The rapidly evolving role of cryo-EM in drug design

Drug Discov Today Technol. 2020 Dec:38:91-102. doi: 10.1016/j.ddtec.2020.12.003. Epub 2021 Jan 11.


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.

Keywords: Cryo-EM SBDD; Drug discovery; Epitope mapping; Lead optimization; Protein structure.

Publication types

  • Review

MeSH terms

  • Cryoelectron Microscopy
  • Drug Design*
  • Drug Discovery*
  • Proteins


  • Proteins