Cargando…

Discovery of a potent protein kinase D inhibitor: insights in the binding mode of pyrazolo[3,4-d]pyrimidine analogues

In this study, we set out to rationally optimize PKD inhibitors based on the pyrazolo[3,4-d]pyrimidine scaffold. The lead compound for this study was 1-NM-PP1, which was previously found by us and others to inhibit PKD. In our screening we identified one compound (3-IN-PP1) displaying a 10-fold incr...

Descripción completa

Detalles Bibliográficos
Autores principales: Verschueren, Klaas, Cobbaut, Mathias, Demaerel, Joachim, Saadah, Lina, Voet, Arnout R. D., Van Lint, Johan, De Borggraeve, Wim M.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Royal Society of Chemistry 2017
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5567267/
https://www.ncbi.nlm.nih.gov/pubmed/28890776
http://dx.doi.org/10.1039/c6md00675b