Geahlen R L, McLaughlin J L
Department of Medicinal Chemistry and Pharmacognosy School of Pharmacy, Purdue University, West Lafayette, Indiana 47907.
Biochem Biophys Res Commun. 1989 Nov 30;165(1):241-5. doi: 10.1016/0006-291x(89)91060-7.
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.
白皮杉醇（3,4,3′,5′-四羟基反式芪）是一种植物次生天然产物，此前已被鉴定为抗白血病成分，现已证明它是一种蛋白酪氨酸激酶活性抑制剂。白皮杉醇通过竞争肽或蛋白质底物结合位点（Ki = 15微摩尔）来抑制纯化的胸腺细胞蛋白酪氨酸激酶p40。白皮杉醇还能抑制在LSTRA细胞膜或完整细胞中测得的p56lck蛋白酪氨酸激酶的活性。相比之下，白皮杉醇并不抑制环磷酸腺苷依赖性蛋白激酶的活性。
