Rosaria Benedetti, Carmela Dell'Aversana, Tommaso De Marchi, Dante Rotili, Ning Qing Liu, Boris Novakovic, Serena Boccella, Salvatore Di Maro, Sandro Cosconati, Alfonso Baldi, Emma Niméus, Johan Schultz, Urban Höglund, Sabatino Maione, Chiara Papulino, Ugo Chianese, Francesco Iovino, Antonio Federico, Antonello Mai, Hendrik G Stunnenberg, Angela Nebbioso, Lucia Altucci
In breast cancer, Lysine-specific demethylase-1 (LSD1) and other lysine demethylases (KDMs), such as Lysine-specific demethylase 6A also known as Ubiquitously transcribed tetratricopeptide repeat, X chromosome (UTX), are co-expressed and co-localize with estrogen receptors (ERs), suggesting the potential use of hybrid (epi)molecules to target histone methylation and therefore regulate/redirect hormone receptor signaling. Here, we report on the biological activity of a dual-KDM inhibitor (MC3324), obtained by coupling the chemical properties of tranylcypromine, a known LSD1 inhibitor, with the 2OG competitive moiety developed for JmjC inhibition...
December 16, 2019: Cancers