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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
10
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pubmed:dateCreated |
2002-5-6
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pubmed:abstractText |
Starting from the tetrapeptide Ac-pYEEI-NHMe and using a structure-based approach, we have designed and synthesised a peptidomimetic ligand for p56(lck) SH2 domain containing a conformationally restricted replacement for the two glutamate residues. We have explored replacments for the isoleucine residue in the pY+3 pocket and thus identified 1-(R)-amino-3-(S)-indaneacetic acid as the most potent replacement. We also report the X-ray crystal structures of two of the antagonists.
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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 |
May
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pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:BannerDavidD,
pubmed-author:BitRino ARA,
pubmed-author:BorkakotiNeeraN,
pubmed-author:CansfieldAndrew DAD,
pubmed-author:HarrisBillB,
pubmed-author:HillChristopher HCH,
pubmed-author:HilyardKatherine LKL,
pubmed-author:HobbsChristopher JCJ,
pubmed-author:KilfordIan RIR,
pubmed-author:KitasEricE,
pubmed-author:KroehnAntoninA,
pubmed-author:LovellPeterP,
pubmed-author:PoleDavidD,
pubmed-author:RugmanPaulP,
pubmed-author:SherborneBrad SBS,
pubmed-author:SmithIan E DIE,
pubmed-author:SurgenorAllanA,
pubmed-author:VeseyDavid RDR,
pubmed-author:WalmsleyD LeeDL,
pubmed-author:WhittakerDavidD,
pubmed-author:WilliamsGlynG,
pubmed-author:WilsonFionaF
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pubmed:issnType |
Print
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pubmed:day |
20
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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 |
1365-9
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
pubmed-meshheading:11992778-Animals,
pubmed-meshheading:11992778-Cricetinae,
pubmed-meshheading:11992778-Crystallography, X-Ray,
pubmed-meshheading:11992778-Drug Design,
pubmed-meshheading:11992778-Enzyme Inhibitors,
pubmed-meshheading:11992778-Glutamic Acid,
pubmed-meshheading:11992778-Ligands,
pubmed-meshheading:11992778-Lymphocyte Specific Protein Tyrosine Kinase p56(lck),
pubmed-meshheading:11992778-Models, Molecular,
pubmed-meshheading:11992778-Molecular Conformation,
pubmed-meshheading:11992778-Oligopeptides,
pubmed-meshheading:11992778-Structure-Activity Relationship,
pubmed-meshheading:11992778-src Homology Domains
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pubmed:year |
2002
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pubmed:articleTitle |
Structure-based design of peptidomimetic antagonists of p56(lck) SH2 domain.
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pubmed:affiliation |
Roche Products Limited, 40 Broadwater Road, Welwyn Garden City, AL7 3AY, Hertfordshire, UK. chobbs@ionixpharma.com
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pubmed:publicationType |
Journal Article
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