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Identification of Potent and Selective Aminobipyridyl Inhibitors of Protein Kinase D

Meredith, Erik, Burgis, Robin, Beattie, Kimberley, Capparelli, Michael, Dipietro, Lucian, Gamber, Gabriel, Hosagrahara, Vinayak, Jewell, Charles, Lee, Wendy, Miranda, Karl, Rao, Chang, Rozhitskaya, Olga, Soldermann, Nicolas, Van Eis, Maurice, Vega, Richard, Yan, Wanlin, Zhu, Qingming, Monovich, Lauren, Chapo, Joseph, Hood, David, Koch, Keith, Lemon, Douglas, McKinsey, Timothy, Pagratis, Nikos, Phan, Dillon, Plato, Craig, Springer, Clayton and Enyedy, Istvan (2010) Identification of Potent and Selective Aminobipyridyl Inhibitors of Protein Kinase D. Journal of Medicinal Chemistry, 53 (15). pp. 5422-5438. ISSN 1520-4804


The synthesis and biological evaluation of potent and selective PKD inhibitors is 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 the current understanding of cardiac myocyte signal transduction. The in vivo efficacy of a representative example compound on heart morphology is reported herein.

Item Type: Article
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Additional Information: archiving not formally supported by this publisher
Keywords: protein kinase D, PKD, inhibitor, bipyridyl, cardiac myocyte, cardiac hypertrophy, histone deacetylase, HDAC
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Date Deposited: 13 Oct 2015 13:16
Last Modified: 13 Oct 2015 13:16


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