| Literature DB >> 34281791 |
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.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