Properly Substituted Analogues of BIX-01294 Lose Inhibition of G9a Histone Methyltransferase and Gain Selective Anti-DNA Methyltransferase 3A Activity

Dante Rotili; Domenico Tarantino; Biagina Marrocco; Christina Gros; Véronique Masson; Valérie Poughon; Fréderic Ausseil; Yanqi Chang; Donatella Labella; Sandro Cosconati; Salvatore Di Maro; Ettore Novellino; Michael Schnekenburger; Cindy Grandjenette; Celine Bouvy; Marc Diederich; Xiaodong Cheng; Paola B. Arimondo; Antonello Mai

doi:10.1371/journal.pone.0096941

Loading metrics

Open Access

Peer-reviewed

Research Article

Properly Substituted Analogues of BIX-01294 Lose Inhibition of G9a Histone Methyltransferase and Gain Selective Anti-DNA Methyltransferase 3A Activity

Dante Rotili,

Affiliation Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, Roma, IT
⨯
Domenico Tarantino,

Affiliation Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, Roma, IT
⨯
Biagina Marrocco,

Affiliation Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, Roma, IT
⨯
Christina Gros,

Affiliation USR3388 CNRS-Pierre Fabre ETaC, CRDPF, Toulouse, France
⨯
Véronique Masson,

Affiliation USR3388 CNRS-Pierre Fabre ETaC, CRDPF, Toulouse, France
⨯
Valérie Poughon,

Affiliation USR3388 CNRS-Pierre Fabre ETaC, CRDPF, Toulouse, France
⨯
Fréderic Ausseil,

Affiliation USR3388 CNRS-Pierre Fabre ETaC, CRDPF, Toulouse, France
⨯
Yanqi Chang,

Affiliation Department of Biochemistry, Emory University School of Medicine, Atlanta, Georgia, United States of America
⨯
Donatella Labella,

Affiliation Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, Roma, IT
⨯
Sandro Cosconati,

Affiliation DiSTABiF, Seconda Università di Napoli, Caserta, Italy
⨯
Salvatore Di Maro,

Affiliation Dipartimento di Farmacia, Università di Napoli “Federico II”, Napoli, IT
⨯
Ettore Novellino,

Affiliation Dipartimento di Farmacia, Università di Napoli “Federico II”, Napoli, IT
⨯
Michael Schnekenburger,

Affiliation Laboratoire de Biologie Moléculaire et Cellulaire du Cancer (LBMCC), Luxembourg, Luxembourg
⨯
Cindy Grandjenette,

Affiliation Laboratoire de Biologie Moléculaire et Cellulaire du Cancer (LBMCC), Luxembourg, Luxembourg
⨯
Celine Bouvy,

Affiliation Laboratoire de Biologie Moléculaire et Cellulaire du Cancer (LBMCC), Luxembourg, Luxembourg
⨯
Marc Diederich,

Affiliations Laboratoire de Biologie Moléculaire et Cellulaire du Cancer (LBMCC), Luxembourg, Luxembourg, Department of Pharmacy, College of Pharmacy, Seoul National University, Seoul, Korea
⨯
Xiaodong Cheng,

Affiliation Department of Biochemistry, Emory University School of Medicine, Atlanta, Georgia, United States of America
⨯
Paola B. Arimondo,

Affiliation USR3388 CNRS-Pierre Fabre ETaC, CRDPF, Toulouse, France
⨯
[ ... ],
Antonello Mai

* E-mail: antonello.mai@uniroma1.it

Affiliations Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, Roma, IT, Istituto Pasteur-Fondazione Cenci Bolognetti, Sapienza Università di Roma, Roma, IT
⨯
[ view all ]
[ view less ]

Properly Substituted Analogues of BIX-01294 Lose Inhibition of G9a Histone Methyltransferase and Gain Selective Anti-DNA Methyltransferase 3A Activity

Dante Rotili,
Domenico Tarantino,
Biagina Marrocco,
Christina Gros,
Véronique Masson,
Valérie Poughon,
Fréderic Ausseil,
Yanqi Chang,
Donatella Labella,
Sandro Cosconati

Published: May 8, 2014
https://doi.org/10.1371/journal.pone.0096941

Reader Comments (0)

Post a new comment on this article

Subject Areas
?

For more information about PLOS Subject Areas, click here.
We want your feedback. Do these Subject Areas make sense for this article? Click the target next to the incorrect Subject Area and let us know. Thanks for your help!

DNA methylation
Is the Subject Area "DNA methylation" applicable to this article?

Thanks for your feedback.
Methyltransferases
Is the Subject Area "Methyltransferases" applicable to this article?

Thanks for your feedback.
Enzyme inhibitors
Is the Subject Area "Enzyme inhibitors" applicable to this article?

Thanks for your feedback.
Raji cells
Is the Subject Area "Raji cells" applicable to this article?

Thanks for your feedback.
Histones
Is the Subject Area "Histones" applicable to this article?

Thanks for your feedback.
Human cytomegalovirus
Is the Subject Area "Human cytomegalovirus" applicable to this article?

Thanks for your feedback.
Luciferase
Is the Subject Area "Luciferase" applicable to this article?

Thanks for your feedback.
Computer software
Is the Subject Area "Computer software" applicable to this article?

Thanks for your feedback.