A multiwell assay for inhibitors of phosphatidylinositol-3-kinase and the identification of natural product inhibitors

Anticancer Res. 1994 Nov-Dec;14(6B):2425-8.

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

  • Comparative Study
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Anthracenes
  • Anti-Infective Agents / chemistry
  • Anti-Infective Agents / pharmacology
  • Antibodies
  • Brain / enzymology
  • Cattle
  • Cyclopentane Monoterpenes
  • Emodin / chemistry
  • Emodin / pharmacology
  • Enzyme Inhibitors / analysis*
  • Enzyme Inhibitors / pharmacology
  • Glucosides / chemistry
  • Glucosides / pharmacology
  • Glycosides / chemistry
  • Glycosides / pharmacology
  • Immunoassay / methods
  • Kinetics
  • Molecular Structure
  • Perylene / analogs & derivatives
  • Perylene / chemistry
  • Perylene / pharmacology*
  • Phosphatidylinositol 3-Kinases
  • Phosphotransferases (Alcohol Group Acceptor) / antagonists & inhibitors*
  • Protein Kinase C / antagonists & inhibitors
  • Pyrans / chemistry
  • Pyrans / pharmacology
  • Rats
  • Signal Transduction
  • Spirostans / chemistry
  • Spirostans / pharmacology
  • Structure-Activity Relationship

Substances

  • Anthracenes
  • Anti-Infective Agents
  • Antibodies
  • Cyclopentane Monoterpenes
  • Enzyme Inhibitors
  • Glucosides
  • Glycosides
  • Pyrans
  • Spirostans
  • uttronin A
  • Perylene
  • hypericin
  • Phosphotransferases (Alcohol Group Acceptor)
  • Protein Kinase C
  • Emodin
  • asperuloside