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Maxamycins: Durable Antibiotics Derived by Rational Redesign of Vancomycin
Accounts of Chemical Research ( IF 18.3 ) Pub Date : 2020-11-02 , DOI: 10.1021/acs.accounts.0c00569
Zhi-Chen Wu 1 , Dale L Boger 1
Affiliation  

Since its discovery, vancomycin has been used in the clinic for >60 years. Because of their durability, vancomycin and related glycopeptides serve as the antibiotics of last resort for the treatment of protracted bacterial infections of resistant Gram-positive pathogens, including methicillin-resistant Staphylococcus aureus (MRSA) and multidrug-resistant (MDR) Streptococcus pneumoniae. After 30 years of use, vancomycin resistance was first observed and is now widespread in enterococci and more recently in S. aureus. The widespread prevalence of vancomycin-resistant enterococci (VRE) and the emergence of vancomycin-resistant S. aureus (VRSA) represent a call to focus on the challenge of resistance, highlight the need for new therapeutics, and provide the inspiration for the design of more durable antibiotics less prone to bacterial resistance than even vancomycin.

中文翻译:

Maxamycins:万古霉素的合理重新设计衍生的耐用抗生素

自发现以来,万古霉素已用于临床超过 60 年。由于其耐用性,万古霉素和相关糖肽可作为治疗耐药革兰氏阳性病原体长期细菌感染的最后手段,包括耐甲氧西林金黄色葡萄球菌(MRSA) 和耐多药 (MDR)肺炎链球菌。使用 30 年后,首次观察到万古霉素耐药性,现在广泛存在于肠球菌和最近的金黄色葡萄球菌中。耐万古霉素肠球菌 (VRE) 的普遍流行和耐万古霉素的金黄色葡萄球菌的出现 (VRSA) 代表呼吁关注耐药性挑战,强调对新疗法的需求,并为设计更耐用的抗生素提供灵感,该抗生素甚至比万古霉素更不容易产生细菌耐药性。
更新日期:2020-11-17
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