Lauryl Gallate Inhibits the Activity of Protein Tyrosine Kinase c-Src Purified from Human Platelets

C. Palacios, C. Cespón, C. Martín de la Vega, G. Roy, A. Serrano, M. Salinas, P. Gónzalez-Porqué
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引用次数: 9

Abstract

The inhibitory effect of gallic acid (3,4,5-trihydroxybenzoic acid), and its ester derivatives methyl, propyl, octyl and lauryl has been tested on the tyrosine kinase activity of affinity purified c-Src from human platelets, using the artificial substrate Poly (Glu.Na, Tyr) 4:1. When tested as inhibitor of the autophosphorylation of the enzyme and the phosphorylation of the protein tyrosine phosphatase SHP-1 by c-Src, lauryl gallate was found to be a more potent inhibitor than other widely used protein tyrosine kinase (PTK) inhibitors such as genistein and herbimycin A. However, lauryl gallate did not inhibit the activity of the serine threonine kinases protein kinase A (PKA) and casein kinase II (CKII) from rat brain.
十二烷基没食子酸酯抑制人血小板纯化蛋白酪氨酸激酶c-Src的活性
采用人工底物Poly (Glu)检测没食子酸(3,4,5-三羟基苯甲酸)及其酯衍生物甲基、丙基、辛基和十二烷基对亲和纯化的人血小板c-Src酪氨酸激酶活性的抑制作用。《提珥书》4:1。当用c-Src作为自磷酸化酶和蛋白酪氨酸磷酸酶SHP-1的抑制剂进行测试时,发现没食子酸月桂酯比其他广泛使用的蛋白酪氨酸激酶(PTK)抑制剂(如染料木素和herbimcin a)更有效。然而,没食子酸月桂酯不抑制大鼠脑中丝氨酸苏氨酸激酶蛋白激酶a (PKA)和酪蛋白激酶II (CKII)的活性。
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