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Activation of signaling pathways in models of t(6;9)-acute myeloid leukemia.
Chiriches C, Khan D, Wieske M, Guillen N, Rokicki M, Guy C, Wilson M, Heesom KJ, Ottmann OG, Ruthardt M. Chiriches C, et al. Among authors: ruthardt m. Ann Hematol. 2022 Oct;101(10):2179-2193. doi: 10.1007/s00277-022-04905-9. Epub 2022 Aug 8. Ann Hematol. 2022. PMID: 35941390 Free PMC article.
Crizotinib acts as ABL1 inhibitor combining ATP-binding with allosteric inhibition and is active against native BCR-ABL1 and its resistance and compound mutants BCR-ABL1T315I and BCR-ABL1T315I-E255K.
Mian AA, Haberbosch I, Khamaisie H, Agbarya A, Pietsch L, Eshel E, Najib D, Chiriches C, Ottmann OG, Hantschel O, Biondi RM, Ruthardt M, Mahajna J. Mian AA, et al. Among authors: ruthardt m. Ann Hematol. 2021 Aug;100(8):2023-2029. doi: 10.1007/s00277-020-04357-z. Epub 2021 Jun 10. Ann Hematol. 2021. PMID: 34110462 Free PMC article.
The gatekeeper mutation T315I confers resistance against small molecules by increasing or restoring the ABL-kinase activity accompanied by aberrant transphosphorylation of endogenous BCR, even in loss-of-function mutants of BCR/ABL.
Mian AA, Schüll M, Zhao Z, Oancea C, Hundertmark A, Beissert T, Ottmann OG, Ruthardt M. Mian AA, et al. Among authors: ruthardt m. Leukemia. 2009 Sep;23(9):1614-21. doi: 10.1038/leu.2009.69. Epub 2009 Apr 16. Leukemia. 2009. PMID: 19369965
68 results