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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
11
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pubmed:dateCreated |
2006-5-25
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pubmed:abstractText |
A series of peptide analogues of Ac-CIYKYY (1) were synthesized by functional group modifications in peptide side chains or by introducing conformational constraints, to improve the inhibitory potency against active Src kinase. Ac-CIYKF(4-NO2)Y (2, IC50 = 0.53 microM) and conformationally constrained peptide 31 (IC50 = 0.28 microM) exhibited 750- and 1400-fold higher inhibitory activities, respectively, versus that of 1 (IC50 = 400 microM). Compound 2 exhibited a partial competitive inhibition pattern against ATP.
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pubmed:grant |
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pubmed:commentsCorrections |
http://linkedlifedata.com/resource/pubmed/commentcorrection/16722659-10218099,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16722659-10495352,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16722659-10637290,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16722659-10966463,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16722659-14632929,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16722659-14759738,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16722659-15163193,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16722659-15170449,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16722659-15498652,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16722659-7558590,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16722659-9024658,
http://linkedlifedata.com/resource/pubmed/commentcorrection/16722659-9632358
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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 |
Jun
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pubmed:issn |
0022-2623
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
1
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pubmed:volume |
49
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3395-401
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
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pubmed:year |
2006
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pubmed:articleTitle |
Synthesis and structure-activity relationships of linear and conformationally constrained peptide analogues of CIYKYY as Src tyrosine kinase inhibitors.
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pubmed:affiliation |
Department of Biomedical and Pharmaceutical Sciences, University of Rhode Island, Kingston, Rhode Island 02881, USA.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't,
Research Support, N.I.H., Extramural
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