Apelin, Elabela/Toddler, and biased agonists as novel therapeutic agents in the cardiovascular system

摘要: Apelin and its G protein-coupled receptor (GPCR) have emerged as a key signalling pathway in the cardiovascular system. The peptide is potent inotropic agent vasodilator. Remarkably, peptide, Elabela/Toddler, that has little sequence similarity to apelin, been proposed second endogenous apelin ligand encoded by gene from region of genome previously classified ‘non-coding’. downregulated pulmonary arterial hypertension heart failure. To replace missing ‘biased’ agonists designed preferentially activate protein pathways, resulting reduced β-arrestin recruitment internalisation, with additional benefit attenuating detrimental signalling. Proof-of-concept studies support clinical potential for biased agonists.