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互隔交链孢酚单甲醚是一种新型且特异性的丝氨酸/苏氨酸蛋白磷酸酶1(PP1)抑制剂。

Tautomycetin is a novel and specific inhibitor of serine/threonine protein phosphatase type 1, PP1.

作者信息

Mitsuhashi S, Matsuura N, Ubukata M, Oikawa H, Shima H, Kikuchi K

机构信息

Division of Biochemical Oncology and Immunology, Institute for Genetic Medicine, Hokkaido University, Kita-15, Nishi-7, Kita-ku, Sapporo 060-0815, Japan.

出版信息

Biochem Biophys Res Commun. 2001 Sep 21;287(2):328-31. doi: 10.1006/bbrc.2001.5596.

Abstract

Here we isolated tautomycetin, TC, and examined its phosphatase inhibitory activity. Recently we have reported that the left-hand moiety of tautomycin, TM, and the right one containing the spiroketal are essentially required for inhibition of protein phosphatase, PP, and induction of apoptosis, respectively. TC is structurally almost identical to TM except that TC is lacking the spiroketal, which has the potential apoptosis-inducing activity. TC specifically inhibited PP1 activity, IC50 values for purified PP1 and PP2A enzymes being 1.6 and 62 nM, respectively, whereas the IC50 values of TM were 0.21 and 0.94 nM, respectively. These results demonstrate that TC is the most specific PP1 inhibitor out of over 40 species of natural phosphatase inhibitors reported, strongly suggesting that TC is a novel powerful tool to elucidate the physiological roles of PP1 in various biological events.

摘要

我们在此分离出了互隔交链孢酚(TC),并检测了其磷酸酶抑制活性。最近我们报道过,互隔交链孢霉素(TM)的左手部分以及含有螺环缩酮的右手部分,分别是抑制蛋白磷酸酶(PP)和诱导细胞凋亡所必需的。TC在结构上与TM几乎相同,只是TC缺少具有潜在凋亡诱导活性的螺环缩酮。TC特异性抑制PP1活性,纯化的PP1和PP2A酶的IC50值分别为1.6和62 nM,而TM的IC50值分别为0.21和0.94 nM。这些结果表明,TC是已报道的40多种天然磷酸酶抑制剂中最具特异性的PP1 抑制剂,这有力地表明TC是阐明PP1在各种生物学事件中的生理作用的一种新型有力工具。 94 nM。这些结果表明,TC是已报道的40多种天然磷酸酶抑制剂中最具特异性PP1抑制剂,这有力地表明TC是阐明PP1在各种生物学事件中的生理作用的一种新型有力工具。94 nM。这些结果表明,TC是已报道的40多种天然磷酸酶抑制剂中最具特异性PP1抑制剂,这有力地表明TC是阐明PP1在各种生物学事件中的生理作用的一种新型有力工具。

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