Identification of a novel PPARγ modulator with good anti-diabetic therapeutic index via structure-based screening, optimization and biological validation

PPARγ is well-known as the target receptor of TZD anti-diabetic drugs. However, recently the therapeutic benefits of these TZD drugs have been compromised by many severe side effects because of their full PPARγ agonistic action to lock the AF-2 helix. Herein, we conducted a virtual screening in the...

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Bibliographic Details
Main Authors: Fangyuan Chen, Lei Ma, Guihui Cai, Junyuan Tang, Yi Wang, Qingmei Liu, Xiawen Liu, Ning Hou, Zhi Zhou, Wei Yi
Format: Article
Language:English
Published: Elsevier 2022-10-01
Series:Biomedicine & Pharmacotherapy
Subjects:
Online Access:http://www.sciencedirect.com/science/article/pii/S0753332222010423