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

doi:10.1016/j.bcp.2010.01.007

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

Résultats de recherche: Contribution à un journal/une revue › Article › Revue par des pairs

Résumé

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.

langue originale	Anglais
Pages (de - à)	1462-1472
Nombre de pages	11
journal	Biochemical Pharmacology
Volume	79
Numéro de publication	10
Les DOIs	https://doi.org/10.1016/j.bcp.2010.01.007
Etat de la publication	Publié - 15 mai 2010

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10.1016/j.bcp.2010.01.007

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Wouters, J. (!!Manager) & Aprile, C. (!!Manager)
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Renard, P. (!!Manager)
Plateforme technologique Proteomique et spectrometrie de masse
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title = "Pyrazolo[4,3-c]isoquinolines as potential inhibitors of NF-κB activation",

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.",

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AU - Mortier, J.

AU - Frederick, R.

AU - Pochet, L.

AU - Wouters, J.

AU - Masereel, B.

AU - Ganeff, C.

AU - Remouchamps, C.

AU - Piette, J.

AU - Dejardin, E.

AU - Talaga, P.

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PY - 2010/5/15

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

Résumé

Accès au document

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Physico-chimie et caractérisation (PC2)

Spectrométrie de masse (MASUN)

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