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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
3
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pubmed:dateCreated |
2007-1-22
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pubmed:abstractText |
VLA-4 is implicated in several inflammatory and autoimmune disease states. A series of cyclic beta-amino acids (beta-aa) was studied as VLA-4 antagonists. Binding affinity was highly dependent on the dihedral angle (phi) between the amino and the carboxyl termini of the beta-aa. Compound 5 m where the beta-aa is embedded in a bicycle possesses the most preferred phi (120 degrees). It is a potent and bioavailable VLA-4 antagonist (VCAM-Ig alpha4beta1 IC50 = 54 nM, rat po F = 49%).
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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 |
Feb
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pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:ChangLinda LLL,
pubmed-author:DossGeorge AGA,
pubmed-author:ForrestGailG,
pubmed-author:HagmannWilliam KWK,
pubmed-author:LyonsKathrynK,
pubmed-author:MacCossMalcolmM,
pubmed-author:McCauleyErmengildaE,
pubmed-author:MumfordRichardR,
pubmed-author:SchmidtJohn AJA,
pubmed-author:TruongQuangQ,
pubmed-author:VincentStellaS
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pubmed:issnType |
Print
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pubmed:day |
1
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pubmed:volume |
17
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
597-601
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pubmed:meshHeading |
pubmed-meshheading:17118652-Bicyclo Compounds,
pubmed-meshheading:17118652-Biological Availability,
pubmed-meshheading:17118652-Half-Life,
pubmed-meshheading:17118652-Humans,
pubmed-meshheading:17118652-Indicators and Reagents,
pubmed-meshheading:17118652-Integrin alpha4beta1,
pubmed-meshheading:17118652-Integrins,
pubmed-meshheading:17118652-Jurkat Cells,
pubmed-meshheading:17118652-Magnetic Resonance Spectroscopy,
pubmed-meshheading:17118652-Molecular Conformation,
pubmed-meshheading:17118652-Stereoisomerism,
pubmed-meshheading:17118652-Structure-Activity Relationship,
pubmed-meshheading:17118652-Vascular Cell Adhesion Molecule-1
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pubmed:year |
2007
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pubmed:articleTitle |
Highly constrained bicyclic VLA-4 antagonists.
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pubmed:affiliation |
Department of Medicinal Chemical Research, Merck Research Laboratories, Rahway, NJ 07065, USA.
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pubmed:publicationType |
Journal Article
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