Abstract
The metabolic syndrome is strongly associated with insulin resistance and consists of a constellation of factors such as hypertension and hyperlipidemia that raise the risk for cardiovascular diseases and diabetes mellitus. There is widespread agreement that the renin-angiotensin system (RAS) plays a pivotal role in the pathogenesis of insulin resistance and cardiovascular disease in diabetes. Indeed, large clinical trials have demonstrated substantial benefit of the blockade of this system for cardiovascular end-organ protection. Thus the blockade of the RAS may be a promising strategy for the treatment of the patients with the metabolic syndrome. Although several types of angiotensin II type 1 (AT1) receptor blockers (ARBs) are commercially available for the treatment of patients with hypertension, we have recently found that telmisartan (Micardis®) could have the strongest binding affinity to AT1 receptor. Further, telmisartan is reported to act as a partial agonist of peroxisome proliferator-activated receptor-γ (PPAR-γ). These observations suggest that, due to its unique PPAR-γ-modulating activity, telmisartan may be one of the most promising sartans for the treatment of cardiometabolic disorders. In this paper, we reviewed the potential utility of telmisartan in insulin resistance and vascular complications in diabetes.
Keywords: AGEs, angiotensin II, diabetic vascular complications, insulin resistance, PPAR-γ, RAGE
Current Molecular Medicine
Title: Potential Utility of Telmisartan, an Angiotensin II Type 1 Receptor Blocker with Peroxisome Proliferator-Activated Receptor-γ (PPAR-γ)-Modulating Activity for the Treatment of Cardiometabolic Disorders
Volume: 7 Issue: 5
Author(s): Sho-ichi Yamagishi, Kazuo Nakamura and Takanori Matsui
Affiliation:
Keywords: AGEs, angiotensin II, diabetic vascular complications, insulin resistance, PPAR-γ, RAGE
Abstract: The metabolic syndrome is strongly associated with insulin resistance and consists of a constellation of factors such as hypertension and hyperlipidemia that raise the risk for cardiovascular diseases and diabetes mellitus. There is widespread agreement that the renin-angiotensin system (RAS) plays a pivotal role in the pathogenesis of insulin resistance and cardiovascular disease in diabetes. Indeed, large clinical trials have demonstrated substantial benefit of the blockade of this system for cardiovascular end-organ protection. Thus the blockade of the RAS may be a promising strategy for the treatment of the patients with the metabolic syndrome. Although several types of angiotensin II type 1 (AT1) receptor blockers (ARBs) are commercially available for the treatment of patients with hypertension, we have recently found that telmisartan (Micardis®) could have the strongest binding affinity to AT1 receptor. Further, telmisartan is reported to act as a partial agonist of peroxisome proliferator-activated receptor-γ (PPAR-γ). These observations suggest that, due to its unique PPAR-γ-modulating activity, telmisartan may be one of the most promising sartans for the treatment of cardiometabolic disorders. In this paper, we reviewed the potential utility of telmisartan in insulin resistance and vascular complications in diabetes.
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Cite this article as:
Sho-ichi Yamagishi , Kazuo Nakamura and Takanori Matsui , Potential Utility of Telmisartan, an Angiotensin II Type 1 Receptor Blocker with Peroxisome Proliferator-Activated Receptor-γ (PPAR-γ)-Modulating Activity for the Treatment of Cardiometabolic Disorders, Current Molecular Medicine 2007; 7 (5) . https://dx.doi.org/10.2174/156652407781387073
DOI https://dx.doi.org/10.2174/156652407781387073 |
Print ISSN 1566-5240 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5666 |
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