A novel action of terpendole E on the motor activity of mitotic Kinesin Eg5 |
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Authors: | Nakazawa Junko Yajima Junichiro Usui Takeo Ueki Masashi Takatsuki Akira Imoto Masaya Toyoshima Yoko Y Osada Hiroyuki |
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Affiliation: | Antibiotics Laboratory, RIKEN Institute for Discovery Research, Hirosawa 2-1,Wako-shi, Saitama 351-0198, Japan. |
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Abstract: | To reveal the mechanism of mitosis, the development of M phase-specific inhibitors is an important strategy. We have been screening microbial products to find specific M phase inhibitors that do not directly target tubulins, and rediscovered terpendole E (TerE) as a novel Eg5 inhibitor. TerE did not affect microtubule integrity in interphase, but induced formation of a monoastral spindle in M phase. TerE inhibited both motor and microtubule-stimulated ATPase activities of human Eg5, but did not affect conventional kinesin from either Drosophila or bovine brain. Although terpendoles have been reported as inhibitors of acyl-CoA:cholesterol O-acyltransferase (ACAT), the Eg5 inhibitory activity of TerE was independent of ACAT inhibition. Taken together, we demonstrate that TerE is a novel Eg5 inhibitor isolated from a fungal strain. |
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