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


Journal

ACS medicinal chemistry letters
ISSN: 1948-5875
Titre abrégé: ACS Med Chem Lett
Pays: United States
ID NLM: 101521073

Informations de publication

Date de publication:
14 May 2020
Historique:
received: 09 01 2020
accepted: 19 03 2020
entrez: 22 5 2020
pubmed: 22 5 2020
medline: 22 5 2020
Statut: epublish

Résumé

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

Identifiants

pubmed: 32435414
doi: 10.1021/acsmedchemlett.0c00014
pmc: PMC7236245
doi:

Types de publication

Journal Article

Langues

eng

Pagination

977-983

Subventions

Organisme : NIGMS NIH HHS
ID : R01 GM114306
Pays : United States

Informations de copyright

Copyright © 2020 American Chemical Society.

Déclaration de conflit d'intérêts

The authors declare no competing financial interest.

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Auteurs

Annalisa Romanelli (A)

Department of Drug Chemistry and Technologies, Sapienza University of Rome, P. le A. Moro 5, 00185 Rome, Italy.

Giulia Stazi (G)

Department of Drug Chemistry and Technologies, Sapienza University of Rome, P. le A. Moro 5, 00185 Rome, Italy.

Rossella Fioravanti (R)

Department of Drug Chemistry and Technologies, Sapienza University of Rome, P. le A. Moro 5, 00185 Rome, Italy.

Clemens Zwergel (C)

Department of Drug Chemistry and Technologies, Sapienza University of Rome, P. le A. Moro 5, 00185 Rome, Italy.
Department of Medicine of Precision, University of Campania Luigi Vanvitelli, Via L. De Crecchio 7, 80138 Naples, Italy.

Elisabetta Di Bello (E)

Department of Drug Chemistry and Technologies, Sapienza University of Rome, P. le A. Moro 5, 00185 Rome, Italy.

Silvia Pomella (S)

Department of Oncohematology, Bambino Gesù Children's Hospital, IRCCS, Viale San Paolo 15, 00146 Rome, Italy.

Clara Perrone (C)

Department of Oncohematology, Bambino Gesù Children's Hospital, IRCCS, Viale San Paolo 15, 00146 Rome, Italy.

Cecilia Battistelli (C)

Department of Molecular Medicine, Sapienza University of Rome, P. le A. Moro 5, 00185 Rome, Italy.

Raffaele Strippoli (R)

Department of Molecular Medicine, Sapienza University of Rome, P. le A. Moro 5, 00185 Rome, Italy.
National Institute for Infectious Diseases L. Spallanzani, IRCCS, Via Portuense 292, 00149 Rome, Italy.

Marco Tripodi (M)

Department of Molecular Medicine, Sapienza University of Rome, P. le A. Moro 5, 00185 Rome, Italy.
National Institute for Infectious Diseases L. Spallanzani, IRCCS, Via Portuense 292, 00149 Rome, Italy.

Donatella Del Bufalo (D)

Preclinical Models and New Therapeutic Agents Unit, IRCCS Regina Elena National Cancer Institute, Viale Regina Elena 291,295, 00100 Rome, Italy.

Rossella Rota (R)

Department of Oncohematology, Bambino Gesù Children's Hospital, IRCCS, Viale San Paolo 15, 00146 Rome, Italy.

Daniela Trisciuoglio (D)

Institute of Molecular Biology and Pathology, National Research Council (CNR), Via Degli Apuli 4, Rome 00185, Italy.
Preclinical Models and New Therapeutic Agents Unit, IRCCS Regina Elena National Cancer Institute, Viale Regina Elena 291,295, 00100 Rome, Italy.

Antonello Mai (A)

Department of Drug Chemistry and Technologies, Sapienza University of Rome, P. le A. Moro 5, 00185 Rome, Italy.

Sergio Valente (S)

Department of Drug Chemistry and Technologies, Sapienza University of Rome, P. le A. Moro 5, 00185 Rome, Italy.

Classifications MeSH