The DOI matches its Crossref record; 1 of the 1 references it cites were found in a registry or an index.
Discovery of a novel Raf kinase inhibitor.
Open accessAbstract
We discuss the biology of Ras signal transduction and the epidemiology of ras mutations in association with disease as a background for the development of a Raf kinase inhibitor, BAY 43-9006. Knowledge of Ras effector pathways has permitted genetic validation of numerous targets involved in the Ras signaling cascade. A key Ras effector pathway involves the kinase cascade RAF/MEK/ERK (MEK: MAP/ERK kinase; ERK: extracellular signal related kinase). Indeed, we present studies of cell lines stably expressing mutant MEK constructs, which point to Raf kinase as a target for therapeutics with selective anti-tumor activity. Finally, a small molecule drug discovery program based on inhibition of Raf kinase activity is outlined and the initial pre-clinical development process of the Raf kinase inhibitor BAY 43-9006 is discussed.
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Cites
Increasing complexity of Ras signaling
Campbell, S. L., Khosravi-Far, R., Rossman, K. L., Clark, G. J., & Der, C. J. (1998) · Oncogene · doi:10.1038/sj.onc.1202174 · Cited by 1,079
Cited by
Targeting the Raf-MEK-ERK mitogen-activated protein kinase cascade for the treatment of cancer
Roberts, P. J., & Der, C. J. (2007) · Oncogene · doi:10.1038/sj.onc.1210422 · Cited by 2,788
Distinct Sets of Genetic Alterations in Melanoma
Curtin, J. A., Fridlyand, J., Kageshita, T., Patel, H. N., Busam, K. J., Kutzner, H., Cho, K.-H., Aiba, S., Bröcker, E.-B., LeBoit, P. E., et al. (2005) · New England Journal of Medicine · doi:10.1056/nejmoa050092 · Cited by 2,747
Drugging the undruggable RAS: Mission Possible?
Cox, A. D., Fesik, S. W., Kimmelman, A. C., Luo, J., & Der, C. J. (2014) · Nature Reviews Drug Discovery · doi:10.1038/nrd4389 · Cited by 1,997
Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity
Tsai, J., Lee, J. T., Wang, W., Zhang, J., Cho, H., Mamo, S., Bremer, R., Gillette, S., Kong, J., Haass, N. K., et al. (2008) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0711741105 · Cited by 1,346
Self-citationRAS Interaction with PI3K: More Than Just Another Effector Pathway
Castellano, E., & Downward, J. (2011) · Genes & Cancer · doi:10.1177/1947601911408079 · Cited by 762
Metadata
- Authors
- Lyons, J. F., Wilhelm, S., Hibner, B., & Bollag, G.
- Venue
- Endocrine-related cancer
- Publisher
- Bioscientifica
- Published
- 2001-09
- Volume
- 8
- Issue
- 3
- Pages
- 219-225
- ISSN
- 1351-0088 (ISSN-L)
- OpenAlex
- W2144785546
- Cited by
- 416
- References
- 1
- FWCI
- 6.95
- Type
- journal article
- Language
- en
- Open access
- bronze
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- Lyons, J. F., Wilhelm, S., Hibner, B., & Bollag, G. (2001). Discovery of a novel Raf kinase inhibitor. Endocrine-related cancer. https://doi.org/10.1677/erc.0.0080219
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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