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针对动基体原生动物感染的基于靶点的药物设计概述:人类非洲锥虫病、恰加斯病和利什曼病

An Overview on Target-Based Drug Design against Kinetoplastid Protozoan Infections: Human African Trypanosomiasis, Chagas Disease and Leishmaniases.

作者信息

Kourbeli Violeta, Chontzopoulou Eleni, Moschovou Kalliopi, Pavlos Dimitrios, Mavromoustakos Thomas, Papanastasiou Ioannis P

机构信息

Department of Pharmacy, Division of Pharmaceutical Chemistry, School of Health Sciences, National and Kapodistrian University of Athens, Panepistimioupoli-Zografou, 157 84 Athens, Greece.

Department of Organic Chemistry, Faculty of Chemistry, National and Kapodistrian University of Athens, Panepistimioupoli-Zografou, 157 71 Athens, Greece.

出版信息

Molecules. 2021 Jul 30;26(15):4629. doi: 10.3390/molecules26154629.

Abstract

The protozoan diseases Human African Trypanosomiasis (HAT), Chagas disease (CD), and leishmaniases span worldwide and therefore their impact is a universal concern. The present regimen against kinetoplastid protozoan infections is poor and insufficient. Target-based design expands the horizon of drug design and development and offers novel chemical entities and potential drug candidates to the therapeutic arsenal against the aforementioned neglected diseases. In this review, we report the most promising targets of the main kinetoplastid parasites, as well as their corresponding inhibitors. This overview is part of the Special Issue, entitled "Advances of Medicinal Chemistry against Kinetoplastid Protozoa ( and spp.) Infections: Drug Design, Synthesis and Pharmacology".

摘要

原生动物疾病——人类非洲锥虫病(HAT)、恰加斯病(CD)和利什曼病遍布全球,因此它们的影响是全球普遍关注的问题。目前针对动基体原生动物感染的治疗方案效果不佳且不足。基于靶点的设计拓展了药物设计与开发的视野,并为治疗上述被忽视疾病的药物库提供了新的化学实体和潜在的候选药物。在本综述中,我们报告了主要动基体寄生虫最有前景的靶点及其相应的抑制剂。本综述是名为“抗动基体原生动物(及 spp.)感染的药物化学进展:药物设计、合成与药理学”特刊的一部分。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3961/8348971/a01bbb4d4fdd/molecules-26-04629-g001.jpg

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