Rapid proteasomal degradation of mutant feline McDonough sarcoma-like tyrosine kinase-3 overcomes tyrosine kinase inhibitor resistance of acute myeloid leukemia cells
Melisa Halilovic, Mohamed Abdalla M. Abdelsalam, Andreas O. Mieland, Sarah Neuroth, Ramy Ashry, Joanna Zabkiewicz, Michelle Lazenby, Caroline L. Alvares, Matthias Schmidt, Walburgis Brenner, Sara Najafi, Ina Oehme, Christoph Hieber, Yanira Zeyn, Matthias Bros, , Oliver Holger Krämer
This study develops MA191, a PROTAC degrader of FLT3-ITD, which overcomes resistance in AML cells by rapidly degrading the mutant protein and shows efficacy in vivo.
bioRxiv · Jun 20, 2025 · PreprintPharmacology & Toxicology