背景:大环内酯类药物通过阻止蛋白质生物合成过程中多肽的伸长来抑制细菌细胞的生长,包括天然的,合成,和半合成产品。这是通过阻断多肽链的通过而发生的,因为大环内酯类在新生的肽出口通道处结合。
目的:最近通过ribo-seq进行核糖体谱分析的数据进一步证明,除了阻断多肽链,大环内酯类也能影响单个蛋白质的合成。因此,这表明大环内酯类的作用方式比我们最初想象的要复杂得多。自从1950年代发现大环内酯类药物以来,它们已被广泛用于兽医,农业,和医学。由于滥用和过度使用抗生素;细菌已获得对它们的抗性。因此,充分了解大环内酯类药物的作用方式以及对大环内酯类药物的耐药机制,以减轻抗生素耐药性问题,对我们来说至关重要。
背景:随着对大环内酯类作用方式的更好理解,可以进行化学修饰以提高其效力。此外,由于新的发现挑战了已经存在的理论-由于这种模糊不清,对大环内酯类作用模式的完整详细理解仍然含糊不清,对大环内酯类药物作用方式的研究一直持续到今天。
结论:在这篇综述中,我们概述了大环内酯类抗生素,重点介绍了有关大环内酯类抗生素的作用方式和细菌对大环内酯类抗生素的耐药机制的最新知识。
BACKGROUND: Macrolides inhibit the growth of bacterial cells by preventing the elongation of polypeptides during protein biosynthesis and includes natural, synthetic, and semisynthetic products. This occurs by blocking the passage of the polypeptide chain as macrolides bind at the nascent peptide exit tunnel.
OBJECTIVE: Recent data of ribosome profiling via ribo-seq further proves that other than blocking the polypeptide chain, macrolides are also able to affect the synthesis of individual proteins. Thus, this shows that the mode of action of macrolides is more complex than we initially thought. Since the discovery of macrolides in the 1950s, they have been widely used in veterinary, agriculture, and medicine. Due to misuse and overuse of antibiotics; bacteria have acquired resistance against them. Hence, it is of utmost importance for us to fully understand the mode of action of macrolides as well as the mechanism of resistance against macrolides to mitigate the antibiotic resistance issues.
BACKGROUND: With a better understanding on the mode of actions of macrolides, chemical modifications can be performed to improve its potency. Furthermore, the complete detailed understanding of the mode of action of macrolides remained vague as new findings challenged the theory that was already in existence - due to this obscurity, research into macrolides\' mode of action continues up to this day.
CONCLUSIONS: In this review, we present an overview of macrolide antibiotics with the emphasis on the latest knowledge regarding the mode of action of macrolides and mechanism of resistance employed in bacteria against macrolides.