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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Autores principales: 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
Formato: article
Lenguaje:EN
Publicado: Nature Portfolio 2021
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Acceso en línea:https://doaj.org/article/9fb0e318fb534431a1e30f0ac4d27ca1
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Sumario: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.