SUMO-activating enzyme (SAE) inhibitor / ML792 is a potent (IC50’s = 3 nM SUMO1; 11 nM SUMO2) and selective( IC50 = 32 µM for NEDD8-activating enzyme (NAE)) mechanism-based inhibitor of SUMO-activating enzyme (SAE).1 Treatment of multiple cancer cell lines led to failure of mitotic progression and induction of endoreduplication with MYC-amplified cell lines showing higher sensitivity. ML792 inhibited B-cell growth and promoted cell death in Epstein-Barr virus (EBV)-positive B cells and nasopharyngeal carcinoma cells. It also modulated Latent Membrane Protein-1-induced cell migration and cell adhesion suggesting therapeutic potential in treating EBV-associated malignancies.2
Biochemicals & reagents
1644342-14-2
1) He et al. (2017), Probing the roles of SUMOylation in cancer cell biology by using a selective SAE inhibitor; Nat. Chem. Biol. 13 1164 2) Garcia et al. (2021); Effects of targeting sumoylation processes during latent and induced Epstein-Barr virus infections using the small molecules inhibitor ML-792, Antiviral Res., 188 105038
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TARGET: Ubiquitin ligase -- PATHWAY: Posttranslational modification; Cell migration; Cell adhesion -- RESEARCH AREA: Ubiquitin/Proteasome -- DISEASE AREA: Cancer