Scientists discover a new type of leukemia inhibitor

Liu Qingsong's pharmaceutical team from the Institute of Health and Medical Technology, Hefei Institute of Material Science, Chinese Academy of Sciences recently discovered a new type of inhibitor, which is of great significance for the treatment of positive acute myeloid leukemia caused by mutations in the FLT3-ITD gene
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The results were published online in "Signal Transduction and Targeted Therapy" a few days ago

In acute myeloid leukemia, about a quarter of patients carry FLT3-ITD gene mutations, which cause FLT3 kinase activation, which in turn leads to abnormal proliferation of leukemia cells.
Therefore, the use of FLT3 kinase inhibitors can effectively inhibit tumors.
Curative effect
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However, long-term use of FLT3 kinase inhibitors can lead to resistance mutations in the FLT3 gene, which in turn leads to resistance to FLT3 inhibitors

Liu Qingsong’s team found in the research that compound QL47 has strong anti-proliferative activity against FLT3-ITD mutation-positive acute myeloid leukemia cell lines and can degrade FLT3-ITD protein
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QL47 irreversibly binds to the heat shock protein HSP70 and inhibits the HSP70 auxiliary protein folding function, which in turn leads to the degradation of FLT3-ITD and inhibits the activation of the FLT3 signaling pathway

The efficacy evaluation results on primary patient cells and animal tumor models show that the inhibitor QL47 can effectively induce the degradation of FLT3-ITD protein and the occurrence of apoptosis in primary patient cells; in the cellular mouse orthotopic tumor model, Can effectively extend the survival time of animals

Related paper information: https://doi.