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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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Detalles Bibliográficos
Autores principales: 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.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Nature Publishing Group UK 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6224492/
https://www.ncbi.nlm.nih.gov/pubmed/30409975
http://dx.doi.org/10.1038/s41467-018-07133-w