Abstract
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.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Adenosine Triphosphate / antagonists & inhibitors
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Adenosine Triphosphate / chemistry
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Oligopeptides / chemical synthesis*
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Oligopeptides / chemistry
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Protein Conformation
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Proto-Oncogene Proteins pp60(c-src) / antagonists & inhibitors
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Proto-Oncogene Proteins pp60(c-src) / chemistry
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Structure-Activity Relationship
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src-Family Kinases / antagonists & inhibitors*
Substances
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Oligopeptides
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Adenosine Triphosphate
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Proto-Oncogene Proteins pp60(c-src)
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src-Family Kinases