Article
Targeting KRAS-dependent tumors with AZD4785, a high-affinity therapeutic antisense oligonucleotide inhibitor of KRAS.
Science translational medicine - 14 Jun 2017
Ross Sarah J, Revenko Alexey S, Hanson Lyndsey L, Ellston Rebecca, Staniszewska Anna, Whalley Nicky, Pandey Sanjay K, Revill Mitchell, Rooney Claire, Buckett Linda K, Klein Stephanie K, Hudson Kevin, Monia Brett P, Zinda Michael, Blakey David C, Lyne Paul D, Macleod A Robert
Abstract excerpt
Activating mutations in KRAS underlie the pathogenesis of up to 20% of human tumors, and KRAS is one of the most frequently mutated genes in cancer. Developing therapeutics to block KRAS activity has proven difficult, and no direct inhibitor of KRAS function has entered clinical trials. We describe the preclinical evaluation of AZD4785, a high-affinity constrained ethyl-containing therapeutic antisense...
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