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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
14
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pubmed:dateCreated |
2006-6-5
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pubmed:abstractText |
A series of 3-arylpropionic acids were synthesized as S1P1 receptor agonists. Structure-activity relationship studies on the pendant phenyl ring revealed several structural features offering selectivity of S1P1 binding against S1P2-5. These highly selective S1P1 agonists induced peripheral blood lymphocyte lowering in mice and one of them was found to be efficacious in a rat skin transplantation model, supporting that S1P1 agonism is primarily responsible for the immunosuppressive efficacy observed in preclinical animal models.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Jul
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pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:BergstromJamesJ,
pubmed-author:CardDeborahD,
pubmed-author:ChrebetGaryG,
pubmed-author:DohertyGeorgeG,
pubmed-author:HajduRichardR,
pubmed-author:HaleJeffrey JJJ,
pubmed-author:JkoE SES,
pubmed-author:KeohaneCarol ACA,
pubmed-author:MandalaSuzanne MSM,
pubmed-author:MilliganJames AJA,
pubmed-author:MillsSander GSG,
pubmed-author:OrrV BVB,
pubmed-author:QuackenbushElizabethE,
pubmed-author:RosenbachMark JMJ,
pubmed-author:SheiGan-JuGJ,
pubmed-author:TothLesileL,
pubmed-author:WickhamAlexandraA
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pubmed:issnType |
Print
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pubmed:day |
15
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pubmed:volume |
16
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3679-83
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pubmed:meshHeading |
pubmed-meshheading:16697189-Animals,
pubmed-meshheading:16697189-CHO Cells,
pubmed-meshheading:16697189-Cricetinae,
pubmed-meshheading:16697189-Immunosuppressive Agents,
pubmed-meshheading:16697189-Ligands,
pubmed-meshheading:16697189-Lymphocyte Count,
pubmed-meshheading:16697189-Mice,
pubmed-meshheading:16697189-Phenylpropionates,
pubmed-meshheading:16697189-Rats,
pubmed-meshheading:16697189-Receptors, Lysosphingolipid,
pubmed-meshheading:16697189-Skin Transplantation,
pubmed-meshheading:16697189-Structure-Activity Relationship
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pubmed:year |
2006
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pubmed:articleTitle |
Discovery of 3-arylpropionic acids as potent agonists of sphingosine-1-phosphate receptor-1 (S1P1) with high selectivity against all other known S1P receptor subtypes.
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pubmed:affiliation |
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. lin_yan@merck.com
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pubmed:publicationType |
Journal Article
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