从天然和合成资源中发现抗疟药物。

IF 3.5 4区 医学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY Current medicinal chemistry Pub Date : 2025-01-01 DOI:10.2174/0109298673312727240527064833
Nik Nur Solehah Fitri Nik Mohd Azam, Shatrah Othman, Yeun-Mun Choo
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引用次数: 0

摘要

尽管为根除疟疾做出了大量努力,但疟疾仍然是对全球健康的重大威胁。在根除这一疾病的过程中仍然面临着众多挑战,其中最主要的挑战是寄生虫的变异能力,从而导致抗药性。抗疟药物的发现一直依赖于表型和靶向两种方法。表型筛选已经发现了有希望的候选药物,而基于靶点的方法则通过利用化学验证的靶点和计算工具提供了一种更精确的方法。对疟原虫蛋白质结构的分析揭示了可用于药物治疗的靶点,为硅学筛选提供了机会。在基于靶点的方法中结合天然和合成来源的化合物,可加速新抗疟药物的发现。这篇综述探讨了以前从天然产品和合成来源发现抗疟药物的突破性进展,强调了它们在疟原虫中的特定靶蛋白。
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Antimalarial Drug Discovery from Natural and Synthetic Sources.

Malaria remains a significant global health threat despite extensive efforts aimed at its eradication. Numerous challenges persist in eliminating the disease, chief among them being the parasite's ability to mutate, resulting in drug resistance. The discovery of antimalarial drugs has relied on both phenotypic and target-based approaches. While phenotypic screening has identified promising candidates, target-based methods offer a more precise approach by leveraging chemically validated targets and computational tools. Analysis of Plasmodium spp . protein structures reveal druggable targets, offering opportunities for in silico screening. Combining compounds from natural and synthetic sources in a target-based approach accelerates the discovery of new antimalarial agents. This review explores previous breakthroughs in antimalarial drug discovery from natural products and synthetic origins, emphasizing their specific target proteins within Plasmodium species.

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来源期刊
Current medicinal chemistry
Current medicinal chemistry 医学-生化与分子生物学
CiteScore
8.60
自引率
2.40%
发文量
468
审稿时长
3 months
期刊介绍: Aims & Scope Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews and guest edited thematic issues written by leaders in the field covering a range of the current topics in medicinal chemistry. The journal also publishes reviews on recent patents. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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