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抗结核肽及肽模拟物的合成与生物活性:最新进展

Synthesis and bioactivity of antitubercular peptides and peptidomimetics: an update.

作者信息

De Leon Rodriguez Luis M, Kaur Harveen, Brimble Margaret A

机构信息

School of Chemical Sciences, The University of Auckland, Auckland, New Zealand.

出版信息

Org Biomol Chem. 2016 Jan 28;14(4):1177-87. doi: 10.1039/c5ob02298c. Epub 2015 Dec 8.

DOI:10.1039/c5ob02298c
PMID:26645944
Abstract

Mycobacterium tuberculosis is the causative agent of tuberculosis (TB), an infection that has been declared a global public health emergency by the World Health Organization. Current anti-TB therapies are limited in their efficacy and have failed to prevent the spread of TB, due to the long term drug compliance required and the genesis of multidrug-resistant strains (MDR). The number of chemotherapeutic agents currently available to treat MDR is limited, therefore there is a great need for new anti-TB drugs. Anti-TB peptides and peptidomimetics have emerged as an important and growing class of chemotherapeutic agents. This mini-review provides an update on peptides that exhibit very potent anti-TB activity, and their chemical syntheses, which could potentially be included in the pipeline for new anti-TB drug development.

摘要

结核分枝杆菌是结核病(TB)的病原体,结核病已被世界卫生组织宣布为全球突发公共卫生事件。由于需要长期药物依从性以及多重耐药菌株(MDR)的产生,目前的抗结核疗法疗效有限,无法阻止结核病的传播。目前可用于治疗耐多药结核病的化疗药物数量有限,因此迫切需要新型抗结核药物。抗结核肽和拟肽已成为一类重要且不断发展的化疗药物。本综述提供了具有非常强效抗结核活性的肽及其化学合成的最新信息,这些肽有可能被纳入新的抗结核药物研发流程中。

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Structure-Activity Relationships of Wollamide Cyclic Hexapeptides with Activity against Drug-Resistant and Intracellular .
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AntiTbPdb: a knowledgebase of anti-tubercular peptides.抗结核肽数据库:抗结核肽知识库。
Database (Oxford). 2018 Jan 1;2018. doi: 10.1093/database/bay025.