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Sinefungin derivatives as small molecule chemical probes of SET domain-containing histone methyltransferase function

Sinefungin derivatives could be used to probe the therapeutic potential of inhibiting SET domain-containing histone methyltransferases. Misregulation of SET activity has been linked to multiple diseases, including cancer. In vitro studies identified a derivative of the natural compound sinefungin that specifically inhibited SET domain containing 2 (SETD2) at submicromolar concentrations. Next steps include developing more potent sinefungin derivatives that target SETD2 and other methyltransferases.

SciBX 5(45); doi:10.1038/scibx.2012.1192
Published online Nov. 15, 2012

Patent application filed; available for licensing

Zheng, W. et al. J. Am. Chem. Soc.; published online Oct. 8, 2012;
Contact: Minkui Luo, Memorial Sloan-Kettering Cancer Center, New York, N.Y.
Contact: Jinrong Min, Structural Genomics Consortium, University of Toronto, Toronto, Ontario, Canada