title: A multiwell assay for inhibitors of phosphatidylinositol-3-kinase and the identification of natural product inhibitors.
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.
authors.affiliation: Arizona Cancer Center, University of Arizona, Tucson 85724.
authors.forename: T
authors.initials: T
authors.lastname: Frew
authors.forename: G
authors.initials: G
authors.lastname: Powis
authors.forename: M
authors.initials: M
authors.lastname: Berggren
authors.forename: R T
authors.initials: RT
authors.lastname: Abraham
authors.forename: C L
authors.initials: CL
authors.lastname: Ashendel
authors.forename: L H
authors.initials: LH
authors.lastname: Zalkow
authors.forename: C
authors.initials: C
authors.lastname: Hudson
authors.forename: S
authors.initials: S
authors.lastname: Qazia
authors.forename: E
authors.initials: E
authors.lastname: Gruszecka-Kowalik
authors.forename: R
authors.initials: R
authors.lastname: Merriman
mesh_terms: D000818:Animals; D000873:Anthracenes; D000890:Anti-Infective Agents / Q000737:chemistry / Q000494:pharmacology; D000906:Antibodies; D001921:Brain / Q000201:enzymology; D002417:Cattle; D000081004:Cyclopentane Monoterpenes; D004642:Emodin / Q000737:chemistry / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000032:analysis* / Q000494:pharmacology; D005960:Glucosides / Q000737:chemistry / Q000494:pharmacology; D006027:Glycosides / Q000737:chemistry / Q000494:pharmacology; D007118:Immunoassay / Q000379:methods; D007700:Kinetics; D015394:Molecular Structure; D010569:Perylene / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology*; D019869:Phosphatidylinositol 3-Kinases; D017853:Phosphotransferases (Alcohol Group Acceptor) / Q000037:antagonists & inhibitors*; D011493:Protein Kinase C / Q000037:antagonists & inhibitors; D011714:Pyrans / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D015398:Signal Transduction; D013150:Spirostans / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000873:Anthracenes; D000890:Anti-Infective Agents; D000906:Antibodies; D000081004:Cyclopentane Monoterpenes; D004642:Emodin; D004791:Enzyme Inhibitors; D005960:Glucosides; D006027:Glycosides; D010569:Perylene; D019869:Phosphatidylinositol 3-Kinases; D017853:Phosphotransferases (Alcohol Group Acceptor); D011493:Protein Kinase C; D011714:Pyrans; D013150:Spirostans; C092288:uttronin A; C004965:hypericin; C077956:asperuloside