G protein receptor kinase type 2: A novel target in cardiovascular drug development

Abstract

In spite of significant advancement in pharmacotherapy, heart failure remains one of the main causes of death worldwide. The existing treatment of heart failure prolongs life span by slowing down the pathological process but does not induce heart healing. The β adrenergic receptor dysfunction is a hallmark abnormality of advanced stages of heart failure, and increased expression of G-protein-coupled receptor kinase 2 (GRK-2) involved in down regulation of β adrenergic receptors, occurs in early stages of heart failure. Thus a new drug candidate, an inhibitor of G-protein-coupled receptor kinase 2 (βARKct) that prevents βAR down-regulation and desensitization, is being developed. Experimental data are encouraging.

Keywords

• heart failure
• β adrenergic receptor
• G protein kinase 2 inhibitor