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斑蝥素,另一种抑制1型和2A型丝氨酸/苏氨酸蛋白磷酸酶活性的天然毒素。

Cantharidin, another natural toxin that inhibits the activity of serine/threonine protein phosphatases types 1 and 2A.

作者信息

Honkanen R E

机构信息

Department of Biochemistry, College of Medicine, University of South Alabama, Mobile 36688.

出版信息

FEBS Lett. 1993 Sep 20;330(3):283-6. doi: 10.1016/0014-5793(93)80889-3.

Abstract

Cantharidin, a natural toxicant of blister beetles, is a strong inhibitor of protein phosphatases types 1 (PP1) and 2A (PP2A). Like okadaic acid, cantharidin inhibits the activity of the purified catalytic subunit of PP2A (IC50 = 0.16 microM) at a lower concentration than that of PP1 (IC50 = 1.7 microM) and only inhibits the activity of protein phosphatase type 2B (PP2B) at high concentrations. Dose-inhibition studies conducted with whole cell homogenates indicate that cantharidin also inhibits the native forms of these enzymes. Thus, cantharidin, which is economical and readily available, may be useful as an additional probe for studying the functions of serine/threonine protein phosphatases.

摘要

斑蝥素是一种斑蝥甲虫的天然毒素,是蛋白磷酸酶1型(PP1)和2A型(PP2A)的强效抑制剂。与冈田酸一样,斑蝥素在比PP1(IC50 = 1.7 microM)更低的浓度下就能抑制纯化的PP2A催化亚基的活性(IC50 = 0.16 microM),并且只有在高浓度时才会抑制蛋白磷酸酶2B型(PP2B)的活性。用全细胞匀浆进行的剂量抑制研究表明,斑蝥素也能抑制这些酶的天然形式。因此,经济且易于获得的斑蝥素可能作为研究丝氨酸/苏氨酸蛋白磷酸酶功能的额外探针。

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