Probing the Complex Binding Modes of the PPARγ Partial Agonist 2-chloro-N-(3-chloro-4-((5-chlorobenzo[d]thiazol-2-yl)thio)phenyl)-4-(trifluoromethyl)benzenesulfonamide (T2384) to Orthosteric and Allosteric Sites with NMR Spectroscopy

In a previous study, a co-crystal structure of PPARγ bound to 2-chloro-N-(3-chloro-4-((5-chlorobenzo[d]thiazol-2-yl)thio)phenyl)-4-(trifluoromethyl)benzenesulfonamide (1, T2384) revealed two orthosteric pocket binding modes attributed to a concentration-dependent biochemical activity profile. Howeve...

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Udgivet i:J Med Chem
Main Authors: Hughes, Travis S., Shang, Jinsai, Brust, Richard, de Vera, Ian Mitchelle S., Fuhrmann, Jakob, Ruiz, Claudia, Cameron, Michael D., Kamenecka, Theodore M., Kojetin, Douglas J.
Format: Artigo
Sprog:Inglês
Udgivet: 2016
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Article
Online adgang:https://ncbi.nlm.nih.gov/pmc/articles/PMC5179221/
https://ncbi.nlm.nih.gov/pubmed/27783520
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.6b01340
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