Extended Data Fig. 2: DNMT1 residues important for compound binding and inhibition. | Nature Cancer

Extended Data Fig. 2: DNMT1 residues important for compound binding and inhibition.

From: Discovery of a first-in-class reversible DNMT1-selective inhibitor with improved tolerability and efficacy in acute myeloid leukemia

Extended Data Fig. 2

a, Analogues containing a photoreactive benzophenone or diazerine moiety. b, c, Murine DNMT1 (731-1602) spectra in the absence or presence of a 45-minute photolysis step with 14-mer hemi-methylated DNA and GSK3844831 (b) or GSK3901839 (c). d, Dose response curves for HEK293 cells expressing either wild-type or site-directed alanine mutant DNMT1 (n = 2; technical replicates) treated for 6 days with decitabine or GSK3685032. Dashed line represents starting cell number (T0). e, Dose response curves (n = 4 biologically independent samples; average ± s.d.) for full-length wild-type or H1507Y DNMT1 activity in a radioactive SPA assay.

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