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

Small chemical modifications can have significant effects on ligand efficacy and receptor activity, but the underlying structural mechanisms can be difficult to predict from static crystal structures alone. Here we show how a simple phenyl-to-pyridyl substitution between two common covalent orthoste...

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Bibliographic Details
Published in:Nat Commun
Main Authors: Brust, Richard, Shang, Jinsai, Fuhrmann, Jakob, Mosure, Sarah A., Bass, Jared, Cano, Andrew, Heidari, Zahra, Chrisman, Ian M., Nemetchek, Michelle D., Blayo, Anne-Laure, Griffin, Patrick R., Kamenecka, Theodore M., Hughes, Travis S., Kojetin, Douglas J.
Format: Artigo
Language:Inglês
Published: Nature Publishing Group UK 2018
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Article
Online Access:https://ncbi.nlm.nih.gov/pmc/articles/PMC6224492/
https://ncbi.nlm.nih.gov/pubmed/30409975
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1038/s41467-018-07133-w
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