International Union of Basic and Clinical Pharmacology. LXXXVIII. G Protein-Coupled Receptor List: Recommendations for New Pairings with Cognate Ligands

Cardiovascular Actions of Incretin-Based Therapies

“…CXCL12 also binds to a second receptor, CXC chemokine receptor type-7; however, the importance, if any, of CXC chemokine receptor type-7 for CXCL12 action in the injured heart remains uncertain. 95 The plasma levels of circulating CXCL12, derived from endothelial cells and cardiomyocytes at the site of ischemic injury, serve as a biomarker of cardiac injury in human subjects with MI. 96 Enhancing CXCL12 activity, by administration of CXCL12, by viral, cellular, or plasmid-mediated overexpression of CXCL12, or through inhibition of DPP-4 activity, resulted in cardioprotective actions in the setting of acute ischemic cardiac injury.…”

FAM19A4 is a novel cytokine ligand of formyl peptide receptor 1 (FPR1) and is able to promote the migration and phagocytosis of macrophages

“…More recently, synthetic low-molecular-weight ligands for FPR1 have emerged from a number of compound library screens. 10 By binding to FPR1, they function as agonists of FPR1 to promote migration, phagocytosis and the release of the superoxide ion from macrophages and neutrophils, 11 resulting in the systemic inflammatory response syndrome. 12 However, these ligands are either from the infecting pathogens or serve as damageassociated molecular patterns, also called alarmins.…”

The adipokine chemerin amplifies electrical field-stimulated contraction in the isolated rat superior mesenteric artery

“…This can occur by secretion of adipokines that directly affect vascular tone, such as the relaxant adiponectin (25). We recently discovered the protein chemerin in PVAT and demonstrated that a shorter chemerin agonist, chemerin-9, caused direct arterial contraction through activation of the best-characterized chemerin receptor, ChemR23 (3,8,27,33,38,48). Chemerin is secreted from the liver and fat depots (10), functioning as an adipokine that regulates adipogenesis (12,31,32) and as an activator of inflammatory cells (13,50,52).…”