Figure 8.
Summary of dose-dependent activation of mutant HDAC8 activity by TM251. Data for the P91L, H180R, D233G, G117E, and G304 mutants are recorded in Table 3; data for the C153F, A188T, I243N, T311M, and H334R mutants are reported by Decroos and colleagues.34 The activity level for wild-type HDAC8 in the absence of activator is indicated by a dashed line. Catalytic activity for several mutants can be restored to wild-type level or better by TM251, and all but two mutants (H180R and G304R) exhibit at least some activation by TM251.