Piceatannol (3,4,3',5'-tetrahydroxy-trans-stilbene) is a naturally occurring protein-tyrosine kinase inhibitor |
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Authors: | R L Geahlen J L McLaughlin |
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Institution: | Department of Medicinal Chemistry and Pharmacognosy School of Pharmacy, Purdue University, West Lafayette, Indiana 47907. |
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Abstract: | 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. |
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