A molecular switch regulating transcriptional repression and activation of PPARγ

Structural studies of nuclear receptor transcription factors revealed that nearly all nuclear receptors share a conserved helix 12 dependent transcriptional activation mechanism. Here the authors present two crystal structures of peroxisome proliferator-activated receptor gamma (PPARγ) in an inverse...

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Autores principales: Jinsai Shang, Sarah A. Mosure, Jie Zheng, Richard Brust, Jared Bass, Ashley Nichols, Laura A. Solt, Patrick R. Griffin, Douglas J. Kojetin
Formato: article
Lenguaje:EN
Publicado: Nature Portfolio 2020
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Acceso en línea:https://doaj.org/article/9d32e7db99b24a56b787934b31a56130
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Sumario:Structural studies of nuclear receptor transcription factors revealed that nearly all nuclear receptors share a conserved helix 12 dependent transcriptional activation mechanism. Here the authors present two crystal structures of peroxisome proliferator-activated receptor gamma (PPARγ) in an inverse agonist/corepressor-bound transcriptionally repressive conformation, where helix 12 is located within the orthosteric ligand-binding pocket instead, and discuss mechanistic implications.