In a recent paper published in PNAS, Wang et al. show that the inhibition of the deubiquitinase USP9x by the small molecule WP-1130 is able to induce degradation of the transcription factor E-twenty-six related gene (ERG).
In addition, USP9X KnockDown (KD) HeLa cells have increased ubiquitinated ERG levels together with ERG depletion (after 72 hours of treatment of HeLa cells with siRNA against USP9X and controls ). (1)
Interestingly, ERG is an important driver of prostate cancer. Fused with the Androgen-responsive Gene Transmembrane Protease, Serine 2 (TMPRSS2) gene, ERG gene is overexpressed in 40% of prostate tumors.
In this study, the authors demonstrate that:
1/ USP9X is potential druggable target in prostate cancer.
2/ WP1130 is a possible lead compound for prostate cancer.
3/ By inhibiting USPX9, the WP1130 small molecule induces a ERG depletion and impacts prostate tumor growth.
(1) Wang et al. “Ablation of the oncogenic transcription factor ERG by deubiquitinase inhibition in prostate cancer” (2014) PNAS, vol. 111 n° 11, 4251-4256. DOI10.1073/pnas.132219811
5 validated prostate cancer research tools
- WP1130 (98% pure) is a novel DUB inhibitor potentially usefull for the development of ERG-depleting drugs in prostate cancer. (1)
- USP9X stable KD ready-to-use HeLa cell line includes the Silencix® technology (using a unique siRNA Delivery system) and brings stability and efficiency of knockdown in a syngenic model.
- Human USP9X specific mouse monoclonal (1C4) antibody and Human ERG specific rabbit polyclonal antibody are 100% guaranteed for Western Blotting, IF, ELISA and Western Blotting, ICC and IF respectively.
- VU-1 is a monoclonal antibody recognizes free ubiquitin, K48-, K63-, K11- and linear chains on Western blot and is ideal for immunostaining to detect subcellular ubiquitin localization.
- PSA antibody [C2C3] is a rabbit polyclonal antibody ideal for the Prostate-Specific Antigen (PSA) detection in Human tissues by IHC.
Experimental data gallery related to ERG, USP9X and DUB inhibitor