Identification of orally available naphthyridine protein kinase D inhibitors.

  title={Identification of orally available naphthyridine protein kinase D inhibitors.},
  author={Erik L Meredith and Ophelia Ardayfio and Kimberly Beattie and Markus R Dobler and Istvan J. Enyedy and Christoph Gaul and Vinayak P Hosagrahara and Charles Jewell and Keith A Koch and Wendy S. C. Lee and Hansjoerg Lehmann and Timothy A McKinsey and Karl Miranda and Nikos C Pagratis and Margaret R Pancost and Anup Patnaik and Dillon Phan and Craig F. Plato and Ming Qian and V. Rajaraman and Chang Rao and Olga Rozhitskaya and Thomas Ruppen and Jie Shi and Sarah J Siska and Clayton Springer and Maurice J van Eis and Richard B Vega and Anette von Matt and Lihua Yang and Taeyoung Yoon and Ji-Hu Zhang and N X Zhu and Lauren G Monovich},
  journal={Journal of medicinal chemistry},
  volume={53 15},
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 and heart failure. The present study describes the… CONTINUE READING


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