Abstract
New fumagillin analogues were designed through structure-based molecular modeling with a human methionine aminopeptidase-2. Among the fumagillin analogues, cinnamic acid ester derivative CKD-731 showed 1000-fold more potent proliferation inhibitory activity on endothelial cell than TNP-470.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Amino Acid Sequence
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Aminopeptidases / chemistry*
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Angiogenesis Inhibitors / chemical synthesis*
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Angiogenesis Inhibitors / chemistry
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Angiogenesis Inhibitors / pharmacology*
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Animals
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Cattle
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Cell Line
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Cinnamates / chemical synthesis
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Cinnamates / pharmacology
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Cyclohexanes
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Drug Design
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Epoxy Compounds / chemical synthesis
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Epoxy Compounds / pharmacology
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Fatty Acids, Unsaturated / chemical synthesis*
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Fatty Acids, Unsaturated / pharmacology*
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Growth Inhibitors / pharmacology
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Humans
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Leukemia P388 / pathology
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Metalloendopeptidases / chemistry*
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Mice
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Models, Molecular
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Molecular Sequence Data
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Sequence Homology, Amino Acid
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Sesquiterpenes
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Structure-Activity Relationship
Substances
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Angiogenesis Inhibitors
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Cinnamates
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Cyclohexanes
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Epoxy Compounds
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Fatty Acids, Unsaturated
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Growth Inhibitors
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Sesquiterpenes
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CKD 731
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fumagillin
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Aminopeptidases
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methionine aminopeptidase 2
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Metalloendopeptidases