Figure 5: Inhibition of HDAC1:MTA1 by a novel peptide-based inhibitor.
From: Insights into the activation mechanism of class I HDAC complexes by inositol phosphates
(a) Inhibition curve of HDAC1:MTA1 by the histone H4 peptide H4K16Hx. (b)The position of H4K16Hx (pink) bound to the active site of HDAC1 (purple). The sidechain of HDAC1 residue D99 undergoes a significant rearrangement (indicated by arrow) to coordinate binding of the peptide (apo-HDAC1 shown in grey). (c) The D99A HDAC1 mutant does not show deacetylase activity and activity is not rescued on addition of InsP6. HDAC assays were performed using an electrophoretic mobility shift assay on the caliper platform. Error bars indicate±s.e.m. (n=3).
