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Multitargeted bioactive ligands for PPAR s discovered in the last decade
Author(s) -
Zhang Jun,
Liu Xin,
Xie XianBin,
Cheng XianChao,
Wang RunLing
Publication year - 2016
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12806
Subject(s) - rosiglitazone , ppar agonist , peroxisome proliferator activated receptor , partial agonist , agonist , type 2 diabetes , pharmacology , receptor , insulin resistance , medicine , diabetes mellitus , chemistry , endocrinology
Type 2 diabetes took insulin resistance as the main clinical manifestation. PPAR s have been reported to be the therapeutic targets of metabolic disorders, such as obesity, hypertension, diabetes, and cardiovascular disease. Previously, PPAR γ agonist rosiglitazone was restricted in clinic due to cardiomyocytes infarction, weight gain, and other serious side‐effects, which were mainly due to the single and selective PPAR γ agonism. In recent years, multitarget‐directed PPAR agonists with synergistic reaction as well as fewer side‐effect have been the hot topic in designing promising agents. In this review, we updated and generalized the development of PPAR γ partial agonists, PPAR γ antagonists, PPAR α/γ dual agonists, PPAR δ partial agonists, PPAR δ antagonists, PPAR α/δ dual agonists, PPAR γ/δ dual agonists, and PPAR α/γ/δ pan‐agonists published in recent decade. Most of these molecules were modified from known structures or came from high‐throughput screening. Among these molecules, some were expected to be promising drugs against metabolic disorders, while others seemed to provide new insight for designing novel PPAR agents.