RAS-inhibiting biologics identify and probe druggable pockets including an SII-α3 allosteric site

RAS-inhibiting biologics identify and probe druggable pockets including an SII-α3 allosteric site

Oncogenic RAS mutants remain difficult to target with small molecules. Here, the authors show that RAS-binding Affimer proteins inhibit RAS signaling while binding diverse regions on the RAS surface, suggesting the potential to use Affimers as tools to identify new binding pockets and pharmacophores...

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Bibliographic Details
Main Authors: Katarzyna Z. Haza, Heather L. Martin, Ajinkya Rao, Amy L. Turner, Sophie E. Saunders, Britta Petersen, Christian Tiede, Kevin Tipping, Anna A. Tang, Modupe Ajayi, Thomas Taylor, Maia Harvey, Keri M. Fishwick, Thomas L. Adams, Thembaninkosi G. Gaule, Chi H. Trinh, Matthew Johnson, Alexander L. Breeze, Thomas A. Edwards, Michael J. McPherson, Darren C. Tomlinson
Format: Article
Language:English
Published: Nature Portfolio 2021-06-01
Series:Nature Communications
Online Access:https://doi.org/10.1038/s41467-021-24316-0
Description
Summary:Oncogenic RAS mutants remain difficult to target with small molecules. Here, the authors show that RAS-binding Affimer proteins inhibit RAS signaling while binding diverse regions on the RAS surface, suggesting the potential to use Affimers as tools to identify new binding pockets and pharmacophores.
ISSN:2041-1723

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