Discovery of a Potent Class I Protein Arginine Methyltransferase Fragment Inhibitor

Protein methyltransferases (PMTs) are a promising target class in oncology and other disease areas. They are composed of SET domain methyltransferases and structurally unrelated Rossman-fold enzymes that include protein arginine methyltransferases (PRMTs). In the absence of a well-defined medicinal...

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Veröffentlicht in:	Journal of medicinal chemistry 2016-02, Vol.59 (3), p.1176-1183
Hauptverfasser:	Ferreira de Freitas, Renato, Eram, Mohammad S, Szewczyk, Magdalena M, Steuber, Holger, Smil, David, Wu, Hong, Li, Fengling, Senisterra, Guillermo, Dong, Aiping, Brown, Peter J, Hitchcock, Marion, Moosmayer, Dieter, Stegmann, Christian M, Egner, Ursula, Arrowsmith, Cheryl, Barsyte-Lovejoy, Dalia, Vedadi, Masoud, Schapira, Matthieu
Format:	Artikel
Sprache:	eng
Schlagworte:	Dose-Response Relationship, Drug Drug Discovery Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Humans Models, Molecular Molecular Structure Protein-Arginine N-Methyltransferases - antagonists & inhibitors Protein-Arginine N-Methyltransferases - metabolism Repressor Proteins - antagonists & inhibitors Repressor Proteins - metabolism Structure-Activity Relationship
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