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Identification of potent and selective amidobipyridyl inhibitors of protein kinase D.
J Med Chem ; 53(15): 5422-38, 2010 Aug 12.
Article en En | MEDLINE | ID: mdl-20684592
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 understanding of cardiac myocyte signal transduction. The in vivo efficacy of a representative example compound on heart morphology is reported herein.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Piperazinas / Proteína Quinasa C / 2,2'-Dipiridil / Aminopiridinas / Naftiridinas Tipo de estudio: Diagnostic_studies Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2010 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Estados Unidos

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Piperazinas / Proteína Quinasa C / 2,2'-Dipiridil / Aminopiridinas / Naftiridinas Tipo de estudio: Diagnostic_studies Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2010 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Estados Unidos