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
Materias:	Science Q
Acceso en línea:	https://doaj.org/article/9fb0e318fb534431a1e30f0ac4d27ca1
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spelling	oai:doaj.org-article:9fb0e318fb534431a1e30f0ac4d27ca12021-12-02T14:34:12ZRAS-inhibiting biologics identify and probe druggable pockets including an SII-α3 allosteric site10.1038/s41467-021-24316-02041-1723https://doaj.org/article/9fb0e318fb534431a1e30f0ac4d27ca12021-06-01T00:00:00Zhttps://doi.org/10.1038/s41467-021-24316-0https://doaj.org/toc/2041-1723Oncogenic 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.Katarzyna Z. HazaHeather L. MartinAjinkya RaoAmy L. TurnerSophie E. SaundersBritta PetersenChristian TiedeKevin TippingAnna A. TangModupe AjayiThomas TaylorMaia HarveyKeri M. FishwickThomas L. AdamsThembaninkosi G. GauleChi H. TrinhMatthew JohnsonAlexander L. BreezeThomas A. EdwardsMichael J. McPhersonDarren C. TomlinsonNature PortfolioarticleScienceQENNature Communications, Vol 12, Iss 1, Pp 1-15 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	Science Q
spellingShingle	Science Q 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 RAS-inhibiting biologics identify and probe druggable pockets including an SII-α3 allosteric site
description	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.
format	article
author	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
author_facet	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
author_sort	Katarzyna Z. Haza
title	RAS-inhibiting biologics identify and probe druggable pockets including an SII-α3 allosteric site
title_short	RAS-inhibiting biologics identify and probe druggable pockets including an SII-α3 allosteric site
title_full	RAS-inhibiting biologics identify and probe druggable pockets including an SII-α3 allosteric site
title_fullStr	RAS-inhibiting biologics identify and probe druggable pockets including an SII-α3 allosteric site
title_full_unstemmed	RAS-inhibiting biologics identify and probe druggable pockets including an SII-α3 allosteric site
title_sort	ras-inhibiting biologics identify and probe druggable pockets including an sii-α3 allosteric site
publisher	Nature Portfolio
publishDate	2021
url	https://doaj.org/article/9fb0e318fb534431a1e30f0ac4d27ca1
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RAS-inhibiting biologics identify and probe druggable pockets including an SII-α3 allosteric site

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