Piceatannol (3,4,3',5'-tetrahydroxy-trans-stilbene) is a naturally occurring protein-tyrosine kinase inhibitor.
Piceatannol (3,4,3'5'-tetrahydroxy-trans-stilbene), a plant secondary natural product that had previously been identified as an antileukemic principle, has been shown to be an inhibitor of protein-tyrosine kinase activity. Piceatannol inhibits the purified thymocyte protein-tyrosine kinase, p40, by competing for the peptide or protein substrate binding site (Ki = 15 microM). Piceatannol also inhibits the activity of the p56lck protein-tyrosine kinase measured either in LSTRA cell membranes or in intact cells. In contrast, piceatannol does not inhibit the activity of the cAMP-dependent protein kinase.
Geahlen
R L
RL
Department of Medicinal Chemistry and Pharmacognosy School of Pharmacy, Purdue University, West Lafayette, Indiana 47907.
McLaughlin
J L
JL
D000595:Amino Acid Sequence; D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000494:pharmacology*; D002417:Cattle; D002462:Cell Membrane / Q000201:enzymology; D002478:Cells, Cultured; D007700:Kinetics; D008969:Molecular Sequence Data; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors*; D013267:Stilbenes / Q000494:pharmacology*; D013379:Substrate Specificity; D013950:Thymus Gland / Q000201:enzymology
D000972:Antineoplastic Agents, Phytogenic; D013267:Stilbenes; C041525:3,3',4,5'-tetrahydroxystilbene; D011505:Protein-Tyrosine Kinases