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在抗生素发现中靶向革兰氏阴性外膜的创意。

Creative targeting of the Gram-negative outer membrane in antibiotic discovery.

机构信息

Michael G. DeGroote Institute for Infectious Disease Research, Department of Biochemistry and Biomedical Sciences, McMaster University, Hamilton, Ontario, Canada.

出版信息

Ann N Y Acad Sci. 2020 Jan;1459(1):69-85. doi: 10.1111/nyas.14280. Epub 2019 Nov 24.

Abstract

The rising threat of multidrug-resistant Gram-negative bacteria is exacerbated by the scarcity of new antibiotics in the development pipeline. Permeability through the outer membrane remains one of the leading hurdles in discovery efforts. However, the essentiality of a robust outer membrane makes itself an intriguing antimicrobial target. Herein, we review drug discovery efforts targeting the outer membrane and the prospective antimicrobial leads identified.

摘要

革兰氏阴性菌的耐药性日益严重,而新抗生素的研发却乏善可陈,这使得情况更加恶化。通过外膜的通透性仍然是发现工作中的主要障碍之一。然而,坚固的外膜的必要性使其本身成为一个有趣的抗菌靶点。本文综述了针对外膜的药物发现工作以及已确定的有前景的抗菌先导化合物。

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