Abstract
A pyrene-functionalized peptidic inhibitor binds to and inhibits β-tryptase in a non-competitive and reversible manner even in cells. Upon protein binding a fluorescence increase of the two pyrene fluorophores is observed which allows using as a fluorescent light-up probe for this enzyme.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Cell Death / drug effects
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Cell Survival / drug effects
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Dose-Response Relationship, Drug
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Fluorescent Dyes / chemical synthesis
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Fluorescent Dyes / chemistry
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Fluorescent Dyes / pharmacology*
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Humans
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Light*
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Mast Cells
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Models, Molecular
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Molecular Conformation
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Serine Proteinase Inhibitors / chemical synthesis
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Serine Proteinase Inhibitors / chemistry
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Serine Proteinase Inhibitors / pharmacology*
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Structure-Activity Relationship
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Tryptases / antagonists & inhibitors*
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Tryptases / metabolism
Substances
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Fluorescent Dyes
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Serine Proteinase Inhibitors
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Tryptases