Trends in pharmacological sciences
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Trends Pharmacol. Sci. · Sep 2015
ReviewApelin, Elabela/Toddler, and biased agonists as novel therapeutic agents in the cardiovascular system.
Apelin and its G protein-coupled receptor (GPCR) have emerged as a key signalling pathway in the cardiovascular system. The peptide is a potent inotropic agent and vasodilator. ⋯ To replace the missing endogenous peptide, 'biased' apelin agonists have been designed that preferentially activate G protein pathways, resulting in reduced β-arrestin recruitment and receptor internalisation, with the additional benefit of attenuating detrimental β-arrestin signalling. Proof-of-concept studies support the clinical potential for apelin receptor biased agonists.