Research Article

Inhibition of Nek2 by Small Molecules Affects Proteasome Activity

Figure 5

The sensitivity of cancer cell lines to Nek2 inhibitors is correlated with their proteasome activity. (a) Cell lines sensitive to HCI-2184 treatment had, on average, higher proteasome activity compared to resistant cell lines. (b) Cell lines sensitive to HCI-2389 treatment had, on average, higher proteasome activity compared to resistant cell lines. These cancer cell lines were selected from the 150 cell lines in our lab, based on whether or not they were sensitive to both HCI-2184 or HCI-2389. “Sensitive” was defined as an value of 1 μM or lower. The 26S proteasomes were isolated by ultracentrifugation and proteasome activity measured by Proteasome-Glo Assay.
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