Llwytho...

Modification of the Orthosteric PPARγ Covalent Antagonist Scaffold Yields an Improved Dual-Site Allosteric Inhibitor

GW9662 and T0070907 are widely used commercially available irreversible antagonists of peroxisome proliferator-activated receptor gamma (PPARγ). These antagonists covalently modify Cys285 located in an orthosteric ligand-binding pocket embedded in the PPARγ ligand-binding domain and are used to bloc...

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Wedi'i Gadw mewn:
Manylion Llyfryddiaeth
Cyhoeddwyd yn:ACS Chem Biol
Prif Awduron: Brust, Richard, Lin, Hua, Fuhrmann, Jakob, Asteian, Alice, Kamenecka, Theodore M., Kojetin, Douglas J.
Fformat: Artigo
Iaith:Inglês
Cyhoeddwyd: 2017
Pynciau:
Mynediad Ar-lein:https://ncbi.nlm.nih.gov/pmc/articles/PMC5652320/
https://ncbi.nlm.nih.gov/pubmed/28165718
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acschembio.6b01015
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