ARTICLE | Targets & Mechanisms

Golden State of DUBs

How four new DUB inhibitor papers boost the proteasome space

November 2, 2017 11:34 PM UTC

Four papers in the last two weeks describing inhibitors of the ubiquitin-regulating protein USP7 could signal an important breakthrough in the ability to drug DUBs, a class of enzymes that has been stubbornly intractable until now. The activity is the latest example of drug developers turning to the proteasome to control aberrant protein activity in cancer and other diseases.

USP7 is a deubiquitinase (DUB) that has drawn attention because it acts to regulate levels of p53, a key tumor suppressor protein that has eluded translation for decades...