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Identification of Potent and Selective Aminobipyridyl Inhibitors of Protein Kinase D

Meredith, Erik and Burgis, Robin and Beattie, Kimberley and Capparelli, Michael and Dipietro, Lucian and Gamber, Gabriel and Hosagrahara, Vinayak and Jewell, Charles and Lee, Wendy and Miranda, Karl and Rao, Chang and Rozhitskaya, Olga and Soldermann, Nicolas and Van Eis, Maurice and Vega, Richard and Yan, Wanlin and Zhu, Qingming and Monovich, Lauren and Chapo, Joseph and Hood, David and Koch, Keith and Lemon, Douglas and McKinsey, Timothy and Pagratis, Nikos and Phan, Dillon and Plato, Craig and 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

Abstract

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
URI: https://oak.novartis.com/id/eprint/2844

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