| Autor: |
Lefranc, J., Schulze, V., Hillig, R., Briem, H., Prinz, F., Mengel, A., Heinrich, T., Balint, J., Rengachari, S., Irlbacher, H., Stockigt, D., Bömer, U., Bader, B., Gradl, S., Nising, C., von Nussbaum, F., Mumberg, D., Panne, D., Wengner, A. |
| Jazyk: |
angličtina |
| Rok vydání: |
2020 |
| Zdroj: |
Journal of Medicinal Chemistry |
| Popis: |
The serine/threonine kinase TBK1 (TANK-binding kinase 1) and its homologue IKK epsilon are noncanonical members of the inhibitor of the nuclear factor kappa B (I kappa B) kinase family. These kinases play important roles in multiple cellular pathways and, in particular, in inflammation. Herein, we describe our investigations on a family of benzimidazoles and the identification of the potent and highly selective TBK1/IKK epsilon inhibitor BAY-985. BAY-985 inhibits the cellular phosphorylation of interferon regulatory factor 3 and displays antiproliferative efficacy in the melanoma cell line SK-MEL-2 but showed only weak antitumor activity in the SK-MEL-2 human melanoma xenograft model. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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