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毁灭菌素B,一种液泡型H(+)转运ATP酶的特异性且易于逆转的抑制剂。

Destruxin B, a specific and readily reversible inhibitor of vacuolar-type H(+)-translocating ATPase.

作者信息

Muroi M, Shiragami N, Takatsuki A

机构信息

Animal and Cellular Systems Laboratory, Physical and Chemical Research Institute (RIKEN), Saitama, Japan.

出版信息

Biochem Biophys Res Commun. 1994 Dec 15;205(2):1358-65. doi: 10.1006/bbrc.1994.2815.

Abstract

Destruxin B, a peptide antibiotic, inhibits vacuolar-type ATPase (V-ATPase) specifically and dose-dependently among ATPases examined. Acidification of intracellular organelles is also blocked by destruxin B at comparable concentrations when assessed by accumulation of acridine orange. The inhibitory activity of destruxin B is weaker than that of bafilomycin A1 and folimycin, well known macrolide inhibitors of V-ATPase, when compared at the same molar concentration. Unlike the macrolide antibiotics, however, the inhibitory activity of destruxin B is readily reversible. This novel feature of destruxin B should make it a useful probe in the analysis of V-ATPase function in cell physiology.

摘要

环肽毒素B是一种肽类抗生素,在所检测的ATP酶中,它能特异性且剂量依赖性地抑制液泡型ATP酶(V-ATP酶)。当通过吖啶橙积累来评估时,在相当的浓度下,环肽毒素B也会阻断细胞内细胞器的酸化。当以相同摩尔浓度进行比较时,环肽毒素B的抑制活性弱于巴弗洛霉素A1和磷霉素,这两种是广为人知的V-ATP酶大环内酯类抑制剂。然而,与大环内酯类抗生素不同的是,环肽毒素B的抑制活性很容易逆转。环肽毒素B的这一新颖特性使其成为细胞生理学中分析V-ATP酶功能的有用探针。

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