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

Nat Commun. 2021-06; 
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
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Gene Synthesis NRAS gene sequences (residues 1–166, with an N-terminal His-tag and C-terminal BAP-tag, were synthesized by GenScript (Piscataway, USA) Get A Quote

摘要

RAS mutations are the most common oncogenic drivers across human cancers, but there remains a paucity of clinically-validated pharmacological inhibitors of RAS, as druggable pockets have proven difficult to identify. Here, we identify two RAS-binding Affimer proteins, K3 and K6, that inhibit nucleotide exchange and downstream signaling pathways with distinct isoform and mutant profiles. Affimer K6 binds in the SI/SII pocket, whilst Affimer K3 is a non-covalent inhibitor of the SII region that reveals a conformer of wild-type RAS with a large, druggable SII/α3 pocket. Competitive NanoBRET between the RAS-binding Affimers and known RAS binding small-molecules demonstrates the potential to use Affimers as tools t... More

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