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Comprehensive insights in GRK4 and hypertension: From mechanisms to potential therapeutics.


ABSTRACT: G protein-coupled receptors (GPCRs) mediate cellular responses to diverse extracellular stimuli that play vital roles in the regulation of biology, including behavior. Abnormal G protein-coupled receptor kinase (GRK)-mediated regulation of GPCR function is involved in the pathogenesis of hypertension. Among the seven GRK subtypes, GRK4 has attracted attention because of its constitutive activity and tissue-specific expression. Increasing number of studies show that GRK4 affects blood pressure by GPCR-mediated regulation of renal and arterial function. The target receptor of GRK4 is confined not only to GPCRs, but also to other blood pressure-regulating receptors, such as the adiponectin receptor. Genetic studies in humans show that in several ethnic groups, GRK4 gene variants (R65L, A142V,

SUBMITTER: Yang J 

PROVIDER: S-EPMC9728143 | biostudies-literature | 2022 Nov

REPOSITORIES: biostudies-literature