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Design, Synthesis, and Biological Evaluation of PKD Inhibitors

Protein kinase D (PKD) belongs to a family of serine/threonine kinases that play an important role in basic cellular processes and are implicated in the pathogenesis of several diseases. Progress in our understanding of the biological functions of PKD has been limited due to the lack of a PKD-specif...

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Detalles Bibliográficos
Autores principales: George, Kara M., Frantz, Marie-Céline, Bravo-Altamirano, Karla, LaValle, Courtney R., Tandon, Manuj, Leimgruber, Stephanie, Sharlow, Elizabeth R., Lazo, John S., Wang, Q. Jane, Wipf, Peter
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2011
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3261798/
https://www.ncbi.nlm.nih.gov/pubmed/22267986
http://dx.doi.org/10.3390/pharmaceutics3020186
Descripción
Sumario:Protein kinase D (PKD) belongs to a family of serine/threonine kinases that play an important role in basic cellular processes and are implicated in the pathogenesis of several diseases. Progress in our understanding of the biological functions of PKD has been limited due to the lack of a PKD-specific inhibitor. The benzoxoloazepinolone CID755673 was recently reported as the first potent and kinase-selective inhibitor for this enzyme. For structure-activity analysis purposes, a series of analogs was prepared and their in vitro inhibitory potency evaluated.