Novel compounds are in development, which are selective PPAR modulators (SPPARMs) and have more potent PPAR-alpha agonist activity. These may prove to have advantages in the treatment of dyslipidemia, insulin resistance and non-alcoholic fatty liver disease (NAFLD).Liu, Zhong-MinHu, MiaoChan, ...
Cevoglitazar, a Novel Peroxisome Proliferator-Activated Receptor-α/γ Dual Agonist, Potently Reduces Food Intake and Body Weight in Obese Mice and Cynomol... Dual activation of PPARalpha and -gamma is a therapeutic approach in development for the treatment of type 2 diabetes mellitus and ...
There remains an acute need for development of safe and effective drugs for the treatment of NASH. The current study evaluated the effects of saroglitazar, a PPAR-α/γ agonist in a preclinical model of NASH. It demonstrated a systemic effect of the drug with decreased weight gain, improved...
Fibrates are widely used hypolipidemic drugs that regulate the expression of many genes involved in lipid metabolism by activating the peroxisome proliferator-activated receptor alpha (PPARalpha). The objective of this study was to investigate the mechanism of action of peroxisome proliferators and PPAR...
Structure of the PPARalpha and -gamma ligand binding domain in complex with AZ 242; ligand selectivity and agonist activation in the PPAR family Structure (2001) K.M. Darwish et al. Design, synthesis, and biological evaluation of novel thiazolidinediones as PPARgamma/FFAR1 dual agonists Eur. J...
KasaiS,Inoue T,Yoshitomi H,et al.Antidiabetic and hypolipidemic effects of a novel dual peroxisome proliferator-activated receptor(PPAR)alpha/gamma agonist,... SJ Nicholls,AM Lincoff,RR Henry,... 被引量: 5发表: 2010年 The ligands/activators for peroxisome proliferator-activated receptor alpha (...
The PPAR receptors have 3 identified subtypes: PPARα, PPARβ and PPARγ, all of which have been treated as attractive targets for developing drugs to treat type 2 diabetes. Due to the undesirable side-effects, many PPAR agonists including PPARα/γ and PPARβ/γ dual agonists are stopped ...
Therapeutic Potential of Aleglitazar, a New Dual PPAR-α/γ Agonist Preventing morbidity and mortality from diabetes mellitus is of paramount importance as the incidence of this disease is increasing across the world. While... MA Cavender,...
Am J Cardiovasc Drugs 2002; 2: 125–32. 15 Nissen SE, Nicholls SJ, Wolski K, Howey DC, McErlean E, Wang MD, et al. Effects of a potent and selective PPAR-alpha agonist in patients with atherogenic dyslipidemia or hypercholesterolemia: two randomized controlled trials. JAMA 2007; 297: ...
Different binding and recognition modes of Gl479, a dual agonist of peroxisome proliferator-activated receptor Alpha/Gamma. J Struct Biol. 2015;191:332. Article PubMed CAS Google Scholar Traves PG, Hortelano S, Zeini M, Chao TH, Lam T, Neuteboom ST, et al. Selective activation of liver ...