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抗药物发现:现状与直觉。

Anti- Drug Discovery: Current Status and Gut Feelings.

机构信息

Commonwealth Scientific and Industrial Research Organization, Biomedical Manufacturing, Clayton, Victoria 3168, Australia.

Griffith Institute for Drug Discovery, Griffith University, Nathan, Queensland 4111, Australia.

出版信息

J Med Chem. 2020 Nov 25;63(22):13330-13354. doi: 10.1021/acs.jmedchem.0c00910. Epub 2020 Sep 16.

DOI:10.1021/acs.jmedchem.0c00910
PMID:32869995
Abstract

parasites are ubiquitous protozoans of global importance that impact a wide range of animals including humans. They are the most common enteric pathogen of cats and dogs in developed countries and infect ∼1 billion people worldwide. While infections can be asymptomatic, they often result in severe and chronic diseases. There is also mounting evidence that they are linked to postinfection disorders. Despite growing evidence of the widespread morbidity associated with infections, current treatment options are limited to compound classes with broad antimicrobial activity. Frontline anti- drugs are also associated with increasing drug resistance and treatment failures. To improve the health and well-being of millions, new selective anti- drugs are needed alongside improved health education initiatives. Here we discuss current treatment options together with recent advances and gaps in drug discovery. We also propose criteria to guide the discovery of new anti- compounds.

摘要

寄生虫是具有全球重要性的普遍原生动物,影响包括人类在内的广泛动物。它们是发达国家猫和狗最常见的肠道病原体,全世界有 10 亿人感染。虽然 感染可能无症状,但它们常导致严重和慢性疾病。越来越多的证据表明,它们与感染后疾病有关。尽管越来越多的证据表明与 感染相关的发病率广泛,但目前的治疗选择仅限于具有广泛抗菌活性的化合物类别。一线抗寄生虫药物也与耐药性增加和治疗失败有关。为了改善数百万人的健康和福祉,除了改善健康教育计划外,还需要新的选择性抗寄生虫药物。在这里,我们讨论了当前的治疗选择,以及药物发现的最新进展和差距。我们还提出了指导新抗寄生虫化合物发现的标准。

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