Source:http://linkedlifedata.com/resource/pubmed/id/12069842
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
1-3
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pubmed:dateCreated |
2002-6-18
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pubmed:abstractText |
Recent characterization of lysophosphatidic acid (LPA) receptors has made possible studies elucidating the structure-activity relationships (SAR) for agonist activity at individual receptors. Additionally, the availability of these receptors has allowed the identification of antagonists of LPA-induced effects. Two receptor-subtype selective LPA receptor antagonists, one selective for the LPA1/EDG2 receptor (a benzyl-4-oxybenzyl N-acyl ethanolamide phosphate, NAEPA, derivative) and the other selective for the LPA3/EDG7 receptor (diacylglycerol pyrophosphate, DGPP, 8:0), have recently been reported. The receptor SAR for both agonists and antagonists are reviewed, and the molecular basis for the difference between agonism and antagonism as well as for receptor-subtype antagonist selectivity identified by molecular modeling is described. The implications of the newly available receptor-subtype selective antagonists are also discussed.
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pubmed:grant | |
pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Ligands,
http://linkedlifedata.com/resource/pubmed/chemical/Phospholipids,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Cell Surface,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, G-Protein-Coupled,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Lysophosphatidic Acid
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pubmed:status |
MEDLINE
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pubmed:month |
May
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pubmed:issn |
0006-3002
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
23
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pubmed:volume |
1582
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
309-17
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pubmed:dateRevised |
2007-11-14
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pubmed:meshHeading |
pubmed-meshheading:12069842-Amino Acid Sequence,
pubmed-meshheading:12069842-Animals,
pubmed-meshheading:12069842-Binding Sites,
pubmed-meshheading:12069842-Humans,
pubmed-meshheading:12069842-Ligands,
pubmed-meshheading:12069842-Models, Molecular,
pubmed-meshheading:12069842-Molecular Sequence Data,
pubmed-meshheading:12069842-Phospholipids,
pubmed-meshheading:12069842-Protein Conformation,
pubmed-meshheading:12069842-Receptors, Cell Surface,
pubmed-meshheading:12069842-Receptors, G-Protein-Coupled,
pubmed-meshheading:12069842-Receptors, Lysophosphatidic Acid,
pubmed-meshheading:12069842-Sequence Alignment,
pubmed-meshheading:12069842-Sequence Homology, Amino Acid
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pubmed:year |
2002
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pubmed:articleTitle |
Molecular basis for lysophosphatidic acid receptor antagonist selectivity.
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pubmed:affiliation |
Department of Chemistry and Computational Research on Materials Institute, The University of Memphis, Memphis, TN 38152-6060, USA.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.,
Research Support, U.S. Gov't, Non-P.H.S.,
Review,
Research Support, Non-U.S. Gov't
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