Journal of Medicinal Chemistry p. 4578 - 4600 (2016)
Update date:2022-08-15
Topics:
Eggert, Erik
Hillig, Roman C.
Koehr, Silke
St?ckigt, Detlef
Weiske, J?rg
Barak, Naomi
Mowat, Jeffrey
Brumby, Thomas
Christ, Clara D.
Ter Laak, Antonius
Lang, Tina
Fernandez-Montalvan, Amaury E.
Badock, Volker
Weinmann, Hilmar
Hartung, Ingo V.
Barsyte-Lovejoy, Dalia
Szewczyk, Magdalena
Kennedy, Steven
Li, Fengling
Vedadi, Masoud
Brown, Peter J.
Santhakumar, Vijayaratnam
Arrowsmith, Cheryl H.
Stellfeld, Timo
Stresemann, Carlo
Protein lysine methyltransferases have recently emerged as a new target class for the development of inhibitors that modulate gene transcription or signaling pathways. SET and MYND domain containing protein 2 (SMYD2) is a catalytic SET domain containing methyltransferase reported to monomethylate lysine residues on histone and nonhistone proteins. Although several studies have uncovered an important role of SMYD2 in promoting cancer by protein methylation, the biology of SMYD2 is far from being fully understood. Utilization of highly potent and selective chemical probes for target validation has emerged as a concept which circumvents possible limitations of knockdown experiments and, in particular, could result in an improved exploration of drug targets with a complex underlying biology. Here, we report the development of a potent, selective, and cell-active, substrate-competitive inhibitor of SMYD2, which is the first reported inhibitor suitable for in vivo target validation studies in rodents.
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