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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
4
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pubmed:dateCreated |
2002-3-7
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pubmed:abstractText |
Acylated beta-amino acids are described as potent, specific and orally bioavailable antagonists of VLA-4. The initial lead was identified from a combinatorial library. Subsequent optimization using a traditional medicinal chemistry approach led to significant improvement in potency (up to 8-fold) while maintaining good pharmacokinetic properties.
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pubmed:commentsCorrections |
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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:CollettiAdriaA,
pubmed-author:DurettePhilippe LPL,
pubmed-author:EggerLinda ALA,
pubmed-author:Fenyk-MelodyJudyJ,
pubmed-author:HagmannWilliam KWK,
pubmed-author:KameneckaTheodoreT,
pubmed-author:KidambiUshaU,
pubmed-author:KopkaIhor EIE,
pubmed-author:LanzaThomasTJr,
pubmed-author:LinLinus SLS,
pubmed-author:LyonsKathrynK,
pubmed-author:MacCossMalcolmM,
pubmed-author:MagriotisPlato APA,
pubmed-author:McCauleyErmenegildaE,
pubmed-author:MumfordRichard ARA,
pubmed-author:RiperGail VanGV,
pubmed-author:SchmidtJohn AJA,
pubmed-author:StearnsRalphR,
pubmed-author:TefferaYohannesY,
pubmed-author:TongXinchunX,
pubmed-author:VincentStellaS,
pubmed-author:YoungDavid NDN,
pubmed-author:de LaszloStephen ESE
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pubmed:issnType |
Print
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pubmed:day |
25
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pubmed:volume |
12
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
611-4
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pubmed:dateRevised |
2004-7-15
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pubmed:meshHeading |
pubmed-meshheading:11844683-Acylation,
pubmed-meshheading:11844683-Administration, Oral,
pubmed-meshheading:11844683-Amino Acids,
pubmed-meshheading:11844683-Animals,
pubmed-meshheading:11844683-Biological Availability,
pubmed-meshheading:11844683-Combinatorial Chemistry Techniques,
pubmed-meshheading:11844683-Drug Evaluation, Preclinical,
pubmed-meshheading:11844683-Inflammation Mediators,
pubmed-meshheading:11844683-Integrin alpha4beta1,
pubmed-meshheading:11844683-Metabolic Clearance Rate,
pubmed-meshheading:11844683-Protein Binding,
pubmed-meshheading:11844683-Rats,
pubmed-meshheading:11844683-Rats, Sprague-Dawley,
pubmed-meshheading:11844683-Stereoisomerism,
pubmed-meshheading:11844683-Structure-Activity Relationship
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pubmed:year |
2002
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pubmed:articleTitle |
The discovery of acylated beta-amino acids as potent and orally bioavailable VLA-4 antagonists.
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pubmed:affiliation |
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. linus_lin@merck.com
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pubmed:publicationType |
Journal Article
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