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- Meredith C. Henderson
- 1Arizona Cancer Center,
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- Yeng-Jeng Y. Shaw
- 2BIO5 Institute, and
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- Hong Wang
- 4Translational Genomics Research Institute, Phoenix, Arizona
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- Haiyong Han
- 4Translational Genomics Research Institute, Phoenix, Arizona
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- Laurence H. Hurley
- 1Arizona Cancer Center,
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- Gary Flynn
- 2BIO5 Institute, and
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- Robert T. Dorr
- 1Arizona Cancer Center,
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- Daniel D. Von Hoff
- 4Translational Genomics Research Institute, Phoenix, Arizona
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説明
<jats:title>Abstract</jats:title> <jats:p>Pancreatic carcinoma is the fourth leading cause of death from cancer. Novel targets and therapeutic options are needed to aid in the treatment of pancreatic cancer. The compound UA62784 is a novel fluorenone with inhibitory activity against the centromere protein E (CENP-E) kinesin-like protein. UA62784 was isolated due to its selectivity in isogenic pancreatic carcinoma cell lines with a deletion of the DPC4 gene. UA62784 causes mitotic arrest by inhibiting chromosome congression at the metaphase plate likely through inhibition of the microtubule-associated ATPase activity of CENP-E. Furthermore, CENP-E binding to kinetochores during mitosis is not affected by UA62784, suggesting that the target lies within the motor domain of CENP-E. UA62784 is a novel specific inhibitor of CENP-E and its activity suggests a potential role for antimitotic drugs in treating pancreatic carcinomas. [Mol Cancer Ther 2009;8(1):36–44]</jats:p>
収録刊行物
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- Molecular Cancer Therapeutics
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Molecular Cancer Therapeutics 8 (1), 36-44, 2009-01-01
American Association for Cancer Research (AACR)