Identification of potent and selective amidobipyridyl inhibitors of protein kinase D

…, J Chapo, L DiPietro, G Gamber, I Enyedy…

文献索引：Meredith, Erik L.; Beattie, Kimberly; Burgis, Robin; Capparelli, Michael; Chapo, Joseph; Dipietro, Lucian; Gamber, Gabriel; Enyedy, Istvan; Hood, David B.; Hosagrahara, Vinayak; Jewell, Charles; Koch, Keith A.; Lee, Wendy; Lemon, Douglas D.; Mckinsey, Timothy A.; Miranda, Karl; Pagratis, Nikos; Phan, Dillon; Plato, Craig; Rao, Chang; Rozhitskaya, Olga; Soldermann, Nicolas; Springer, Clayton; Van Eis, Maurice; Vega, Richard B.; Yan, Wanlin; Zhu, Qingming; Monovich, Lauren G. Journal of Medicinal Chemistry, 2010 , vol. 53, # 15 p. 5422 - 5438

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被引用次数: 25

摘要

The synthesis and biological evaluation of potent and selective PKD inhibitors are described herein. The compounds described in the present study selectively inhibit PKD among other putative HDAC kinases. The PKD inhibitors of the present study blunt phosphorylation and subsequent nuclear export of HDAC4/5 in response to diverse agonists. These compounds further establish the central role of PKD as an HDAC4/5 kinase and enhance the current ...