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Article

Mutation-oriented profiling of autoinhibitory kinase conformations predicts RAF inhibitor efficacies.

Proceedings of the National Academy of Sciences of the United States of America - 8 Dec 2020

Mayrhofer Johanna E, Enzler Florian, Feichtner Andreas, Röck Ruth, Fleischmann Jakob, Raffeiner Andrea, Tschaikner Philipp, Ogris Egon, Huber Roland G, Hartl Markus, Schneider Rainer, Troppmair Jakob, Torres-Quesada Omar, Stefan Eduard

Abstract excerpt

Kinase-targeted therapies have the potential to improve the survival of patients with cancer. However, the cancer-specific spectrum of kinase alterations exhibits distinct functional properties and requires mutation-oriented drug treatments. Besides post-translational modifications and diverse intermolecular interactions of kinases, it is the distinct disease mutation which reshapes full-length kinase...

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PMID: 33229534
DOI: 10.1073/pnas.2012150117
PMCID: PMC7733820

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