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Journal articles
Identification of PR-SET7 and EZH2 selective inhibitors inducing cell death in human leukemia U937 cells.
Sergio Valente
1
Ilaria Lepore
2
Carmela Dell'Aversana
2
Maria Tardugno
1, 3
Sabrina Castellano
3
Gianluca Sbardella
3
Stefano Tomassi
4
Salvatore Di Maro
4
Ettore Novellino
4
Roberto Di Santo
1
Roberta Costi
1
Lucia Altucci
2
Antonello Mai
1, *
Sergio Valente 1
Author
Ilaria Lepore 2
Author
Carmela Dell'Aversana 2
Author
Maria Tardugno 1, 3
Author
Sabrina Castellano 3
Author
Gianluca Sbardella 3
Author
Stefano Tomassi 4
Author
Salvatore Di Maro 4
Author
Antonello Mai 1
Correspondent author
1
Department of Medicinal Chemistry and Technologies (Piazzale Aldo Moro 5, I-00185, Rome - Italy)
- Institut Pasteur, Fondation Cenci Bolognetti - Istituto Pasteur Italia, Fondazione Cenci Bolognetti (Université de Rome La Sapienza 5 Place Aldo Moro 00185 Rome - Italy)
- RIIP - Réseau International des Instituts Pasteur (25, rue du Dr Roux 75724 Paris Cedex 15 - France)
- Università degli Studi di Roma "La Sapienza" [Rome] (Piazzale Aldo Moro 5, 00185 Roma - Italy)
2
Dipartimento di Patologia Generale (Italy)
- Seconda Università degli studi di Napoli (Piazza Luigi Miraglia, 2 – 80138 NAPOLI - Italy)
3
Dipartimento di Scienze Farmaceutiche e Biomediche (Italy)
- UNISA - Università degli Studi di Salerno (Via Giovanni Paolo II, 132 - 84084 Fisciano (SA) - Italy)
4
Department of Pharmacy Naples (University of Naples Federico II, via D. Montesano 49, I-80131 Naples - Italy)
- Université de Naples (France)
Abstract : Chemical manipulations undertaken on some bis(bromo- and dibromo-phenol) compounds previously reported by us as wide-spectrum epigenetic inhibitors let us to identify bis (bromo- and dibromo-methoxyphenyl) derivatives highly selective for PR-SET7 and EZH2 (compounds 4, 5, 9, and 10). Western blot analyses were carried out in U937 cells to determine the effects of such compounds on the methyl marks related to the tested enzymes (H3K4me1, H3K9me2, H4H20me1, and H3K27me3). The 1,5-bis(3-bromo-4-methoxyphenyl)penta-1,4-dien-3-one 4 (EC(50) vs EZH2 = 74.9 μM), tested in U937 cells at 50 μM, induced massive cell death and 28% of granulocytic differentiation, highlighting the potential use of EZH2 inhibitors in cancer.
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https://hal-riip.archives-ouvertes.fr/pasteur-00968696
Contributor : Istituto Pasteur Fondazione Cenci Bolognetti <>
Submitted on : Tuesday, April 1, 2014 - 2:14:12 PM
Last modification on : Wednesday, October 28, 2020 - 3:20:08 PM
Contributor : Istituto Pasteur Fondazione Cenci Bolognetti <>
Submitted on : Tuesday, April 1, 2014 - 2:14:12 PM
Last modification on : Wednesday, October 28, 2020 - 3:20:08 PM
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- HAL Id : pasteur-00968696, version 1
- DOI : 10.1016/j.biochi.2012.06.003
- PUBMED : 22709867
Citation
Sergio Valente, Ilaria Lepore, Carmela Dell'Aversana, Maria Tardugno, Sabrina Castellano, et al.. Identification of PR-SET7 and EZH2 selective inhibitors inducing cell death in human leukemia U937 cells.. Biochimie, Elsevier, 2012, 94 (11), pp.2308-13. ⟨10.1016/j.biochi.2012.06.003⟩. ⟨pasteur-00968696⟩
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