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UA62784, a Novel Inhibitor of Centromere Protein E Kinesin-Like Protein

UA62784, a Novel Inhibitor of Centromere Protein E Kinesin-Like Protein

Meredith C Henderson, Yeng-Jeng Y Shaw, Hong Wang, Haiyong Han, Laurence H Hurley, Gary Flynn, Robert T Dorr, Daniel D Von Hoff

Mol Cancer Ther. 2009 Jan;8(1):36-44.

PMID: 19139111

Abstract:

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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP313367929	UA62784		313367-92-9	Price

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