Inhibition of Nek2 by Small Molecules Affects Proteasome Activity
Figure 4
Novel Nek2 inhibitors effectively decrease the proteasome activity in vitro for multiple cancer cell lines. (a) Nek2 was found to be involved in the 26S proteasome in cancer cell lines. The 26S proteasome was isolated by ultracentrifugation and the presence of Nek2 in the 26S proteasome was determined by Western blot. (b), (c), (d), and (e), Incubation of HCI-2184 and HCI-2389 significantly inhibits the proteasome activity for HeLa cells (b), H929 cells (c), KMS28PE cells (d), and ARP1 cells (e). (e) The irreversible Nek2 inhibitor HCI-2389 worked better than HCI-2184 in decreasing the proteasome activity for ARP1 cells that are resistant to bortezomib treatment. For Figures 4(b)–4(e), , , .
