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由于药物滥用等原因造成的耐药性和结核病在世界范围的卷土重来,迫切需要开发新的抗菌药物和靶标。近年来,细菌脂肪酸合成酶系统的单功能酶已成为基因组驱动的新型抗菌药物靶标研究的热点。β-酮酰-ACP缩合酶Ⅲ(KASⅢ,FabH)是催化脂肪酸合成碳链延长循环的起始因子,广泛存在于细菌中,在细菌脂肪酸生物合成中起着必要和调节的作用。FabH抑制剂由于其作用靶点与现有抗菌药物不同,有希望成为克服细菌耐药性的一种途径,也将成为今后研究的一个热点。本文综述了抗菌药物新靶标KASⅢ及其抑制剂的研究进展。
Due to the drug resistance and the worldwide resurgence of TB caused by drug abuse, there is an urgent need to develop new antimicrobial drugs and targets. In recent years, monofunctional enzymes of the bacterial fatty acid synthase system have become hot spots for genome-driven research of novel antimicrobial drug targets. Beta-ketoacyl-ACP synthase III (KASIII, FabH) is a catalytic factor that catalyzes the elongation cycle of fatty acid synthesis of carbon chain. It exists widely in bacteria and plays a necessary and regulatory role in bacterial fatty acid biosynthesis. FabH inhibitors are different from the existing antibacterial drugs because of their target of action. Hopefully, FabH inhibitors will become a way to overcome bacterial resistance and become a hot spot in the future. This review summarizes the research progress of KASⅢand its inhibitors, which is a new target of antibacterials.