Regulation of G protein-coupled receptor kinases.
Publication/Presentation Date
2-1-2000
Abstract
G protein-coupled receptor kinases (GRKs) specifically interact with the agonist-activated form of G protein-coupled receptors (GPCRs) to effect receptor phosphorylation and desensitization. Recent studies demonstrate that GRK function is a highly regulated process, and it is perhaps in this manner that a handful of GRKs (7 have been identified to date) are able to regulate the responsiveness of numerous GPCRs in a given cell type in a coordinated manner. The mechanisms by which GRK activity is regulated can be divided into 3 categories: 1) subcellular localization; 2) alterations in intrinsic kinase activity; and 3) alterations in GRK expression levels. This review will summarize our current understanding of each of these regulatory processes, and offer explanations as to how such mechanisms influence GPCR regulation under various physiologic conditions.
Volume
10
Issue
2
First Page
81
Last Page
89
ISSN
1050-1738
Published In/Presented At
Penn, R. B., Pronin, A. N., & Benovic, J. L. (2000). Regulation of G protein-coupled receptor kinases. Trends in cardiovascular medicine, 10(2), 81–89. https://doi.org/10.1016/s1050-1738(00)00053-0
Disciplines
Business Administration, Management, and Operations | Health and Medical Administration | Management Sciences and Quantitative Methods
PubMedID
11150735
Department(s)
Administration and Leadership
Document Type
Article