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

Authors

Jian Yang, Department of Clinical Nutrition, The Third Affiliated Hospital of Chongqing Medical University, Chongqing, PR China; Research Center for Metabolic and Cardiovascular Diseases, The Third Affiliated Hospital of Chongqing Medical University, Chongqing, China. Electronic address: jianyang@hospital.cqmu.edu.cn.
John E. Hall, Department of Physiology and Biophysics, Mississippi Center for Obesity Research, University of Mississippi Medical Center, Jackson, MS, USA.
Pedro A. Jose, Division of Renal Diseases & Hypertension, The George Washington University School of Medicine & Health Sciences, Washington, DC, USA.
Ken Chen, Department of Cardiology, Daping Hospital, The Third Military Medical University, Chongqing, PR China; Cardiovascular Research Center of Chongqing College, Chinese Academy of Sciences, University of Chinese Academy of Sciences, Chongqing, PR China. Electronic address: chenken@cigit.ac.cn.
Chunyu Zeng, Department of Cardiology, Daping Hospital, The Third Military Medical University, Chongqing, PR China; Heart Center of Fujian Province, Union Hospital, Fujian Medical University, Fuzhou, PR China; Department of Cardiology, Chongqing General Hospital, Chongqing, PR China; Cardiovascular Research Center of Chongqing College, Chinese Academy of Sciences, University of Chinese Academy of Sciences, Chongqing, PR China. Electronic address: zengchunyu@cigit.ac.cn.

Document Type

Journal Article

Publication Date

4-27-2022

Journal

Pharmacology & therapeutics

Volume

239

DOI

10.1016/j.pharmthera.2022.108194

Keywords

Angiotensin II type 1 receptor; Dopamine receptor; G protein-coupled receptor; G protein-coupled receptor kinase type 4; Hypertension

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, and A486V) are associated with salt-sensitive or salt-resistant essential hypertension and blood pressure responses to antihypertensive medicines. In this article, we present a comprehensive overview of GRK-mediated regulation of blood pressure, focusing on the latest research progress on GRK4 and hypertension and highlighting potential and novel strategies for the prevention and treatment of hypertension.

APA Citation

Yang, Jian; Hall, John E.; Jose, Pedro A.; Chen, Ken; and Zeng, Chunyu, "Comprehensive insights in GRK4 and hypertension: From mechanisms to potential therapeutics" (2022). GW Authored Works. Paper 740.
https://hsrc.himmelfarb.gwu.edu/gwhpubs/740

Department

Medicine