Structural basis of altered potency and efficacy displayed by a major in vivo metabolite of the anti-diabetic PPARγ drug pioglitazone

Pioglitazone (Pio) is an FDA-approved drug for type 2 diabetes that binds and activates the nuclear receptor PPARγ. yet it remains unclear how in vivo Pio metabolites affect PPARγ structure and function. Here, we present a structure-function comparison of Pio and its most abundant in vivo metabolite...

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Vydáno v:J Med Chem
Hlavní autoři: Mosure, Sarah A., Shang, Jinsai, Eberhardt, Jerome, Brust, Richard, Zheng, Jie, Griffin, Patrick R., Forli, Stefano, Kojetin, Douglas J.
Médium: Artigo
Jazyk:Inglês
Vydáno: 2019
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On-line přístup:https://ncbi.nlm.nih.gov/pmc/articles/PMC6898968/
https://ncbi.nlm.nih.gov/pubmed/30676741
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.8b01573
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