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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Vydáno v:Nat Commun
Hlavní autoři: 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.
Médium: Artigo
Jazyk:Inglês
Vydáno: Nature Publishing Group UK 2018
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Article
On-line přístup: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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