Design of First-in-Class Dual EZH2/HDAC Inhibitor: Biochemical Activity and Biological Evaluation in Cancer Cells

[Image: see text] Since the histone modifying enzymes EZH2 and HDACs control a number of epigenetic-dependent carcinogenic pathways, we designed the first-in-class dual EZH2/HDAC inhibitor 5 displaying (sub)micromolar inhibition against both targets. When tested in several cancer cell lines, the hyb...

Disgrifiad llawn

Wedi'i Gadw mewn:
Manylion Llyfryddiaeth
Cyhoeddwyd yn:ACS Med Chem Lett
Prif Awduron: Romanelli, Annalisa, Stazi, Giulia, Fioravanti, Rossella, Zwergel, Clemens, Di Bello, Elisabetta, Pomella, Silvia, Perrone, Clara, Battistelli, Cecilia, Strippoli, Raffaele, Tripodi, Marco, del Bufalo, Donatella, Rota, Rossella, Trisciuoglio, Daniela, Mai, Antonello, Valente, Sergio
Fformat: Artigo
Iaith:Inglês
Cyhoeddwyd: American Chemical Society 2020
Mynediad Ar-lein:https://ncbi.nlm.nih.gov/pmc/articles/PMC7236245/
https://ncbi.nlm.nih.gov/pubmed/32435414
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.0c00014
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