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Cryo-EM as a powerful tool for drug discovery.

Authors
  • Van Drie, John H1
  • Tong, Liang2
  • 1 Van Drie Research LLC, 109 Millpond, North Andover, MA 01845, USA. Electronic address: [email protected]
  • 2 Department of Biological Sciences, Columbia University, New York, NY 10027, USA. Electronic address: [email protected]
Type
Published Article
Journal
Bioorganic & medicinal chemistry letters
Publication Date
Nov 15, 2020
Volume
30
Issue
22
Pages
127524–127524
Identifiers
DOI: 10.1016/j.bmcl.2020.127524
PMID: 32890683
Source
Medline
Keywords
Language
English
License
Unknown

Abstract

The recent revolution in cryo-EM has produced an explosion of structures at near-atomic or better resolution. This has allowed cryo-EM structures to provide visualization of bound small-molecule ligands in the macromolecules, and these new structures have provided unprecedented insights into the molecular mechanisms of complex biochemical processes. They have also had a profound impact on drug discovery, defining the binding modes and mechanisms of action of well-known drugs as well as driving the design and development of new compounds. This review will summarize and highlight some of these structures. Most excitingly, the latest cryo-EM technology has produced structures at 1.2 Å resolution, further solidifying cryo-EM as a powerful tool for drug discovery. Therefore, cryo-EM will play an ever-increasing role in drug discovery in the coming years. Copyright © 2020 Elsevier Ltd. All rights reserved.

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