Article
Selective degradation of mutant FMS-like tyrosine kinase-3 requires BIM-dependent depletion of heat shock proteins.
Leukemia - 1 Dec 2024
Halilovic Melisa, Abdelsalam Mohamed, Zabkiewicz Joanna, Lazenby Michelle, Alvares Caroline, Schmidt Matthias, Brenner Walburgis, Najafi Sara, Oehme Ina, Hieber Christoph, Zeyn Yanira, Bros Matthias, Sippl Wolfgang, Krämer Oliver H
Abstract excerpt
Internal tandem duplications in the FMS-like tyrosine kinase-3 (FLT3-ITD) are common mutations in acute myeloid leukemia (AML). Proteolysis-targeting chimeras (PROTACs) that induce proteasomal degradation of mutated FLT3 emerge as innovative pharmacological approach. Molecular mechanisms that control targeted proteolysis beyond the ubiquitin-proteasome-system are undefined and PROTACs are the only known type of...
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