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肽基氟甲基酮对锥虫的裂解作用。

Lysis of trypanosomes by peptidyl fluoromethyl ketones.

作者信息

Ashall F, Angliker H, Shaw E

机构信息

Department of Pure and Applied Biology, Imperial College of Science, Technology and Medicine, South Kensington, London, UK.

出版信息

Biochem Biophys Res Commun. 1990 Jul 31;170(2):923-9. doi: 10.1016/0006-291x(90)92179-4.

DOI:10.1016/0006-291x(90)92179-4
PMID:2116800
Abstract

Peptidyl fluoromethyl ketones, improved reagents for inactivating cysteinyl and serine proteinases, have provided unexpected results when applied to intact trypanosomes. A lethal effect was observed but limited to the infectious phase of the parasitic growth cycle. Since the inhibitors are known only to act on proteases, the result implies the existence of a protease of critical importance during the infectious phase. A labelled inhibitor, Cbz-Ala-[3H]Phe-CH2F, indicated that the killing effect correlated with the labelling of a 68 kd protein in the trypomastigotes which we deduce is an essential protease.

摘要

肽基氟甲基酮是用于使半胱氨酸和丝氨酸蛋白酶失活的改良试剂,当应用于完整的锥虫时产生了意想不到的结果。观察到了致死效应,但仅限于寄生虫生长周期的感染阶段。由于已知这些抑制剂仅作用于蛋白酶,该结果意味着在感染阶段存在一种至关重要的蛋白酶。一种标记抑制剂Cbz-Ala-[³H]Phe-CH₂F表明,杀伤效应与锥鞭毛体中一种68kd蛋白质的标记相关,我们推断该蛋白质是一种必需的蛋白酶。

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The cysteine proteinase inhibitor Z-Phe-Ala-CHN2 alters cell morphology and cell division activity of Trypanosoma brucei bloodstream forms in vivo.
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Cysteine protease inhibitors cure an experimental Trypanosoma cruzi infection.半胱氨酸蛋白酶抑制剂可治愈实验性克氏锥虫感染。
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Trypanosomatid cysteine protease activity may be enhanced by a kininogen-like moiety from host serum.锥虫类半胱氨酸蛋白酶的活性可能会被宿主血清中一种类似激肽原的成分增强。
Biochem J. 1995 Jan 15;305 ( Pt 2)(Pt 2):549-56. doi: 10.1042/bj3050549.