Abstract
A convenient and reliable multisample assay for the screening of inhibitors of the growth factor signalling enzyme phosphatidylinositol-3-kinase (PtdIns-3-K) has been developed. Four natural product inhibitors of Ptdlns-3-K have been identified with IC50 values for hypericin 0.18 microM, emodin 3.3 microM, asperuloside 2.0 microM and uttronin A 1.1 microM.
Publication types
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Comparative Study
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Animals
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Anthracenes
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Anti-Infective Agents / chemistry
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Anti-Infective Agents / pharmacology
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Antibodies
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Brain / enzymology
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Cattle
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Cyclopentane Monoterpenes
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Emodin / chemistry
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Emodin / pharmacology
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Enzyme Inhibitors / analysis*
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Enzyme Inhibitors / pharmacology
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Glucosides / chemistry
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Glucosides / pharmacology
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Glycosides / chemistry
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Glycosides / pharmacology
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Immunoassay / methods
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Kinetics
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Molecular Structure
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Perylene / analogs & derivatives
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Perylene / chemistry
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Perylene / pharmacology*
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Phosphatidylinositol 3-Kinases
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Phosphotransferases (Alcohol Group Acceptor) / antagonists & inhibitors*
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Protein Kinase C / antagonists & inhibitors
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Pyrans / chemistry
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Pyrans / pharmacology
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Rats
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Signal Transduction
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Spirostans / chemistry
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Spirostans / pharmacology
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Structure-Activity Relationship
Substances
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Anthracenes
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Anti-Infective Agents
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Antibodies
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Cyclopentane Monoterpenes
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Enzyme Inhibitors
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Glucosides
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Glycosides
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Pyrans
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Spirostans
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uttronin A
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Perylene
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hypericin
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Phosphotransferases (Alcohol Group Acceptor)
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Protein Kinase C
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Emodin
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asperuloside