Article
Identification of a highly efficient dual type I/II FMS-like tyrosine kinase inhibitor that disrupts the growth of leukemic cells.
Cell chemical biology - 17 Mar 2022
Beyer Mandy, Henninger Sven J, Haehnel Patricia S, Mustafa Al-Hassan M, Gurdal Ece, Schubert Bastian, Christmann Markus, Sellmer Andreas, Mahboobi Siavosh, Drube Sebastian, Sippl Wolfgang, Kindler Thomas, Krämer Oliver H
Abstract excerpt
Internal tandem duplications (ITDs) in the FMS-like tyrosine kinase-3 (FLT3) are causally linked to acute myeloid leukemia (AML) with poor prognosis. Available FLT3 inhibitors (FLT3i) preferentially target inactive or active conformations of FLT3. Moreover, they co-target kinases for normal hematopoiesis, are vulnerable to therapy-associated tyrosine kinase domain (TKD) FLT3 mutants, or lack low nanomolar...
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