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Acta Physiol (Oxf). 2014 May;211(1):20-35. doi: 10.1111/apha.12281. Epub 2014 Apr 4.

Therapeutic implications of peptide interactions with G-protein-coupled receptors in diabetic vasculopathy.

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Department of Physiology, Georgia Regents University, Augusta, GA, USA.


The dramatic worldwide increase in the prevalence of diabetes has generated an attempt by the scientific community to identify strategies for its treatment and prevention. Vascular dysfunction is a hallmark of diabetes and frequently leads to the development of atherosclerosis, coronary disease-derived myocardial infarction, stroke, peripheral arterial disease and diabetic 'triopathy' (retinopathy, nephropathy and neuropathy). These vascular complications, developing in an increasingly younger cohort of patients with diabetes, contribute to morbidity and mortality. Despite the development of new anti-diabetic or anti-hyperglycaemic drugs, vascular complications remain to be a problem. This warrants a need for new therapeutic strategies to tackle diabetic vasculopathy. There is a growing body of evidence showing that peptide-binding G-protein-coupled receptors (peptide-binding GPCRs) play an important role in the pathophysiology of vascular dysfunction during diabetes. Thus, in this review, we discuss some of the peptide-binding GPCRs involved in the regulation of vascular function that have potential to be a therapeutic target in the treatment of diabetic vasculopathy.


diabetic vascular complications; endothelial cells; peptide ligand; vascular smooth muscle cells; vasoconstriction; vasodilatation

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