Abstract
The syntheses of a new class of barbiturate-based inhibitors for human and Escherichia Coli methionine aminopeptidase-1 (MetAP-1) are described. Some of the synthesized inhibitors show selective inhibition of the human enzyme with high potency.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, U.S. Gov't, Non-P.H.S.
MeSH terms
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Aminopeptidases / antagonists & inhibitors*
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Barbiturates / chemistry
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Barbiturates / pharmacology*
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Binding Sites
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Crystallography, X-Ray
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Escherichia coli / enzymology*
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Humans
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Methionyl Aminopeptidases
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Models, Chemical
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Protease Inhibitors / chemical synthesis
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Protease Inhibitors / pharmacology*
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Structure-Activity Relationship
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Substrate Specificity
Substances
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Barbiturates
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Protease Inhibitors
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Aminopeptidases
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Methionyl Aminopeptidases
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barbituric acid