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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
12
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pubmed:dateCreated |
1992-7-30
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pubmed:abstractText |
Different hypotheses of the structure of platelet-activating factor (PAF) receptor based on structure-activity relationships of agonists and antagonists are reviewed. For an agonistic effect, strong hydrophobic interactions and an ether function are required in position-1 of the glycerol backbone; chain length limitations and steric hindrance demand a small group in position-2. The unusual structural properties of non-PAF-like antagonists required 3-D electrostatic potential calculations. This method applied to seven potent antagonists suggests a strong "Cache-orielles" (ear-muff) effect, i.e., two strong electronegative wells (isocontour at -10 Kcal/mole) are located at 180 degrees to each other and at a relatively constant distance. Initial consideration of the "Cache-oreilles" effect implied the structure of a bipolarized cylinder of 10-12 A diameter for the receptor. However, very recent results on studies with agonists and antagonists structurally similar to PAF suggest that the receptor may in fact be a multi-polarized cylinder.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Platelet Activating Factor,
http://linkedlifedata.com/resource/pubmed/chemical/Platelet Membrane Glycoproteins,
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/platelet activating factor receptor
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pubmed:status |
MEDLINE
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pubmed:month |
Dec
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pubmed:issn |
0024-4201
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
26
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pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
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pubmed:pagination |
1162-6
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:1668112-Models, Molecular,
pubmed-meshheading:1668112-Molecular Conformation,
pubmed-meshheading:1668112-Platelet Activating Factor,
pubmed-meshheading:1668112-Platelet Membrane Glycoproteins,
pubmed-meshheading:1668112-Protein Conformation,
pubmed-meshheading:1668112-Receptors, Cell Surface,
pubmed-meshheading:1668112-Receptors, G-Protein-Coupled,
pubmed-meshheading:1668112-Structure-Activity Relationship
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pubmed:year |
1991
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pubmed:articleTitle |
PAF receptor structure: a hypothesis.
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pubmed:affiliation |
Laboratoire de Pharmacochimie Moléculaire, Université Paris 7, France.
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pubmed:publicationType |
Journal Article,
Comparative Study,
Review
|