Abstract
The synthesis and biochemical characterization of AX4697, a fluorescent, bisindolylmaleimide-derived probe for PKCalpha and beta, is described. AX4697 was able to quantify changes in PKC expression in drug-treated Jurkat cells and was shown to covalently label PKCalpha on C619, a residue that sits just outside the active site.
MeSH terms
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Catalytic Domain
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Drug Design
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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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Indoles / chemical synthesis*
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Indoles / chemistry
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Indoles / pharmacology*
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Jurkat Cells
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Maleimides / chemical synthesis*
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Maleimides / chemistry
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Maleimides / pharmacology*
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Molecular Structure
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Protein Kinase C / metabolism*
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Protein Kinase C beta
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Protein Kinase C-alpha / metabolism*
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Structure-Activity Relationship
Substances
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AX4697
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Fluorescent Dyes
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Indoles
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Maleimides
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Protein Kinase C
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Protein Kinase C beta
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Protein Kinase C-alpha
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bisindolylmaleimide