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Targeting MYCN-Driven Transcription By BET-Bromodomain Inhibition.
Henssen A, Althoff K, Odersky A, Beckers A, Koche R, Speleman F, Schäfers S, Bell E, Nortmeyer M, Westermann F, De Preter K, Florin A, Heukamp L, Spruessel A, Astrahanseff K, Lindner S, Sadowski N, Schramm A, Astorgues-Xerri L, Riveiro ME, Eggert A, Cvitkovic E, Schulte JH. Henssen A, et al. Clin Cancer Res. 2016 May 15;22(10):2470-81. doi: 10.1158/1078-0432.CCR-15-1449. Epub 2015 Dec 2. Clin Cancer Res. 2016. PMID: 26631615
When MYCN was ectopically expressed, BET inhibition still disrupted MYCN target gene transcription without affecting MYCN expression. ...CONCLUSIONS: We show that OTX015 is effective against mouse and human MYCN-driven …
When MYCN was ectopically expressed, BET inhibition still disrupted MYCN target gene transcription …
Synergistic efficacy of inhibiting MYCN and mTOR signaling against neuroblastoma.
Kling MJ, Griggs CN, McIntyre EM, Alexander G, Ray S, Challagundla KB, Joshi SS, Coulter DW, Chaturvedi NK. Kling MJ, et al. BMC Cancer. 2021 Sep 26;21(1):1061. doi: 10.1186/s12885-021-08782-9. BMC Cancer. 2021. PMID: 34565342 Free PMC article.
We used two well-established BET (bromodomain extra-terminal) protein inhibitors (JQ1, OTX-015), and a clinically relevant mTOR inhibitor, temsirolimus, to target MYCN transcription and mTOR signaling, respectively. ...CONCLUSIONS: Together, our …
We used two well-established BET (bromodomain extra-terminal) protein inhibitors (JQ1, OTX-015), and a clinically relevant mTO …