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Prospects for antimicrobial development in the cryo-EM era - a focus on the ribosome.
FEMS Microbiology Reviews ( IF 10.1 ) Pub Date : 2020-07-27 , DOI: 10.1093/femsre/fuaa032
Alba Herrero Del Valle 1 , C Axel Innis 1
Affiliation  

Resistance to antimicrobial drugs used to treat bacterial, viral, fungal and parasitic infections is a major health concern requiring a coordinated response across the globe. An important aspect in the fight against antimicrobial resistance is the development of novel drugs that are effective against resistant pathogens. Drug development is a complex trans-disciplinary endeavor, in which structural biology plays a major role by providing detailed functional and mechanistic information on an antimicrobial target and its interactions with small molecule inhibitors. Although X-ray crystallography and nuclear magnetic resonance have until now been the methods of choice to characterize microbial targets and drive structure-based drug development, cryo-electron microscopy is rapidly gaining ground in these areas. In this perspective, we will discuss how cryo-electron microscopy is changing our understanding of an established antimicrobial target, the ribosome, and how methodological developments could help this technique become an integral part of the antimicrobial drug discovery pipeline.

中文翻译:

冷冻电镜时代抗菌剂发展的前景——关注核糖体。

对用于治疗细菌、病毒、真菌和寄生虫感染的抗菌药物的耐药性是一个主要的健康问题,需要在全球范围内采取协调一致的应对措施。抗击抗菌素耐药性的一个重要方面是开发对耐药病原体有效的新型药物。药物开发是一项复杂的跨学科工作,其中结构生物学通过提供有关抗菌靶标及其与小分子抑制剂相互作用的详细功能和机制信息而发挥重要作用。尽管迄今为止,X 射线晶体学和核磁共振一直是表征微生物目标和推动基于结构的药物开发的首选方法,但冷冻电子显微镜在这些领域正在迅速取得进展。从这个角度来看,
更新日期:2020-07-27
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