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

ABSTRACT: 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 hybrid 5 impaired cell viability at low micromolar level and in leukemia U937 and rhabdomyosarcoma RH4 cells provided G1 arrest, apoptotic induction, and increased differentiation, associated with an increase of acetyl-H3 and acetyl-α-tubulin and a decrease of H3K27me3 levels. In glioblastoma U87 cells, 5 hampered epithelial to mesenchymal transition by increasing the E-cadherin expression, thus proposing itself as a useful candidate for anticancer therapy.

SUBMITTER: Romanelli A

PROVIDER: S-EPMC7236245 | biostudies-literature | 2020 May

REPOSITORIES: biostudies-literature

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

Romanelli Annalisa A Stazi Giulia G Fioravanti Rossella R Zwergel Clemens C Di Bello Elisabetta E Pomella Silvia S Perrone Clara C Battistelli Cecilia C Strippoli Raffaele R Tripodi Marco M Del Bufalo Donatella D Rota Rossella R Trisciuoglio Daniela D Mai Antonello A Valente Sergio S

ACS medicinal chemistry letters 20200319 5

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 <b>5</b> displaying (sub)micromolar inhibition against both targets. When tested in several cancer cell lines, the hybrid <b>5</b> impaired cell viability at low micromolar level and in leukemia U937 and rhabdomyosarcoma RH4 cells provided G1 arrest, apoptotic induction, and increased differentiation, associated with an increas ...[more]

PMID: 32435414

Dataset Information

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

Publications

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

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