Home > Haematology > Inhibiting the LSD1 enzyme renders some leukemia cells sensitive to TKI treatment

Inhibiting the LSD1 enzyme renders some leukemia cells sensitive to TKI treatment


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Journal
Science Signaling
Reuters Health -  25/04/2022 - A laboratory study suggests that inhibition of LSD1 (lysine-specific demethylase) renders some patient-derived acute myeloid leukemia (AML) cells sensitive to the MEK inhibitor trametinib. Typically, AML is resistant to tyrosine kinase inhibitors such trametinib. "We know that resistance often happens because there are several biochemical pathways in cancer cells that can compensate for the inhibition of a given kinase," Dr. Pedro Cutillas of Queen Mary University of London, UK, told Reuters Health by email. "We wanted to use this knowledge to identify ways to remodel the biology of cancer so that previously resistant cancer cells could become sensitive to treatment." The team found that LSD1 inhibitors increase the activity of MEK, which is trametinib's target, "while dampening compensatory pathways," he explained. "Thus, cancer cells can no longer compensate for MEK inhibition and die when treated with the LSD1 inhibitor follo...


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