Abstract
Small molecules that specifically activate an intracellular protein of interest are highly desirable. A generally applicable strategy, however, remains elusive. Herein we describe a small molecule-triggered bioorthogonal protein decaging technique that relies on the inverse electron-demand Diels-Alder reaction for eliminating a chemically caged protein side chain within living cells. This method permits the efficient activation of a given protein (for example, an enzyme) in its native cellular context within minutes.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Cycloaddition Reaction*
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Electrons
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Enzyme Activation
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Escherichia coli / genetics
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Escherichia coli / metabolism
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Gene Expression
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Genes, Reporter
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HEK293 Cells
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Humans
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Luciferases / chemistry*
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Luciferases / genetics
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Luciferases / metabolism
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Luminescent Measurements
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Lysine / chemistry*
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Molecular Conformation
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Plasmids
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Recombinant Proteins / chemistry
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Recombinant Proteins / genetics
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Recombinant Proteins / metabolism
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Small Molecule Libraries / chemistry*
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Staining and Labeling / methods
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Tetrazoles / chemistry*
Substances
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Recombinant Proteins
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Small Molecule Libraries
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Tetrazoles
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Luciferases
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Lysine