Document Detail


Regulation of G protein-coupled receptor kinases by phospholipids.
MedLine Citation:
PMID:  23151001     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
G protein coupled-receptor (GPCR) kinases (GRKs) initiate the deactivation of GPCRs by phosphorylating their cytoplasmic loops and C-terminal tails. They are regulated not only by allosteric interactions with activated GPCRs, but also by the membrane environment itself. Herein we describe how the various GRKs are recruited to lipid bilayers and, where evident, how specific anionic phospholipids help regulate their activity. Using crystal structures representing each of the three vertebrate GRK subfamilies, we map the lipid binding sites in order to better understand how these enzymes are oriented at the cell surface. This analysis suggests that GRKs bind lipid and active GPCRs in a coordinated manner.
Authors:
K T Homan; A Glukhova; J J G Tesmer
Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't; Review    
Journal Detail:
Title:  Current medicinal chemistry     Volume:  20     ISSN:  1875-533X     ISO Abbreviation:  Curr. Med. Chem.     Publication Date:  2013  
Date Detail:
Created Date:  2013-01-17     Completed Date:  2013-05-06     Revised Date:  2013-09-27    
Medline Journal Info:
Nlm Unique ID:  9440157     Medline TA:  Curr Med Chem     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  39-46     Citation Subset:  IM    
Affiliation:
Life Sciences Institute and the Department of Pharmacology, University of Michigan, Ann Arbor, Michigan 48109, USA.
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MeSH Terms
Descriptor/Qualifier:
Amino Acid Sequence
Animals
Binding Sites
G-Protein-Coupled Receptor Kinases / chemistry*,  metabolism*
Humans
Lipid Bilayers / metabolism*
Models, Molecular
Molecular Sequence Data
Phospholipids / metabolism*
Protein Structure, Tertiary
Receptors, G-Protein-Coupled / metabolism
Grant Support
ID/Acronym/Agency:
GM081655/GM/NIGMS NIH HHS; HL071818/HL/NHLBI NIH HHS; HL086865/HL/NHLBI NIH HHS; R01 GM081655/GM/NIGMS NIH HHS; R01 HL071818/HL/NHLBI NIH HHS; R01 HL086865/HL/NHLBI NIH HHS
Chemical
Reg. No./Substance:
0/Lipid Bilayers; 0/Phospholipids; 0/Receptors, G-Protein-Coupled; EC 2.7.11.16/G-Protein-Coupled Receptor Kinases

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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