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.
Highlights
Despite of significant progress of pharmacotherapy in last decades of the 20th century, heart failure remains a leading cause of death worldwide [1]
The quality of life and the life span are extended by the use of drugs that modify the function of the renin-angiotensin-aldosterone system, diuretics and beta adrenergic receptor blockers
Studies were excluded based on the following criteria: studies not mentioning G protein kinase 2 inhibitor in the abstract; studies without comparison groups; abstracts presented at conferences, editorials, commentaries, and studies without complete data; cohort studies and case-control studies were excluded
Summary
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. A new drug candidate, an inhibitor of G-protein-coupled receptor kinase 2 (βARKct) that prevents βAR down-regulation and desensitization, is being developed.
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