Linked Life Data

20044245

Source:http://linkedlifedata.com/resource/pubmed/id/20044245

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
7
pubmed:dateCreated
2010-2-17
pubmed:abstractText
G protein-coupled receptors (GPCRs) form a superfamily of cell surface receptors that play fundamental roles in physiology and pathophysiology. Although GPCRs have been the most successful targets for drug discovery, there still remain many orphan GPCRs, which provides opportunities for development of novel drugs. Here, we introduce a new method for evaluation of GPCR activation utilizing a surface plasmon resonance (SPR) sensor. Cells expressing GPCRs were cultured directly on an SPR sensor chip and stimulated with GPCR ligands, resulting in SPR responses that were dependent on the type of G alpha subunits coupling with receptors. Namely G(i)- and/or G(12/13)-coupled receptors evoked SPR responses but G(s)- or G(q)-coupled ones did not. Analyses on the intracellular signal pathways revealed that small G protein Rho/Rac-mediated actin rearrangement plays an important role in the signal transduction pathways leading to the SPR responses. An SPR response was also evoked by insulin-like growth factor-1, which stimulates Rac-dependent stress fiber formation via its receptor-tyrosine kinase. Thus, this method provides a unique opportunity for real-time monitoring of cellular responses involved in cytoskeletal rearrangements, and may be useful in ligand/drug discovery for certain types of receptor, such as G(i)- and G(12/13)-coupled receptors.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Mar
pubmed:issn
1873-4235
pubmed:author
pubmed:copyrightInfo
(c) 2009 Elsevier B.V. All rights reserved.
pubmed:issnType
Electronic
pubmed:day
15
pubmed:volume
25
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
1675-80
pubmed:meshHeading
pubmed:year
2010
pubmed:articleTitle
Detection of G protein-coupled receptor-mediated cellular response involved in cytoskeletal rearrangement using surface plasmon resonance.
pubmed:affiliation
Department of Biochemistry, Gunma University Graduate School of Medicine, 3-39-22 Showa-machi, Maebashi, Gunma 371-8511, Japan. chenkexi@health.gunma-u.ac.jp
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't