Pyrazolo[4,3-c]isoquinolines as potential inhibitors of NF-κB activation

J. Mortier, R. Frederick, L. Pochet, J. Wouters, B. Masereel, C. Ganeff, C. Remouchamps, J. Piette, E. Dejardin, P. Talaga

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Abstract

In this work, we aimed to build a 3D-model of NIK and to study the binding of pyrazolo[4,3-c]isoquinolines with a view to highlight the structural elements responsible for their inhibitory potency. However, in the course of this work, we unexpectedly found that the pyrazolo[4,3-c]isoquinolines initially reported as NIK inhibitors were neither inhibitors of this enzyme nor of the alternative NF-κB pathway, but were in fact inhibitors of another kinase, the TGF-β activated kinase 1 (TAK1) which is involved in the classical NF-κB pathway.
Original languageEnglish
Pages (from-to)1462-1472
Number of pages11
JournalBiochemical Pharmacology
Volume79
Issue number10
DOIs
Publication statusPublished - 15 May 2010

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    Mortier, J., Frederick, R., Pochet, L., Wouters, J., Masereel, B., Ganeff, C., Remouchamps, C., Piette, J., Dejardin, E., & Talaga, P. (2010). Pyrazolo[4,3-c]isoquinolines as potential inhibitors of NF-κB activation. Biochemical Pharmacology, 79(10), 1462-1472. https://doi.org/10.1016/j.bcp.2010.01.007