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N-咖啡酰酪胺通过抑制蛋白质酪氨酸磷酸化和诱导半胱天冬酶-3来阻止U937和Jurkat细胞的生长。

N-Caffeoyltyramine arrests growth of U937 and Jurkat cells by inhibiting protein tyrosine phosphorylation and inducing caspase-3.

作者信息

Park Jae B, Schoene Norberta

机构信息

Phytonutrients Laboratory, US Department of Agriculture, Building 307, Room 313, PL, BHNRC, ARS, Beltsville, MD 20705, USA.

出版信息

Cancer Lett. 2003 Dec 30;202(2):161-71. doi: 10.1016/j.canlet.2003.08.010.

Abstract

N-Cinnamoyltyramine, N-caffeoyltyramine, N-feruloyltyramine, and N-sinapoyltyramine were synthesized and investigated to identify the most potent compound with anti-proliferation effect on HL-60, U937 and Jurkat cells. N-Caffeoyltyramine was the most potent with GI(50)=10 microM. The treatment of the cells with N-caffeoyltyramine activated caspase-3 activity, and inhibited the growth of cells via decreasing in protein tyrosine kinase activity including epidermal growth factor receptor. These data indicate that N-caffeoyltyramine is most potent compound, inducing cell death of the cancer cells by inhibiting protein tyrosine kinases and activating caspase-3 activity.

摘要

合成并研究了N-肉桂酰酪胺、N-咖啡酰酪胺、N-阿魏酰酪胺和N-芥子酰酪胺,以确定对HL-60、U937和Jurkat细胞具有最强抗增殖作用的化合物。N-咖啡酰酪胺的活性最强,其半数生长抑制浓度(GI(50))为10微摩尔。用N-咖啡酰酪胺处理细胞可激活半胱天冬酶-3的活性,并通过降低包括表皮生长因子受体在内的蛋白质酪氨酸激酶活性来抑制细胞生长。这些数据表明,N-咖啡酰酪胺是最有效的化合物,通过抑制蛋白质酪氨酸激酶和激活半胱天冬酶-3的活性来诱导癌细胞死亡。

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