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用化学探针解析抗真菌剂的生物活性

Deciphering the Biological Activities of Antifungal Agents with Chemical Probes.

作者信息

Fridman Micha, Sakurai Kaori

机构信息

School of Chemistry, Raymond & Beverly Sackler Faculty of Exact Sciences, Tel Aviv University, Tel Aviv, 6997801, Israel.

Department of Biotechnology and Life Science, Tokyo University of Agriculture and Technology, 4-24-16, Naka-cho, Koganei-shi, Tokyo, 184-8588, Japan.

出版信息

Angew Chem Int Ed Engl. 2023 Mar 13;62(12):e202211927. doi: 10.1002/anie.202211927. Epub 2023 Jan 26.

DOI:10.1002/anie.202211927
PMID:36628503
Abstract

The growing number of fungal infections caused by pathogens resistant to one or more classes of antifungal drugs emphasizes the threat that these microorganisms pose to animal and human health and global food security. Open questions remain regarding the mechanisms of action of the limited repertoire of antifungal agents, making it challenging to rationally develop more efficacious therapeutics. In recent years, the use of chemical biology approaches has resolved some of these questions and has provided new promising concepts to guide the design of antifungal agents. By focusing on examples from studies carried out in recent years, this minireview describes the key roles that probes based on antifungal agents and their derivatives have played in uncovering details about their activities, in detecting resistance, and in characterizing the interactions between these agents and their targets.

摘要

对一类或多类抗真菌药物耐药的病原体导致的真菌感染日益增多,凸显了这些微生物对动物和人类健康以及全球粮食安全构成的威胁。关于有限种类抗真菌药物的作用机制仍存在一些悬而未决的问题,这使得合理开发更有效的治疗方法具有挑战性。近年来,化学生物学方法的应用解决了其中一些问题,并提供了新的有前景的概念来指导抗真菌药物的设计。通过聚焦近年来开展的研究实例,本综述描述了基于抗真菌药物及其衍生物的探针在揭示其活性细节、检测耐药性以及表征这些药物与其靶点之间相互作用方面所发挥的关键作用。

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Poacic Acid, a Plant-Derived Stilbenoid, Augments Cell Wall Chitin Production, but Its Antifungal Activity Is Hindered by This Polysaccharide and by Fungal Essential Metals.原儿茶酸,一种植物衍生的芪类化合物,可增强细胞壁几丁质的产生,但它的抗真菌活性受到这种多糖和真菌必需金属的抑制。
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