靶向SARS-CoV-2必需蛋白的共价抑制剂结构基础研究进展

IF 3.5 4区 医学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY Current medicinal chemistry Pub Date : 2025-01-03 DOI:10.2174/0109298673323348241208080419
Israr Fatima, Fahad M Alshabrmi, Faris F Aba Alkhayl, Muhammad Qasim, Almera Shafqat, Sara Batool, Muhammad Jawad, Muhammad Tahir Ul Qamar, Abdur Rehman
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引用次数: 0

摘要

共价抑制剂在药物治疗的发展中起着关键作用,因为它们与靶生物分子形成稳定的、不可逆的键,从而延长治疗效果并提高疗效。自19世纪末共价抑制剂首次出现以来,该领域迅速创新,目前共价抑制剂约占所有上市治疗药物的30%。严重急性呼吸综合征冠状病毒2 (SARS-CoV-2)导致2019冠状病毒病(COVID-19)大流行。SARS-CoV-2需要用有益且副作用最小的药物治疗。有必要制定候选药物来治疗这种病原体。本文将简要讨论共价药物的优势,然后介绍其作用方法,并更深入地讨论针对SARS-CoV-2的安全有效的共价酶抑制剂。我们主要关注的是研究共价抑制剂,这些共价抑制剂主要参与阻止病毒SARS-CoV-2进入宿主细胞及其复制和翻译过程。在抗sars - cov -2药物的开发中,研究人员可以使用这些已报道的药物作为潜在的候选药物。
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Advancements in Structural Basis of Covalent Inhibitors Targeting SARS-CoV-2 Essential Proteins.

Covalent inhibitors play a pivotal role in the development of pharmaceutical therapies, as they form stable, irreversible bonds with target biomolecules, leading to prolonged therapeutic effects and enhanced efficacy. Since covalent inhibitors first appeared in the late 1800s, the field has become innovative rapidly, and covalent inhibitors now account for around 30% of all marketed therapeutics. The severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) causes the pandemic of Coronavirus Disease 2019 (COVID-19). SARS-CoV-2 needs to be cured with a medicine that is beneficial and with the least side effects. It is necessary to formulate drug candidates to treat this pathogen. The predominance of covalent medications will be briefly discussed in this review, followed by an introduction to their methods of action, as well as more thorough discussions of the safe and effective covalent enzyme inhibitors against SARS-CoV-2. Our main concern is to study covalent inhibitors which are mainly involved in blocking the viral entry of the virus SARS-CoV-2 into the host cell along with its replication and translation process. In the development of anti-SARS-CoV-2 medicines researchers can use those reported drugs as prospective candidates.

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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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