脂肪酸生物合成:KAS抑制剂的最新进展。

Q3 Pharmacology, Toxicology and Pharmaceutics Current drug discovery technologies Pub Date : 2022-01-01 DOI:10.2174/1570163819666220111113032
Rani Shinde, Vasanti Suvarna
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引用次数: 1

摘要

自20世纪初以来,随着青霉素和链霉素在20世纪40年代的分离,现代抗感染药物的开发获得了动力。由于早期药物发现的巨大成功,许多传染病被成功地预防和根除。然而,这种最初的希望是错误的,病原体演变成对人类健康的重大威胁。耐药性的产生是自然选择的无情压力的结果,需要确定新的药物靶点,并创造绕过现有耐药机制的化疗药物。脂肪酸生物合成是细菌生长发育过程中重要的代谢机制。参与这一生物合成途径的几个关键酶已被确定为新型抗菌剂的潜在靶点。在大肠杆菌中,这一途径已被广泛研究。现就Kas A、Kas B和Fab H抑制剂作为单药抗生素的研究进展作一综述。
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Fatty Acid Biosynthesis: An Updated Review on KAS Inhibitors.

Since the early twentieth century, with the isolation of penicillin and streptomycin in the 1940s, the modern era of anti-infective drug development has gained momentum. Due to the enormous success of early drug discovery, many infectious diseases were successfully prevented and eradicated. However, this initial hope was wrongheaded, and pathogens evolved as a significant threat to human health. Drug resistance develops as a result of natural selection's relentless pressure, necessitating the identification of new drug targets and the creation of chemotherapeutics that bypass existing drug resistance mechanisms. Fatty acid biosynthesis (FAS) is a crucial metabolic mechanism for bacteria during their growth and development. Several crucial enzymes involved in this biosynthetic pathway have been identified as potential targets for new antibacterial agents. In Escherichia coli (E. coli), this pathway has been extensively investigated. The present review focuses on progress in the development of Kas A, Kas B, and Fab H inhibitors as mono-therapeutic antibiotics.

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来源期刊
Current drug discovery technologies
Current drug discovery technologies Pharmacology, Toxicology and Pharmaceutics-Drug Discovery
CiteScore
3.70
自引率
0.00%
发文量
48
期刊介绍: Due to the plethora of new approaches being used in modern drug discovery by the pharmaceutical industry, Current Drug Discovery Technologies has been established to provide comprehensive overviews of all the major modern techniques and technologies used in drug design and discovery. The journal is the forum for publishing both original research papers and reviews describing novel approaches and cutting edge technologies used in all stages of drug discovery. The journal addresses the multidimensional challenges of drug discovery science including integration issues of the drug discovery process.
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