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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...

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Vydáno v:Medchemcomm
Hlavní autoři: Verschueren, Klaas, Cobbaut, Mathias, Demaerel, Joachim, Saadah, Lina, Voet, Arnout R. D., Van Lint, Johan, De Borggraeve, Wim M.
Médium: Artigo
Jazyk:Inglês
Vydáno: Royal Society of Chemistry 2017
Témata:
On-line přístup:https://ncbi.nlm.nih.gov/pmc/articles/PMC5567267/
https://ncbi.nlm.nih.gov/pubmed/28890776
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1039/c6md00675b
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