Noncanonical Roles of G Protein-coupled Receptor Kinases in Cardiovascular Signaling
Year: 2017
Type: review
Abstract: G protein-coupled receptor kinases (GRKs) are classically known for their role in regulating the activity of the largest known class of membrane receptors, which influence diverse biological processes in every cell type in the human body. As researchers have tried to uncover how this family of kinases, containing only 7 members, achieves selective and coordinated control of receptors, they have uncovered a growing number of noncanonical activities for these kinases. These activities include phosphorylation of nonreceptor targets and kinase-independent molecular interactions. In particular, GRK2, GRK3, and GRK5 are the predominant members expressed in the heart. Their canonical and noncanonical actions within cardiac and other tissues have significant implications for cardiovascular function in healthy animals and for the development and progression of disease. This review summarizes what is currently known regarding the activity of these kinases, and particularly the role of GRK2 and GRK5 in the molecular alterations that occur during heart failure. This review further highlights areas of GRK regulation that remain poorly understood and how they may represent novel targets for therapeutic development.
Authors: Sarah M. Schumacher, Walter J. Koch
Institution: Temple University
Language: English
Subfield: Molecular Biology
Domain: Life Sciences
Open Access status: green
Awards: Novel Mechanisms of Cardiac Injury and Repair, Targeting GRK2 in the Heart, Unique Domain Features of GRK2 and Roles in Cardiovascular Disease, Targeting GRK2 (BARK1) in Heart Failure, Improving Cardiac Function After Myocardial Infarction, GRK and b-Arrestin Signaling in Cardiac Regeneration, Novel Mechanisms and Therapies in Heart Failure, Structure, function, and inhibition of G protein-coupled receptor kinases
OpenAlex ID: W2599997917