897019-38-4Relevant academic research and scientific papers
Discovery and Characterization of a Highly Potent and Selective Aminopyrazoline-Based in Vivo Probe (BAY-598) for the Protein Lysine Methyltransferase SMYD2
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
, p. 4578 - 4600 (2016)
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.
CYANOGUANIDINE-SUBSTITUTED PYRAZOLINES
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Page/Page column 44, (2008/06/13)
The invention relates to the field of blood coagulation and, in particular, to the use of cyanoguanidine-substituted pyrazolines as medicaments, novel cyanoguanidine-substituted pyrazolines of formula (1) and to methods for the production thereof, in addition to the use thereof for producing medicaments for treating and/or for the prophylaxis of illnesses, in particular cardiovascular diseases, preferably thromboembolic diseases.
AZETIDINE-SUBSTITUTED PYRAZOLINES AS PAR-1 ANTAGONISTS
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Page/Page column 42-43, (2008/06/13)
The invention relates to blood clotting, and especially to the use of azetidine-substituted pyrazolines as medicaments, novel azetidine-substituted pyrazolines, methods for the production thereof, and the use of the same for producing medicaments for the treatment and/or prophylaxis of diseases, especially cardiovascular diseases, preferably thromboembolic diseases.
