Deubiquitinating Enzyme Inhibitors and their Potential in Cancer Therapy
Affiliation: Institut de Biologia Molecular de Barcelona, CSIC, Barcelona Science Park, Baldiri i Reixac 4, 08028 Barcelona, Spain.
Keywords: Deubiquitinating enzymes, DUBs, inhibitors, proteasome, small-molecule, ubiquitin specific proteases, USP1,
USP7, USP8, USP9x, USP14.
Deubiquitinating enzymes (or DUBs) attack the ubiquitin-based isopeptide bond, thus counteracting ubiquitinprotein
ligase activity in vivo. By disassembling ubiquitin-substrate and ubiquitin-ubiquitin covalent links, deubiquitinating
enzymes exert a very powerful control of many signaling processes within the ubiquitin-proteasome system (UPS). Very
active research in this field in the last decade shows that deubiquitinating enzymes play important regulatory roles in
aspects relevant to cancer, such as proteasome activity, p53 stability, the regulation of fanconi anemia related proteins,
tumor cell apoptosis induction, to mention a few. Thus, deubiquitinating enzymes have emerged as interesting drug
targets in cancer research. Here, the pharmacological inhibition of DUBs and its potential effect in cancer treatment are
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