Literature DB >> 34895645

The rapidly evolving role of cryo-EM in drug design.

Christoph Wigge1, Aleksandar Stefanovic1, Mazdak Radjainia2.   

Abstract

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.
Copyright © 2020 Elsevier Ltd. All rights reserved.

Entities:  

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

Mesh:

Substances:

Year:  2021        PMID: 34895645     DOI: 10.1016/j.ddtec.2020.12.003

Source DB:  PubMed          Journal:  Drug Discov Today Technol        ISSN: 1740-6749


  7 in total

1.  Beyond the Backbone: The Next Generation of Pathwalking Utilities for Model Building in CryoEM Density Maps.

Authors:  Corey F Hryc; Matthew L Baker
Journal:  Biomolecules       Date:  2022-06-02

2.  AlphaFold2 and CryoEM: Revisiting CryoEM modeling in near-atomic resolution density maps.

Authors:  Corey F Hryc; Matthew L Baker
Journal:  iScience       Date:  2022-05-30

3.  On the reduction in the effects of radiation damage to two-dimensional crystals of organic and biological molecules at liquid-helium temperature.

Authors:  Katerina Naydenova; Akiko Kamegawa; Mathew J Peet; Richard Henderson; Yoshinori Fujiyoshi; Christopher J Russo
Journal:  Ultramicroscopy       Date:  2022-03-19       Impact factor: 2.994

4.  Editorial: Tailored Modulation of Interactions Between Biomolecules: Fundamentals and Applications.

Authors:  Matteo Ardini; Paola Baiocco; Adele Di Matteo; Giorgio Giardina; Adriana Erica Miele
Journal:  Front Mol Biosci       Date:  2022-07-14

Review 5.  Targeting Amyloid Fibrils by Passive Immunotherapy in Systemic Amyloidosis.

Authors:  Mario Nuvolone; Alice Nevone; Giampaolo Merlini
Journal:  BioDrugs       Date:  2022-09-12       Impact factor: 7.744

Review 6.  Putting on molecular weight: Enabling cryo-EM structure determination of sub-100-kDa proteins.

Authors:  Koen Wentinck; Christos Gogou; Dimphna H Meijer
Journal:  Curr Res Struct Biol       Date:  2022-10-02

7.  Cryo-EM structure-based selection of computed ligand poses enables design of MTA-synergic PRMT5 inhibitors of better potency.

Authors:  Wei Zhou; Gaya P Yadav; Xiaozhi Yang; Feng Qin; Chenglong Li; Qiu-Xing Jiang
Journal:  Commun Biol       Date:  2022-10-03
  7 in total

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