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news.The University of Oxford and Progenra have announced the data from a new study demonstrating the intracellular selectivity of progenra's novel anti-tumor compound.
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The study published as a research article, ‘Activity-Based Chemical Proteomics Accelerates Inhibitor Development for Deubiquitylating Enzymes’ investigated the details of a novel proteomics based method in detecting inhibition of intracellular deubiquitylating enzymes (DUBs).
The new method utilizes LC-MS-MS to detect DUBs labeled with DUB active site inhibitors and was tested to confirm the inhibitory profile of two small molecule inhibitors, PR-619 and P022077.
The results confirm the selective inhibition of USP7 in human cells treated with P022077, in contrast to the pan-DUB inhibition profile of the tool compound PR-619 in the same cells.
The DUB USP7 is a target for the treatment of neoplastic disease, which stabilizes oncogenic proteins and promotes the degradation of tumor suppressors such as p53.