The DOI matches its Crossref record; 3 of the 3 references it cites were found in a registry or an index.
Aminopyridine-Based c-Jun N-Terminal Kinase Inhibitors with Cellular Activity and Minimal Cross-Kinase Activity
Open accessAbstract
The c-Jun N-terminal kinases (JNK-1, -2, and -3) are members of the mitogen activated protein (MAP) kinase family of enzymes. They are activated in response to certain cytokines, as well as by cellular stresses including chemotoxins, peroxides, and irradiation. They have been implicated in the pathology of a variety of different diseases with an inflammatory component including asthma, stroke, Alzheimer's disease, and type 2 diabetes mellitus. In this work, high-throughput screening identified a JNK inhibitor with an excellent kinase selectivity profile. Using X-ray crystallography and biochemical screening to guide our lead optimization, we prepared compounds with inhibitory potencies in the low-double-digit nanomolar range, activity in whole cells, and pharmacokinetics suitable for in vivo use. The new compounds were over 1,000-fold selective for JNK-1 and -2 over other MAP kinases including ERK2, p38alpha, and p38delta and showed little inhibitory activity against a panel of 74 kinases.
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Cites
A central role for JNK in obesity and insulin resistance
Hirosumi, J., Tuncman, G., Chang, L., Görgün, C. Z., Uysal, K. T., Maeda, K., Karin, M., & Hotamisligil, G. S. (2002) · Nature · doi:10.1038/nature01137 · Cited by 3,359
Aguirre, V., Werner, E. D., Giraud, J., Lee, Y. H., Shoelson, S. E., & White, M. F. (2002) · Journal of Biological Chemistry · doi:10.1074/jbc.m101521200 · Cited by 1,010
The Structure of JNK3 in Complex with Small Molecule Inhibitors
Scapin, G., Patel, S. B., Lisnock, J., Becker, J. W., & LoGrasso, P. V. (2003) · Chemistry & Biology · doi:10.1016/s1074-5521(03)00159-5 · Cited by 131
Cited by
Wang, L., Wu, Y., Deng, Y., Kim, B., Pierce, L., Krilov, G., Lupyan, D., Robinson, S., Dahlgren, M. K., Greenwood, J., et al. (2015) · Journal of the American Chemical Society · doi:10.1021/ja512751q · Cited by 1,313
c-Jun N-terminal kinase (JNK) signaling: Recent advances and challenges
Bogoyevitch, M. A., Ngoei, K. R. W., Zhao, T. T., Yeap, Y. Y. C., & Ng, D. C. H. (2010) · Biochimica et Biophysica Acta (BBA) - Proteins and Proteomics · doi:10.1016/j.bbapap.2009.11.002 · Cited by 323
Assessment of Binding Affinity via Alchemical Free-Energy Calculations
Kuhn, M., Firth-Clark, S., Tosco, P., Mey, A. S. J. S., Mackey, M., & Michel, J. (2020) · Journal of Chemical Information and Modeling · doi:10.1021/acs.jcim.0c00165 · Cited by 222
Adipocyte lipolysis-stimulated interleukin-6 production requires sphingosine kinase 1 activity
Zhang, W., Mottillo, E. P., Zhao, J., Gartung, A., VanHecke, G. C., Lee, J.-F., Maddipati, K. R., Xu, H., Ahn, Y.-H., Proia, R. L., et al. (2014) · Journal of Biological Chemistry · doi:10.1074/jbc.m114.601096 · Cited by 80
Characterization of a novel JNK (c-Jun N-terminal kinase) inhibitory peptide
Ngoei, K. R. W., Catimel, B., Church, N., Lio, D. S., Dogovski, C., Perugini, M. A., Watt, P. M., Cheng, H.-C., Ng, D. C. H., & Bogoyevitch, M. A. (2011) · Biochemical Journal · doi:10.1042/bj20101244 · Cited by 31
Metadata
- Authors
- Szczepankiewicz, B. G., Kosogof, C., Nelson, L. T. J., Liu, G., Liu, B., Zhao, H., Serby, M. D., Xin, Z., Liu, M., Gum, R. J., Haasch, D. L., Wang, S., Clampit, J. E., Johnson, E. F., Lubben, T. H., Stashko, M. A., Olejniczak, E. T., Sun, C., Dorwin, S. A., Haskins, K., Abad-Zapatero, C., Fry, E. H., Hutchins, C. W., Sham, H. L., Rondinone, C. M., & Trevillyan, J. M.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2006-05-20
- Volume
- 49
- Issue
- 12
- Pages
- 3563-3580
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W1984052581
- Cited by
- 159
- References
- 3
- FWCI
- 4.17
- Type
- journal article
- Language
- en
- Open access
- green
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- The paper
- Szczepankiewicz, B. G., Kosogof, C., Nelson, L. T. J., Liu, G., Liu, B., Zhao, H., Serby, M. D., Xin, Z., Liu, M., Gum, R. J., Haasch, D. L., Wang, S., Clampit, J. E., Johnson, E. F., Lubben, T. H., Stashko, M. A., Olejniczak, E. T., Sun, C., Dorwin, S. A., . . . Trevillyan, J. M. (2006). Aminopyridine-Based c-Jun N-Terminal Kinase Inhibitors with Cellular Activity and Minimal Cross-Kinase Activity. Journal of Medicinal Chemistry. https://doi.org/10.1021/jm060199b
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Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
