Article
Resistance to a tyrosine kinase inhibitor mediated by changes to the conformation space of the kinase.
Physical chemistry chemical physics : PCCP - 22 Feb 2023
Freire Thales Souza, Caracelli Ignez, Zukerman-Schpector Julio, Friedman Ran
Abstract excerpt
Gilteritinib is a highly selective and effective inhibitor of the FLT3/ITD mutated protein, and is used successfully in treating acute myeloid leukaemia (AML). Unfortunately, tumour cells gradually develop resistance to gilteritinib due to mutations in the molecular drug target. The atomistic details behind this observed resistance are not clear, since the protein structure of the complex is only available in the...
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