Targeting the RH domain of GRK2: potential therapeutic implications in cardiovascular disease.
AIMS GRK2 is a key regulator of GPCR desensitization through its kinase and RGS homology (RH) domains. Because increased GRK2 activity contribute to cardiovascular diseases, including heart failure, cardiac hypertrophy and hypertension, GRK2 has emerged as an attractive therapeutic target. Most GRK2 inhibitors target i...