Pan-histone demethylase inhibitors simultaneously targeting Jumonji C and lysine-specific demethylases display high anticancer activities.

Pan-histone demethylase inhibitors simultaneously targeting Jumonji C and lysine-specific demethylases display high anticancer activities.

In prostate cancer, two different types of histone lysine demethylases (KDM), LSD1/KDM1 and JMJD2/KDM4, are coexpressed and colocalize with the androgen receptor. We designed and synthesized hybrid LSD1/JmjC or "pan-KDM" inhibitors 1-6 by coupling the skeleton of tranylcypromine 7, a known...

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Bibliographic Details
Main Authors: Rotili, D, Tomassi, S, Conte, M, Benedetti, R, Tortorici, M, Ciossani, G, Valente, S, Marrocco, B, Labella, D, Novellino, E, Mattevi, A, Altucci, L, Tumber, A, Yapp, C, King, O, Hopkinson, R, Kawamura, A, Schofield, C, Mai, A
Format: Journal article
Language:English
Published: 2014

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