Book chapter
Characterization of G protein-coupled receptor kinases
Methods in Enzymology, pp 547-559
01 Jan 2002
PMID: 11665591
Featured in Collection : UN Sustainable Development Goals @ Drexel
Abstract
A basic feature of most cells is the ability to dynamically regulate their responsiveness to extracellular stimuli. Numerous stimuli transmit their signals via interaction with cell surface G protein-coupled receptors (GPCRs). GPCRs are subject to three principal modes of regulation: (1) desensitization, the process by which a receptor becomes refractory to continued stimuli, (2) internalization, whereby receptors are physically removed from the cell surface by endocytosis, and (3) downregulation, where total cellular receptor levels are decreased. This chapter describes some of the current methodologies for analyzing endogenous and expressed GPCR kinases (GRKs) in mammalian cells and strategies for in vitro analysis of GRK phosphorylation of GPCRs. GPCR desensitization is primarily mediated by second messenger responsive kinases—such as protein kinase A (PKA) and protein kinase C (PKC)—and by GRKs. GRKs specifically phosphorylate agonist-occupied GPCRs and initiate the recruitment of additional proteins, termed “arrestins,” which further receptor desensitization and internalization. The seven mammalian GRKs identified can be divided into three subfamilies based on their overall structural organization and homology: (1) GRKl (rhodopsin kinase) and GRK7, (2) GRK2 and GRK3, and (3) GRK4, GRKS, and GRKG.
Metrics
Details
- Title
- Characterization of G protein-coupled receptor kinases
- Creators
- Alexey N. ProninRobert P. LoudonJeffrey L. Benovic
- Publication Details
- Methods in Enzymology, pp 547-559
- Publisher
- Elsevier Science & Technology
- Resource Type
- Book chapter
- Language
- English
- Academic Unit
- Biology
- Web of Science ID
- WOS:000171866900034
- Scopus ID
- 2-s2.0-0034797829
- Other Identifier
- 991020950673004721
UN Sustainable Development Goals (SDGs)
This publication has contributed to the advancement of the following goals:
InCites Highlights
Data related to this publication, from InCites Benchmarking & Analytics tool:
- Collaboration types
- Domestic collaboration
- Web of Science research areas
- Biochemical Research Methods
- Biochemistry & Molecular Biology