Effect of ubiquitin-activating enzyme inhibition on multiple myeloma cell line MM1.S

Resistance to proteasome inhibitors has prompted interest in blocking upstream components of the ubiquitin-proteasome pathway for the treatment of multiple myeloma (MM). We therefore evaluated the activity of TAK-243, a novel and specific inhibitor of E1 ubiquitin activating enzyme (UAE) activity, in the MM cell line MM1.S. Treatment of MM1.S with 25 nM TAK-243 for 24 hr caused extensive changes in gene expression, highly uniform between triplicates. Cells were incubated for 24 hr in triplicate with either DMSO control or 25 nM TAK-243. The submitter did not provide the normalized data.