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半胱氨酸生物合成途径中关键酶抑制剂的研究进展:丝氨酸乙酰转移酶和 O-乙酰丝氨酸巯基转移酶。

Advancements in inhibitors of crucial enzymes in the cysteine biosynthetic pathway: Serine acetyltransferase and O-acetylserine sulfhydrylase.

机构信息

Department of Pharmacy, Henan Provincial People's Hospital, Zhengzhou University People's Hospital, Henan University People's Hospital, Zhengzhou, Henan, China.

Department of Pharmacy, Jinan Vocational College of Nursing, Jinan, China.

出版信息

Chem Biol Drug Des. 2024 Jul;104(1):e14573. doi: 10.1111/cbdd.14573.

DOI:10.1111/cbdd.14573
PMID:38965664
Abstract

Infectious diseases have been jeopardized problem that threaten public health over a long period of time. The growing prevalence of drug-resistant pathogens and infectious cases have led to a decrease in the number of effective antibiotics, which highlights the urgent need for the development of new antibacterial agents. Serine acetyltransferase (SAT), also known as CysE in certain bacterial species, and O-acetylserine sulfhydrylase (OASS), also known as CysK in select bacteria, are indispensable enzymes within the cysteine biosynthesis pathway of various pathogenic microorganisms. These enzymes play a crucial role in the survival of these pathogens, making SAT and OASS promising targets for the development of novel anti-infective agents. In this comprehensive review, we present an introduction to the structure and function of SAT and OASS, along with an overview of existing inhibitors for SAT and OASS as potential antibacterial agents. Our primary focus is on elucidating the inhibitory activities, structure-activity relationships, and mechanisms of action of these inhibitors. Through this exploration, we aim to provide insights into promising strategies and prospects in the development of antibacterial agents that target these essential enzymes.

摘要

传染病一直是威胁公共卫生的一个长期存在的问题。耐药病原体和传染病的日益流行导致有效抗生素的数量减少,这凸显了开发新的抗菌剂的迫切需要。丝氨酸乙酰转移酶(SAT),也称为某些细菌中的 CysE,以及 O-乙酰丝氨酸硫代酶(OASS),也称为某些细菌中的 CysK,是各种致病微生物半胱氨酸生物合成途径中不可缺少的酶。这些酶在病原体的生存中起着至关重要的作用,因此 SAT 和 OASS 成为开发新型抗感染药物的有前途的靶标。在这篇全面的综述中,我们介绍了 SAT 和 OASS 的结构和功能,并概述了现有的 SAT 和 OASS 抑制剂作为潜在的抗菌剂。我们的主要重点是阐明这些抑制剂的抑制活性、构效关系和作用机制。通过这种探索,我们旨在为针对这些必需酶的抗菌剂的开发提供有前途的策略和前景。

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