Abstract
Dual agonism of glucagon and glucagon-like peptide-1 (GLP-1) receptors reduces body weight without inducing hyperglycemia. In addition, coagonists have demonstrated lipid lowering property, which was independent of their anorectic effect. Similarly, GLP-1 modulates cardiovascular function which is favorable for treatment of myocardial injury, cardiac dysfunction, cardiac arrhythmias, endothelial dysfunction, and blood pressure, while glucagon has a positive impact on heart rate, cardiac output, ventricular contraction and enhances cardiac performance in animals and humans. Hence, researchers focused on combining these attributes of GLP-1 and glucagon in a single molecule, which was termed as a coagonist. Oxyntomodulin is the naturally occurring coagonist of GLP-1 and glucagon. This review focusses on the coagonists under clinical development discussing activities affecting cardiovascular functions, lipid modulation, direct effect on cardiac functions or other related functions. A comparative analysis of the in vitro and in vivo properties of GLP-1, glucagon and the coagonists is also carried out. This review discusses potential of GLP-1 and glucagon coagonists in treatment of cardiovascular and hemodynamic diseases with attention to GLP-1 or glucagon receptor specific properties as well as the interaction between other therapies.
Keywords: Cardiovascular effect, coagonist, GLP-1, Glucagon and oxyntomodulin.
Cardiovascular & Hematological Agents in Medicinal Chemistry
Title:Therapeutic Potential of Coagonists of Glucagon and GLP-1
Volume: 12 Issue: 2
Author(s): Vishal J. Patel, Amit A. Joharapurkar, Samadhan G. Kshirsagar, Kartikkumar N. Patel, Gaurang B. Shah and Mukul R. Jain
Affiliation:
Keywords: Cardiovascular effect, coagonist, GLP-1, Glucagon and oxyntomodulin.
Abstract: Dual agonism of glucagon and glucagon-like peptide-1 (GLP-1) receptors reduces body weight without inducing hyperglycemia. In addition, coagonists have demonstrated lipid lowering property, which was independent of their anorectic effect. Similarly, GLP-1 modulates cardiovascular function which is favorable for treatment of myocardial injury, cardiac dysfunction, cardiac arrhythmias, endothelial dysfunction, and blood pressure, while glucagon has a positive impact on heart rate, cardiac output, ventricular contraction and enhances cardiac performance in animals and humans. Hence, researchers focused on combining these attributes of GLP-1 and glucagon in a single molecule, which was termed as a coagonist. Oxyntomodulin is the naturally occurring coagonist of GLP-1 and glucagon. This review focusses on the coagonists under clinical development discussing activities affecting cardiovascular functions, lipid modulation, direct effect on cardiac functions or other related functions. A comparative analysis of the in vitro and in vivo properties of GLP-1, glucagon and the coagonists is also carried out. This review discusses potential of GLP-1 and glucagon coagonists in treatment of cardiovascular and hemodynamic diseases with attention to GLP-1 or glucagon receptor specific properties as well as the interaction between other therapies.
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Cite this article as:
Patel J. Vishal, Joharapurkar A. Amit, Kshirsagar G. Samadhan, Patel N. Kartikkumar, Shah B. Gaurang and Jain R. Mukul, Therapeutic Potential of Coagonists of Glucagon and GLP-1, Cardiovascular & Hematological Agents in Medicinal Chemistry 2014; 12 (2) . https://dx.doi.org/10.2174/1871525712666141019194025
DOI https://dx.doi.org/10.2174/1871525712666141019194025 |
Print ISSN 1871-5257 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6182 |
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