Updated research progress of selective PPARγ modulators
10.16438/j.0513-4870.2020-1022
- VernacularTitle:选择性PPARγ调节剂的研究新进展
- Author:
Yi HUAN
;
Jun PENG
;
Xuan PAN
;
Zhan-zhu LIU
;
Zhu-fang SHEN
- Publication Type:Research Article
- Keywords:
peroxisome proliferator-activated receptor γ;
selective PPARγ modulator;
insulin resistance;
iabetes mellitus;
nonalcoholic fatty liver disease
- From:
Acta Pharmaceutica Sinica
2021;56(2):352-359
- CountryChina
- Language:Chinese
-
Abstract:
Thiazolidinediones (TZDs) are currently the only recognized insulin sensitizers available for the clinical treatment of type 2 diabetes. Although their advantages are recognized, the profiles of numerous adverse effects hinder the continued use of these drugs. Peroxisome proliferator-activated receptor γ (PPARγ) is known as a receptor for TZDs, and its underlying mechanisms of pharmacological actions and adverse effects have been deeply explored. To maximally preserve the PPARγ-mediated insulin sensitizing effects and reduce the occurrence of related adverse effects, the concept of "selective PPARγ modulators (SPPARMs)" has been proposed and developed, guiding the development of new drugs. In this review, we summarize the recent research progress in the definition of SPPARMs, the candidate classification and the molecular underpinnings, as well as present the discovery of the YR series compounds as an example, and discuss the potential application prospects of SPPARMs.
