A multiwell assay for inhibitors of phosphatidylinositol-3-kinase and the identification of natural product inhibitors.
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.
Frew
T
T
Arizona Cancer Center, University of Arizona, Tucson 85724.
Powis
G
G
Berggren
M
M
Abraham
R T
RT
Ashendel
C L
CL
Zalkow
L H
LH
Hudson
C
C
Qazia
S
S
Gruszecka-Kowalik
E
E
Merriman
R
R
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
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