{"title":"Microcrystal electron diffraction in macromolecular and pharmaceutical structure determination","authors":"Max T.B. Clabbers , Hongyi Xu","doi":"10.1016/j.ddtec.2020.12.002","DOIUrl":null,"url":null,"abstract":"<div><p>Microcrystal electron diffraction (MicroED) has recently shown to be a promising technique for structure determination in structural biology and pharmaceutical chemistry. Here, we discuss the unique properties of electrons and motivate its use for diffraction experiments. We review the latest developments in MicroED, and illustrate its applications in macromolecular crystallography, fragment screening and structure guided drug discovery. We discuss the perspectives of MicroED in synthetic chemistry and pharmaceutical development. We anticipate that the rapid advances MicroED showcased here will promote further development of electron crystallography and open up new opportunities for drug discovery.</p></div>","PeriodicalId":36012,"journal":{"name":"Drug Discovery Today: Technologies","volume":"37 ","pages":"Pages 93-105"},"PeriodicalIF":0.0000,"publicationDate":"2020-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.ddtec.2020.12.002","citationCount":"9","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Drug Discovery Today: Technologies","FirstCategoryId":"1085","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S1740674920300354","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"Pharmacology, Toxicology and Pharmaceutics","Score":null,"Total":0}
引用次数: 9
Abstract
Microcrystal electron diffraction (MicroED) has recently shown to be a promising technique for structure determination in structural biology and pharmaceutical chemistry. Here, we discuss the unique properties of electrons and motivate its use for diffraction experiments. We review the latest developments in MicroED, and illustrate its applications in macromolecular crystallography, fragment screening and structure guided drug discovery. We discuss the perspectives of MicroED in synthetic chemistry and pharmaceutical development. We anticipate that the rapid advances MicroED showcased here will promote further development of electron crystallography and open up new opportunities for drug discovery.
微晶电子衍射(Microcrystal electron diffraction, MicroED)是近年来在结构生物学和药物化学等领域研究结构的一种很有前途的技术。在这里,我们讨论了电子的独特性质,并激发了它在衍射实验中的应用。本文综述了MicroED的最新进展,并阐述了其在大分子晶体学、片段筛选和结构导向药物发现等方面的应用。我们讨论了MicroED在合成化学和药物开发方面的前景。我们期待MicroED在这里展示的快速发展将促进电子晶体学的进一步发展,并为药物发现开辟新的机会。
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.