Article
OTX015 (MK-8628), a novel BET inhibitor, exhibits antitumor activity in non-small cell and small cell lung cancer models harboring different oncogenic mutations.
Oncotarget - 20 Dec 2016
Riveiro Maria E, Astorgues-Xerri Lucile, Vazquez Ramiro, Frapolli Roberta, Kwee Ivo, Rinaldi Andrea, Odore Elodie, Rezai Keyvan, Bekradda Mohamed, Inghirami Giorgio, D'Incalci Maurizio, Noel Kay, Cvitkovic Esteban, Raymond Eric, Bertoni Francesco
Abstract excerpt
Inhibitors targeting epigenetic control points of oncogenes offer a potential mean of blocking tumor progression in small cell and non-small cell lung carcinomas (SCLC, NSCLC). OTX015 (MK-8628) is a BET inhibitor selectively blocking BRD2/3/4. OTX015 was evaluated in a panel of NSCLC or SCLC models harboring different oncogenic mutations. Cell proliferation inhibition and cell cycle arrest were seen in sensitive...
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