**Abstract**

G protein-coupled receptor kinases (GRKs), the negative regulators of G proteincoupled receptors (GPCRs), have a key role in cardiovascular disease pathophysiology. Alteration in GRKs' expressions and/or kinase activity has been reported in preclinical animal models as well as in patients with cardiovascular diseases. This alteration might be a contributing factor to disease progression by a variety of mechanisms such as noncanonical transduction pathways. The current chapter is aimed to expand our knowledge and understanding of the function of GRKs in cardiovascular diseases, highlight their involvement, and illustrate the possible mechanistic role of GRKs in hypertensive vascular diseases and cardiac myopathy. The current chapter also is endeavoured to identify the potential molecular mechanisms by which GRKs participate in cardiovascular disease progression. Building the basics knowledge about GRKs in cardiovascular diseases will help to assess the potential utilization of GRKs as therapeutic targets and to examine the possible approaches to modulate their protein expression or to inhibit their kinase activity to prevent or attenuate cardiovascular disease progression.

**Keywords:** GRK2, GRK5, GPCR regulation, cardiovascular diseases, heart failure, hypertension, myocardial infarction
