Identification of orally available naphthyridine protein kinase D inhibitors

…, C Gaul, V Hosagrahara, C Jewell, K Koch…

文献索引：Meredith, Erik L.; Ardayfio, Ophelia; Beattie, Kimberly; Dobler, Markus R.; Enyedy, Istvan; Gaul, Christoph; Hosagrahara, Vinayak; Jewell, Charles; Koch, Keith; Lee, Wendy; Lehmann, HansJoerg; Mckinsey, Timothy A.; Miranda, Karl; Pagratis, Nikos; Pancost, Margaret; Patnaik, Anup; Phan, Dillon; Plato, Craig; Qian, Ming; Rajaraman, Vasumathy; Rao, Chang; Rozhitskaya, Olga; Ruppen, Thomas; Shi, Jie; Siska, Sarah J.; Springer, Clayton; Van Eis, Maurice; Vega, Richard B.; Von Matt, Anette; Yang, Lihua; Yoon, Taeyoung; Zhang, Ji-Hu; Zhu, Na; Monovich, Lauren G. Journal of Medicinal Chemistry, 2010 , vol. 53, # 15 p. 5400 - 5421

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被引用次数: 30

摘要

A novel 2, 6-naphthyridine was identified by high throughput screen (HTS) as a dual protein kinase C/D (PKC/PKD) inhibitor. PKD inhibition in the heart was proposed as a potential antihypertrophic mechanism with application as a heart failure therapy. As PKC was previously identified as the immediate upstream activator of PKD, PKD vs PKC selectivity was essential to understand the effect of PKD inhibition in models of cardiac hypertrophy ...