Nat Chem. Biol.
Sensitivity and engineered resistance of myeloid leukemia cells to BRD9 inhibition.
Hohmann, A.F., Martin, L.J., Minder, J.L., Roe, J.S., Shi, J., Steurer, S., Bader, G., McConnell, D., Pearson, M., Gerstberger, T., Gottschamel, T., Thompson, D., Suzuki, Y., Koegl, M. and Vakoc, C.R.
Notes: The BRD9 subunit of the SWI-SNF chromatin-remodeling complex is investigated in the context of aberrant cell proliferation in acute myeloid leukemia. Specifically, the NanoBRET system was used to measure the interactions of BRD9 and Histone H3.3. A small molecule inhibitor of the BRB9 bromodomain function, BI-7273, was further assessed in HEK293T cells. Disruption of BRB9 interaction with Histone H3.3 was confirmed at sub-micromolar concentrations of BI-7273. Cell viability in the presence of inhibitor was determined using the CellTiter-Glo System. (5079)
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