Fig. 3: Treatment with LSD1 inhibitor (LSD1i) disrupts binding of LSD1 to CoREST and GFI1, attenuates colony growth, and induces differentiation in AML cells.
From: Superior efficacy of co-targeting GFI1/KDM1A and BRD4 against AML and post-MPN secondary AML cells
A–C Immunoprecipitation and immunoblot analysis of OCI-AML5, THP1, and SET-2 cells treated with INCB059872 for 16 h. D Reduced binding of LSD1 and GFI1 (determined by sandwich ELISA assay) following 16 h of treatment with INCB059872. Mean of two independent experiments performed in duplicate + S.D. *p < 0.05, ***p < 0.005 (determined by a two-tailed, unpaired t-test). E, F OCI-AML5, OCI-AML2, THP1, SET-2, and HEL92.1.7 cells were treated with the indicated concentrations of INCB059872 for 96 h. Then, cells were plated in Methocult media and incubated at 37 °C. Colony growth was assessed after 7–10 days. Mean of two independent experiments + S.D. G, H The % of CD86 and/or CD11b-positive OCI-AML5, SET2 and HEL92.1.7 cells was determined by flow cytometry following treatment with INCB059872 for 96 h. Mean of three experiments + S.E.M. ***p < 0.005 in INCB059872-treated cells compared to untreated cells (determined by a two-tailed, unpaired t-test in GraphPad V8).
