Article
Ras-mutant cancers are sensitive to small molecule inhibition of V-type ATPases in mice.
Nature biotechnology - 1 Dec 2022
Tolani Bhairavi, Celli Anna, Yao Yanmin, Tan Yong Zi, Fetter Richard, Liem Christina R, de Smith Adam J, Vasanthakumar Thamiya, Bisignano Paola, Cotton Adam D, Seiple Ian B, Rubinstein John L, Jost Marco, Weissman Jonathan S
Abstract excerpt
Mutations in Ras family proteins are implicated in 33% of human cancers, but direct pharmacological inhibition of Ras mutants remains challenging. As an alternative to direct inhibition, we screened for sensitivities in Ras-mutant cells and discovered 249C as a Ras-mutant selective cytotoxic agent with nanomolar potency against a spectrum of Ras-mutant cancers. 249C binds to vacuolar (V)-ATPase with nanomolar...
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