Proteinase-activated receptor 2 (PAR2) is a cell surface receptor activated by serine proteinases or specific synthetic compounds.\nInterest in PAR2 as a pharmaceutical target for various diseases is increasing. Here we asked two questions relevant to endothelial\ndysfunction and diabetes: How is PAR2 function affected in blood vessels? What role does PAR2 have in promoting obesity,\ndiabetes, and/or metabolic syndrome, specifically via the endothelium and adipose tissues? We conducted a systematic review of\nthe published literature in PubMed and Scopus (July 2015; search terms: par2, par-2, f2lr1, adipose, obesity, diabetes, and metabolic\nsyndrome). Seven studies focused on PAR2 and vascular function. The obesity, diabetes, or metabolic syndrome animal models\ndiffered amongst studies, but each reported that PAR2-mediated vasodilator actions were preserved in the face of endothelial\ndysfunction. The remaining studies focused on non vascular functions and provided evidence supporting the concept that PAR2\nactivation promoted obesity. Key studies showed that PAR2 activation regulated cellular metabolism, and PAR2 antagonists\ninhibited adipose gain and metabolic dysfunction in rats.We conclude that PAR2 antagonists for treatment of obesity indeed show\nearly promise as a therapeutic strategy; however, endothelial-specific PAR2 functions, which may offset mechanisms that produce\nvascular dysfunction in diabetes, warrant additional study.
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