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  Discovery of BAY-985, a highly selective TBK1/IKK epsilon inhibitor.

Lefranc, J., Schulze, V. K., Hillig, R. C., Briem, H., Prinz, F., Mengel, A., et al. (2020). Discovery of BAY-985, a highly selective TBK1/IKK epsilon inhibitor. Journal of Medicinal Chemistry, 63(2), 601-612. doi:10.1021/acs.jmedchem.9b01460.

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Item Permalink: http://hdl.handle.net/21.11116/0000-0005-9B80-B Version Permalink: http://hdl.handle.net/21.11116/0000-0005-9B85-6
Genre: Journal Article

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3191945.pdf (Publisher version), 5MB
 
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 Creators:
Lefranc, J., Author
Schulze, V. K., Author
Hillig, R. C., Author
Briem, H., Author
Prinz, F., Author
Mengel, A., Author
Heinrich, T., Author
Balint, J., Author
Rengachari, S.1, Author              
Irlbacher, H., Author
Stockigt, D., Author
Bömer, U., Author
Bader, B., Author
Gradl, S. N., Author
Nising, C. F., Author
von Nussbaum, F., Author
Mumberg, D., Author
Panne, D., Author
Wengner, A. M., Author
Affiliations:
1Department of Molecular Biology, MPI for Biophysical Chemistry, Max Planck Society, ou_1863498              

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 Abstract: 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.

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Language(s): eng - English
 Dates: 2019-12-202020-01-23
 Publication Status: Published in print
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 Table of Contents: -
 Rev. Type: Peer
 Identifiers: DOI: 10.1021/acs.jmedchem.9b01460
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Title: Journal of Medicinal Chemistry
Source Genre: Journal
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Pages: - Volume / Issue: 63 (2) Sequence Number: - Start / End Page: 601 - 612 Identifier: -