Molecular Characterization of New Selective Peroxisome Proliferator–Activated Receptor γ Modulators With Angiotensin Receptor Blocking Activity

Telmisartan inhibits AGE-induced C-reactive protein production through downregulation of the receptor for AGE via peroxisome proliferator-activated receptor-gamma activation

“…Recently, telmisartan has been shown to have a unique property that activates PPAR-γ [4,7]. Since PPAR-γ influences gene expression involved in carbohydrate and lipid metabolism, and since ligands for PPAR-γ can improve insulin sensitivity, telmisartan could be a promising 'cardiometabolic sartan' that targets both diabetes and cardiovascular disease in patients with hypertension [7].…”

“…Since PPAR-γ influences gene expression involved in carbohydrate and lipid metabolism, and since ligands for PPAR-γ can improve insulin sensitivity, telmisartan could be a promising 'cardiometabolic sartan' that targets both diabetes and cardiovascular disease in patients with hypertension [7]. Indeed, a recent clinical report has shown that replacement of valsartan and candesartan by telmisartan improves insulin resistance and decreases CRP levels in hypertensive patients with type 2 diabetes [8].…”

Telmisartan and Irbesartan Therapy in Type 2 Diabetic Patients Treated with Rosiglitazone: Effects on Insulin-Resistance, Leptin and Tumor Necrosis Factor-.ALPHA.

“…Recently, Schupp et al . demonstrated in vitro that telmisartan and irbesartan could be considered partial and selective peroxisome proliferator-activated receptor (PPAR) γ modulators ( 8 ). The aim of our study was to investigate the metabolic effect of telmisartan and irbesartan in subjects treated with rosiglitazone, a well-known insulin-sensitizing drug, in order to clarify the direct metabolic effects of the two former drugs.…”

Orphan nuclear receptors in drug discovery

“…It encompasses the principle of chemical alteration of PPAR-specific ligands to create compounds that selectively activate specific PPAR functions. For example, selective PPARγ modulation could lead to potent insulin sensitization without adverse effects such as weight gain [32]. Several compounds have now been identified as SPPARMs, and some of them are already in clinical testing [32][33][34][35].…”

“…For example, selective PPARγ modulation could lead to potent insulin sensitization without adverse effects such as weight gain [32]. Several compounds have now been identified as SPPARMs, and some of them are already in clinical testing [32][33][34][35]. In addition, pan-agonists combining PPARα, γ, and δ agonism have the potential to improve insulin resistance and dyslipidemia without causing weight gain.…”