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甲状腺素23-乙酸酯是一种新型的蛋白磷酸酶PP2A特异性抑制剂。

Thyrsiferyl 23-acetate is a novel specific inhibitor of protein phosphatase PP2A.

作者信息

Matsuzawa S, Suzuki T, Suzuki M, Matsuda A, Kawamura T, Mizuno Y, Kikuchi K

机构信息

Section of Biochemistry, Institute of Immunological Science, Hokkaido University, Sapporo, Japan.

出版信息

FEBS Lett. 1994 Dec 19;356(2-3):272-4. doi: 10.1016/0014-5793(94)01281-4.

Abstract

Thyrsiferyl 23-acetate (TF23A), a cytotoxic compound from marine red alga, has been shown to potently and specifically inhibit serine/threonine protein phosphatase 2A (PP2A) with IC50 values of 4-16 microM, depending on the enzyme concentration. TF23A did not affect activity of protein phosphatase 1 (PP1), 2B (PP2B), 2C (PP2C), or protein tyrosine phosphatases (PTP) up to 1 mM. It inhibited PP2A activity in a crude extract of a human T cell line, Jurkat cell, as well as the purified catalytic subunit. Thus, TF23A proved to be a novel useful probe for clearly distinguishing the activity of PP2A from those of the other protein phosphatases in crude cell extracts and identification of cellular processes that are regulated by PP2A.

摘要

23-乙酸甲状腺素(TF23A)是一种从海洋红藻中提取的具有细胞毒性的化合物,已证明它能有效且特异性地抑制丝氨酸/苏氨酸蛋白磷酸酶2A(PP2A),其半数抑制浓度(IC50)值为4 - 16微摩尔,具体数值取决于酶的浓度。在高达1毫摩尔的浓度下,TF23A对蛋白磷酸酶1(PP1)、2B(PP2B)、2C(PP2C)或蛋白酪氨酸磷酸酶(PTP)的活性没有影响。它能抑制人T细胞系Jurkat细胞的粗提物以及纯化的催化亚基中的PP2A活性。因此,TF23A被证明是一种新型的有用探针,可用于在粗细胞提取物中清晰区分PP2A与其他蛋白磷酸酶的活性,并鉴定受PP2A调节的细胞过程。

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