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Small Molecule KRAS Agonist for Mutant KRAS Cancer Therapy by Xu, Ke; Park, Dongkyoo; Magis, Andrew T.; Zhang, Jun; Zhou, Wei; Sica, Gabriel L.; Ramalingam, Suresh S.; Curran, Walter J.; Deng, Xingming is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.
What is Small Molecule KRAS Agonist for Mutant KRAS Cancer Therapy about?
## Background: Lung cancer patients with kras mutation(s) have a poor prognosis due in part to the development of resistance to currently available therapeutic interventions. development of a new class of anticancer agents that directly targets kras may provide a more attractive option for the treatment of kras-mutant lung cancer. ## Results: Here we identified a small molecule kras agonist, kra-533, that binds the gtp/gdp-binding pocket of kras. in vitro gdp/gtp exchange assay reveals that kra-533 activates kras by preventing the cleavage of gtp into gdp, leading to the accumulation of gtp-kras, an active form of kras. treatment of human lung cancer cells with kra-533 resulted in increased kras activity and suppression of cell growth. lung cancer cell lines with kras mutation were relatively more sensitive to kra-533 than cell lines without kras mutation. mutating one of the hydrogen-bonds among the kra-533 binding amino acids in kras (mutant k117a) resulted in failure of kras to bind kra-533. kra-533 had no effect on the activity of k117a mutant kras, suggesting that kra-533 binding to k117 is required for kra-533 to enhance kras activity. intriguingly, kra-533-mediated kras acti
Who reads Small Molecule KRAS Agonist for Mutant KRAS Cancer Therapy?
It is typically read by researchers, students, and practitioners in Biochemistry, Genetics and Molecular Biology.
- Author
- Xu, Ke; Park, Dongkyoo; Magis, Andrew T.; Zhang, Jun; Zhou, Wei; Sica, Gabriel L.; Ramalingam, Suresh S.; Curran, Walter J.; Deng, Xingming
- Publisher
- BioMed Central; Springer (Biomed Central Ltd.); [London]: BioMed Central, c2002-; Springer Science and Business Media LLC; Society for Mining, Metallurgy and Exploration Inc. (ISSN 1476-4598)
- Published
- 2019
- Language
- EN
- Field
- Biochemistry, Genetics and Molecular Biology (Life Sciences)