机构：[1]Department of Nephrology, Kidney Research Institute,West China Hospital, West China Medical School of Sichuan University, Chengdu, People’s Republic of China四川大学华西医院[2]State Key Laboratory of Biotherapy and Cancer Center/Collaborative Innovation Center of Biotherapy, West China Hospital, West China Medical School of Sichuan University, Chengdu, People’s Republic of China四川大学华西医院
Peroxisome proliferator-activated receptor gamma (PPARγ) is a ligand-mediated transcription factor playing key roles in glucose and lipid homeostasis, and PPARγ ligands possess therapeutic potential in these as well as other areas. In this study, a series of phenylthiazole acids have been synthesized and evaluated for agonistic activity by a convenient fluorescence polarization-based PPARγ ligand screening assay. Compound 4t, as a potential PPARγ agonist with half maximal effective concentration (EC50) 0.75±0.20 μM, exhibited in vitro potency comparable with a 0.83±0.14 μM of the positive control rosiglitazone. Molecular docking and molecular dynamics simulations indicated that phenylthiazole acid 4t interacted with the amino acid residues of the active site of the PPARγ complex in a stable manner, consistent with the result of the in vitro ligand assay.
基金：
the Natural Science Foundation of China (no 81402782) and the China Postdoctoral Science Foundation (no 2015T80985).
语种：
外文
PubmedID：
中科院(CAS)分区：
出版当年[2016]版：
大类|3 区医学
小类|3 区药物化学3 区药学
最新[2023]版：
大类|2 区医学
小类|2 区药物化学2 区药学
第一作者：
第一作者机构：[1]Department of Nephrology, Kidney Research Institute,West China Hospital, West China Medical School of Sichuan University, Chengdu, People’s Republic of China[*1]Division of Nephrology, Kidney Research Institute, West China Hospital, West China Medical School of Sichuan University, No 37 Guoxue Xiang, Chengdu 610041, People’s Republic of C hina
共同第一作者：
通讯作者：
通讯机构：[1]Department of Nephrology, Kidney Research Institute,West China Hospital, West China Medical School of Sichuan University, Chengdu, People’s Republic of China[2]State Key Laboratory of Biotherapy and Cancer Center/Collaborative Innovation Center of Biotherapy, West China Hospital, West China Medical School of Sichuan University, Chengdu, People’s Republic of China[*1]Division of Nephrology, Kidney Research Institute, West China Hospital, West China Medical School of Sichuan University, No 37 Guoxue Xiang, Chengdu 610041, People’s Republic of C hina[*2]S tate Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China Medical School of Sichuan University, Chengdu 610041, People’s Republic of China
推荐引用方式(GB/T 7714)：
Ma Liang,Wang Taijin,Shi Min,et al.Synthesis, activity, and docking study of phenylthiazole acids as potential agonists of PPARγ.[J].Drug design, development and therapy.2016,10:1807-15.doi:10.2147/DDDT.S106406.
APA：
Ma Liang,Wang Taijin,Shi Min&Ye Haoyu.(2016).Synthesis, activity, and docking study of phenylthiazole acids as potential agonists of PPARγ..Drug design, development and therapy,10,
MLA：
Ma Liang,et al."Synthesis, activity, and docking study of phenylthiazole acids as potential agonists of PPARγ.".Drug design, development and therapy 10.(2016):1807-15
