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Updated: Jun 3, 2026

Evaluation of Substrate Ubiquitylation by E3 Ubiquitin-ligase in Mammalian Cell Lysates
Published on: May 10, 2022
The multifaceted roles of USP7: new therapeutic opportunities
Benjamin Nicholson1, K G Suresh Kumar
1Progenra Inc, 277 Great Valley Parkway, Malvern, PA 19355, USA. Nicholson@progenra.com
Abstract:
The deubiquitylating enzyme USP7 (HAUSP) sits at a critical node regulating the activities of numerous proteins broadly characterized as tumor suppressors, DNA repair proteins, immune responders, viral proteins, and epigenetic modulators. Aberrant USP7 activity may promote oncogenesis and viral disease making it a compelling target for therapeutic intervention. Disclosed drug discovery programs have identified inhibitors of USP7 such as P005091 with cellular proof of concept and anti-proliferative activity in cancer models. Taken together, USP7 inhibitors hold promise as a new strategy for the treatment of disease.
Insights
The deubiquitylating enzyme USP7 regulates key proteins involved in cancer and viral diseases. Inhibitors like P005091 show promise for new therapeutic strategies against these conditions.
Area of Science:
- Biochemistry
- Molecular Biology
- Oncology
Background:
- The deubiquitylating enzyme USP7 (HAUSP) is a critical regulator of proteins involved in tumor suppression, DNA repair, immune response, viral replication, and epigenetic modification.
- Dysregulated USP7 activity is implicated in oncogenesis and viral pathogenesis, presenting it as a significant therapeutic target.
Purpose of the Study:
- To explore the therapeutic potential of USP7 inhibitors.
- To present evidence for USP7 as a viable drug target.
Main Methods:
- Review of existing literature on USP7 function and inhibition.
- Analysis of drug discovery programs targeting USP7, including specific inhibitor data (e.g., P005091).
Main Results:
- USP7 modulates a wide array of crucial cellular proteins.
- Inhibitors of USP7, such as P005091, have demonstrated cellular proof of concept and anti-proliferative effects in cancer models.
- USP7 inhibitors represent a promising new therapeutic avenue.
Conclusions:
- USP7 is a key enzyme with broad regulatory functions relevant to disease.
- Targeting USP7 with inhibitors offers a potential new strategy for treating cancer and viral diseases.
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