低温电子显微镜在药物设计中的快速发展作用

Q1 Pharmacology, Toxicology and Pharmaceutics

Drug Discovery Today: Technologies Pub Date : 2020-12-01 DOI:10.1016/j.ddtec.2020.12.003

Christoph Wigge, Aleksandar Stefanovic, Mazdak Radjainia

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引用次数: 17

摘要

自2010年初以来，冷冻电子显微镜(cryo-EM)已经发展成为主流的结构生物学方法，被称为“分辨率革命”。制药公司也开始在药物发现中使用低温电镜，越来越多的行业出版物证明了这一点。迄今为止，在分辨率，吞吐量和可获得的分子量方面受到限制，通过新一波的技术进步，低温电子显微镜正在迅速克服其主要限制，以便更广泛地使用。这篇综述讨论了冷冻电镜如何影响药物发现，以及最先进的技术如何准备进一步革新其应用于以前棘手的蛋白质以及新的用例。

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The rapidly evolving role of cryo-EM in drug design

Since the early 2010s, cryo-electron microscopy (cryo-EM) has evolved to a mainstream structural biology method in what has been dubbed the “resolution revolution”. Pharma companies also began to use cryo-EM in drug discovery, evidenced by a growing number of industry publications. Hitherto limited in resolution, throughput and attainable molecular weight, cryo-EM is rapidly overcoming its main limitations for more widespread use through a new wave of technological advances. This review discusses how cryo-EM has already impacted drug discovery, and how the state-of-the-art is poised to further revolutionize its application to previously intractable proteins as well as new use cases.

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来源期刊

Drug Discovery Today: Technologies Pharmacology, Toxicology and Pharmaceutics-Drug Discovery

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期刊介绍： Discovery Today: Technologies compares different technological tools and techniques used from the discovery of new drug targets through to the launch of new medicines.