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- Publisher
- Springer Journals
- Copyright
- Copyright © 1999 by Nature America Inc.
- Subject
- Biomedicine; Biomedicine, general; Cancer Research; Metabolic Diseases; Infectious Diseases; Molecular Medicine; Neurosciences
- ISSN
- 1078-8956
- eISSN
- 1546-170X
- DOI
- 10.1038/10533
- Publisher site
- See Article on Publisher Site
Abstract
The mitogen-activated protein kinase pathway is thought to be essential in cellular growth and differentiation. Here we report the discovery of a highly potent and selective inhibitor of the upstream kinase MEK that is orally active. Tumor growth was inhibited as much as 80% in mice with colon carcinomas of both mouse and human origin after treatment with this inhibitor. Efficacy was achieved with a wide range of doses with no signs of toxicity, and correlated with a reduction in the levels of activated mitogen-activated protein kinase in excised tumors. These data indicate that MEK inhibitors represent a promising, noncytotoxic approach to the clinical management of colon cancer.
Journal
Nature Medicine – Springer Journals
Published: Jul 1, 1999