Literature DB >> 34281791

Drug discovery in the era of cryo-electron microscopy.

Michael J Robertson1, Justin G Meyerowitz2, Georgios Skiniotis3.   

Abstract

Structure-based drug discovery (SBDD) is an indispensable approach for the design and optimization of new therapeutic agents. Here, we highlight the rapid progress that has turned cryo-electron microscopy (cryoEM) into an exceptional SBDD tool, and the wealth of new structural information it is providing for high-value pharmacological targets. We review key advantages of a technique that directly images vitrified biomolecules without the need for crystallization; both in terms of a broader array of systems that can be studied and the different forms of information it can provide, including heterogeneity and dynamics. We discuss near- and far-future developments, working in concert towards achieving the resolution and throughput necessary for cryoEM to make a widespread impact on the SBDD pipeline.
Copyright © 2021 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  biologics; cryo-electron microscopy; pharmacology; single-particle analysis; small molecule; structure-based drug discovery

Mesh:

Year:  2021        PMID: 34281791      PMCID: PMC8760134          DOI: 10.1016/j.tibs.2021.06.008

Source DB:  PubMed          Journal:  Trends Biochem Sci        ISSN: 0968-0004            Impact factor:   13.807


  61 in total

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