C5-DNA Methyltransferase Inhibitors: From Screening to Effects on Zebrafish Embryo Development (pages 1337–1345)
Alexandre Ceccaldi, Arumugam Rajavelu, Christine Champion, Dr. Christine Rampon, Dr. Renata Jurkowska, Gytis Jankevicius, Catherine Sénamaud-Beaufort, Dr. Loïc Ponger, Dr. Nathalie Gagey, Hana Dali Ali, Dr. Jörg Tost, Prof. Sophie Vriz, Dr. Sindu Ros, Dr. Daniel Dauzonne, Prof. Albert Jeltsch, Dr. Dominique Guianvarc'h and Dr. Paola B. Arimondo
Version of Record online: 1 JUN 2011 | DOI: 10.1002/cbic.201100130
Screen shots: A set of flavones and flavanones is described as a new family of nanomolar DNA methyltransferase inhibitors. Structure–activity relationships, enzymatic competition and docking studies (see figure) have provided insights on their mode of action. Two inhibitors effected zebrafish development in a similar fashion to the reference drug, 5-azacytidine.