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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
1
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pubmed:dateCreated |
2010-12-24
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pubmed:abstractText |
This letter describes the structure-activity relationship (SAR) of the 'right-wing' ?-amino acid residue of potent tetrahydroisoquinoline (THIQ)-derived LFA-1/ICAM-1 antagonists. Novel (S)-substituted heteroaryl-bearing ?-amino acids have been identified as replacements of the 'right-wing' (S)-2,3-diaminopropanoic acid (DAP) moiety. Improvement of potency in the Hut-78 assay in the presence of 10% human serum has also been achieved.
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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 |
Jan
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:ArkinMichelle RMR,
pubmed-author:BarrKenneth JKJ,
pubmed-author:BuiMinnaM,
pubmed-author:EvanchikMarc JMJ,
pubmed-author:FlanaganW MikeWM,
pubmed-author:HageJ SJS,
pubmed-author:HananEmily JEJ,
pubmed-author:HydeJenniferJ,
pubmed-author:MartellJose RJR,
pubmed-author:OslobJohan DJD,
pubmed-author:PaulvannanKumarK,
pubmed-author:PrabhuSailetaS,
pubmed-author:ShenWangW,
pubmed-author:SilvermanJeffrey AJA,
pubmed-author:WrightJasminJ,
pubmed-author:YuChul HCH,
pubmed-author:ZhongMinM,
pubmed-author:ZhuJiangJ
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pubmed:copyrightInfo |
Copyright © 2010 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
21
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
307-10
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pubmed:meshHeading |
pubmed-meshheading:21109434-Amino Acids,
pubmed-meshheading:21109434-Animals,
pubmed-meshheading:21109434-Intercellular Adhesion Molecule-1,
pubmed-meshheading:21109434-Lymphocyte Function-Associated Antigen-1,
pubmed-meshheading:21109434-Male,
pubmed-meshheading:21109434-Rats,
pubmed-meshheading:21109434-Rats, Sprague-Dawley,
pubmed-meshheading:21109434-Structure-Activity Relationship,
pubmed-meshheading:21109434-Tetrahydroisoquinolines,
pubmed-meshheading:21109434-beta-Alanine
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pubmed:year |
2011
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pubmed:articleTitle |
Structure-activity relationship (SAR) of the ?-amino acid residue of potent tetrahydroisoquinoline (THIQ)-derived LFA-1/ICAM-1 antagonists.
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pubmed:affiliation |
Sunesis Pharmaceuticals, Inc, 395 Oyster Point Blvd, Suite 400, South San Francisco, CA 94080, USA. mzhong@presidiopharma.com
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pubmed:publicationType |
Journal Article
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