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针对蛋白质组和细胞器寻找潜在的抗疟药物候选物。

Targeting the proteome and organelles for potential antimalarial drug candidates.

作者信息

Abugri James, Ayariga Joseph, Sunwiale Samuel Sunyazi, Wezena Cletus Adiyaga, Gyamfi Julien Agyemang, Adu-Frimpong Michael, Agongo Godfred, Dongdem Julius Tieroyaare, Abugri Daniel, Dinko Bismarck

机构信息

Department of Biochemistry and Forensic Sciences, School of Chemical and Biochemical Sciences, C. K. Tedam University of Technology and Applied Sciences (CKT-UTAS), Navrongo, Ghana.

The Biomedical Engineering Programme, Alabama State University, Montgomery, AL, 36104, USA.

出版信息

Heliyon. 2022 Aug;8(8):e10390. doi: 10.1016/j.heliyon.2022.e10390. Epub 2022 Aug 24.

Abstract

There is an unmet need to unearth alternative treatment options for malaria, wherein this quest is more pressing in recent times due to high morbidity and mortality data arising mostly from the endemic countries coupled with partial diversion of attention from the disease in view of the SARS-Cov-2 pandemic. Available therapeutic options for malaria have been severely threatened with the emergence of resistance to almost all the antimalarial drugs by the parasite in humans, which is a worrying situation. Artemisinin combination therapies (ACT) that have so far been the mainstay of malaria have encountered resistance by malaria parasite in South East Asia, which is regarded as a notorious ground zero for the emergence of resistance to antimalarial drugs. This review analyzes a few key druggable targets for the parasite and the potential of specific inhibitors to mitigate the emerging antimalarial drug resistance problem by providing a concise assessment of the essential proteins of the malaria parasite that could serve as targets. Moreover, this work provides a summary of the advances made in malaria parasite biology and the potential to leverage these findings for antimalarial drug production.

摘要

挖掘疟疾的替代治疗方案存在未满足的需求,鉴于主要来自疟疾流行国家的高发病率和死亡率数据,以及由于新冠疫情导致对该疾病的部分注意力转移,这一需求在近期更为紧迫。疟疾现有的治疗选择因疟原虫对几乎所有抗疟药物产生耐药性而受到严重威胁,这是一个令人担忧的情况。迄今为止作为疟疾主要治疗方法的青蒿素联合疗法(ACT)在东南亚已遭遇疟原虫耐药性问题,东南亚被视为抗疟药物耐药性出现的臭名昭著的源头。本综述分析了疟原虫的一些关键可成药靶点,以及特定抑制剂通过简要评估可作为靶点的疟原虫必需蛋白来缓解新出现的抗疟药物耐药性问题的潜力。此外,这项工作总结了疟原虫生物学方面取得的进展以及利用这些发现生产抗疟药物的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d64e/9433685/1d60f27cc36b/gr1.jpg

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