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在布氏锥虫丝氨酸蛋白酶的RNA干扰筛选中鉴定出的一种必需信号肽肽酶。

An essential signal peptide peptidase identified in an RNAi screen of serine peptidases of Trypanosoma brucei.

作者信息

Moss Catherine X, Brown Elaine, Hamilton Alana, Van der Veken Pieter, Augustyns Koen, Mottram Jeremy C

机构信息

Wellcome Trust Centre for Molecular Parasitology, Institute of Infection, Immunity and Inflammation, College of Medical, Veterinary and Life Sciences, University of Glasgow, Glasgow, United Kingdom.

Medicinal Chemistry (UAMC), Department of Pharmaceutical Sciences, University of Antwerp, Wilrijk, Antwerp, Belgium.

出版信息

PLoS One. 2015 Mar 27;10(3):e0123241. doi: 10.1371/journal.pone.0123241. eCollection 2015.

Abstract

The serine peptidases of Trypanosoma brucei have been viewed as potential drug targets. In particular, the S9 prolyl oligopeptidase subfamily is thought to be a good avenue for drug discovery. This is based on the finding that some S9 peptidases are secreted and active in the mammalian bloodstream, and that they are a class of enzyme against which drugs have successfully been developed. We collated a list of all serine peptidases in T. brucei, identifying 20 serine peptidase genes, of which nine are S9 peptidases. We screened all 20 serine peptidases by RNAi to determine which, if any, are essential for bloodstream form T. brucei survival. All S9 serine peptidases were dispensable for parasite survival in vitro, even when pairs of similar genes, coding for oligopeptidase B or prolyl oligopeptidase, were targeted simultaneously. We also found no effect on parasite survival in an animal host when the S9 peptidases oligopeptidase B, prolyl oligopeptidase or dipeptidyl peptidase 8 were targeted. The only serine peptidase to emerge from the RNAi screen as essential was a putative type-I signal peptide peptidase (SPP1). This gene was essential for parasite survival both in vitro and in vivo. The growth defect conferred by RNAi depletion of SPP1 was rescued by expression of a functional peptidase from an RNAi resistant SPP1 gene. However, expression of catalytically inactive SPP1 was unable to rescue cells from the SPP1 depleted phenotype, demonstrating that SPP1 serine peptidase activity is necessary for T. brucei survival.

摘要

布氏锥虫的丝氨酸蛋白酶被视为潜在的药物靶点。特别是,S9脯氨酰寡肽酶亚家族被认为是药物研发的一个良好途径。这是基于以下发现:一些S9肽酶在哺乳动物血液中分泌并具有活性,而且它们是一类已成功开发出药物的酶。我们整理了布氏锥虫中所有丝氨酸蛋白酶的清单,鉴定出20个丝氨酸蛋白酶基因,其中9个是S9肽酶。我们通过RNA干扰筛选了所有20种丝氨酸蛋白酶,以确定哪些(如果有的话)对布氏锥虫血液型的存活至关重要。所有S9丝氨酸蛋白酶对于体外寄生虫的存活都是非必需的,即使同时靶向编码寡肽酶B或脯氨酰寡肽酶的成对相似基因也是如此。我们还发现,当靶向S9肽酶寡肽酶B、脯氨酰寡肽酶或二肽基肽酶8时,对动物宿主中的寄生虫存活没有影响。RNA干扰筛选中唯一被证明为必需的丝氨酸蛋白酶是一种假定的I型信号肽酶(SPP1)。该基因对于体外和体内的寄生虫存活都是必需的。通过表达来自RNA干扰抗性SPP1基因的功能性肽酶,可以挽救因RNA干扰耗尽SPP1而导致的生长缺陷。然而,催化无活性的SPP1的表达无法使细胞从SPP1耗尽的表型中恢复,这表明SPP1丝氨酸蛋白酶活性对于布氏锥虫的存活是必需的。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cab7/4376731/1a1467b299d2/pone.0123241.g001.jpg

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