Fig. 4

MAKV-8 derivatives display lower potency than their parent compound. (a) Docking poses of MAKV-8 derivatives (stick model) on HDAC6 crystal structure (white; PDB code: 5EDU). Numbered residues forming hydrophobic interactions in the binding sites (stick representation) are indicated. Zinc atom is shown as a purple sphere; nitrogen and oxygen are colored in blue and red, respectively. (b) Histone H4 and α-tubulin acetylation levels were assessed by western blot (upper panel), and cell proliferation and viability were evaluated (lower panel) following treatments of K-562 cells with increasing concentrations of the indicated MAKV-8 derivatives for 24h and up to 72h, respectively. β-actin and histone H1 served as loading controls for α-tubulin and histone H4, respectively. Blots are representative of three independent experiments. SAHA was used as a reference HDACi