Apelin receptor agonists, including G protein-biased peptides, are emerging as promising therapeutic targets for cardiovascular diseases such as pulmonary arterial hypertension.
Apelin receptor agonists, including novel G protein-biased peptides, represent a promising emerging therapeutic class for cardiovascular diseases such as pulmonary arterial hypertension.
]apelin-13 showed additional therapeutic potential, increasing glomerular filtration rate while reducing proteinuria. Identification of these favorable actions in disease has sparked the development of more effective agonists with improved pharmacokinetics and pharmacodynamics profiles. Among these are G protein-biased peptide agonists, designed to minimize receptor desensitization by reducing internalization via the β-arrestin pathway. These have shown efficacy in proof-of-concept studies and in animal models of pulmonary arterial hypertension, one of the most promising therapeutic targets. This review focuses on the clinical pharmacology of the apelin receptor, exploring the pathophysiology of diseases where the apelin signaling pathway is dysregulated that have emerged during the last 5 years. SIGNIFICANCE STATEMENT: This review focuses on the pharmacology of the apelin receptor where structural analysis has generated a molecular map of interaction with endogenous ligands, apelin and Elabela, as well as with peptide and small molecule agonists. Novel unbiased and biased apelin agonists are progressing through the clinic targeting pathophysiological conditions where the apelin signaling pathway is dysregulated.
Davenport et al. (Sat,) conducted a review in Cardiovascular diseases and pulmonary arterial hypertension. Apelin receptor agonists (apelin-13, G protein-biased peptide agonists) was evaluated. Apelin receptor agonists, including G protein-biased peptides, are emerging as promising therapeutic targets for cardiovascular diseases such as pulmonary arterial hypertension.
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