G Protein-Coupled Receptor Kinase 2 (GRK2) as a Potential Therapeutic Target in Cardiovascular and Metabolic Diseases

Frontiers in Pharmacology

Mercedes Salaices⁴  Ana M. Briones⁴  Marta Cruces-Sande⁵  Cristina Murga⁵  Federico Mayor Jr.⁵  Alba C. Arcones⁵ 

[1] CIBER de Enfermedades Cardiovasculares (CIBERCV), Instituto de Salud Carlos III, Madrid, Spain;Departamento de Biología Molecular, Centro de Biología Molecular Severo Ochoa (UAM-CSIC), Universidad Autónoma de Madrid, Madrid, Spain;Departamento de Farmacología, Universidad Autónoma de Madrid (UAM), Madrid, Spain;Instituto de Investigación Hospital Universitario La Paz (IdiPAZ), Madrid, Spain;Instituto de Investigación Sanitaria La Princesa, Madrid, Spain;

关键词: GRK2;    GPCR;    cardiovascular;    obesity;    NAFLD;    insulin resistance;   

DOI  :  10.3389/fphar.2019.00112

来源: DOAJ

【 摘 要 】

G protein-coupled receptor kinase 2 (GRK2) is a central signaling node involved in the modulation of many G protein-coupled receptors (GPCRs) and also displaying regulatory functions in other cell signaling routes. GRK2 levels and activity have been reported to be enhanced in patients or in preclinical models of several relevant pathological situations, such as heart failure, cardiac hypertrophy, hypertension, obesity and insulin resistance conditions, or non-alcoholic fatty liver disease (NAFLD), and to contribute to disease progression by a variety of mechanisms related to its multifunctional roles. Therefore, targeting GRK2 by different strategies emerges as a potentially relevant approach to treat cardiovascular disease, obesity, type 2 diabetes, or NAFLD, pathological conditions which are frequently interconnected and present as co-morbidities.

【 授权许可】

Unknown