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Article

Identification of the nucleotide-free state as a therapeutic vulnerability for inhibition of selected oncogenic RAS mutants.

Cell reports - 8 Feb 2022

Khan Imran, Koide Akiko, Zuberi Mariyam, Ketavarapu Gayatri, Denbaum Eric, Teng Kai Wen, Rhett J Matthew, Spencer-Smith Russell, Hobbs G Aaron, Camp Ernest Ramsay, Koide Shohei, O'Bryan John P

Abstract excerpt

RAS guanosine triphosphatases (GTPases) are mutated in nearly 20% of human tumors, making them an attractive therapeutic target. Following our discovery that nucleotide-free RAS (apo RAS) regulates cell signaling, we selectively target this state as an approach to inhibit RAS function. Here, we describe the R15 monobody that exclusively binds the apo state of all three RAS isoforms in vitro, regardless of the...

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Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

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Identifiers

PMID: 35139380
DOI: 10.1016/j.celrep.2022.110322
PMCID: PMC8936000

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