receptor partial agonism
title_short	Molecular tuning of farnesoid X receptor partial agonism
title_full	Molecular tuning of farnesoid X receptor partial agonism
title_fullStr	Molecular tuning of farnesoid X receptor partial agonism
title_full_unstemmed	Molecular tuning of farnesoid X receptor partial agonism
title_sort	molecular tuning of farnesoid x receptor partial agonism
publisher	Nature Portfolio
publishDate	2019
url	https://doaj.org/article/6e7a5ba2682343c4b07e17fc173490a6
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Molecular tuning of farnesoid X receptor partial agonism

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