ケミカルバイオロジー研究グループ（終了）
Terpendole E, H, C, I
- Structure
-
E:(re-discovered compound)
H:
C:
I:
- Producing organism
- a relative to Albophoma yamanashiensis
- Biological activity
- cell cycle inhibition, inhibition of kinesin Eg5
- 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.
- References
-
isolation and structural determination
- Huang XH, Tomoda H, Nishida H, Masuma R, Omura S.: Terpendoles, novel ACAT inhibitors produced by Albophoma yamanashiensis. I. Production, isolation and biological properties.
J Antibiot, 48(1): 1-4 (1995)
- Matsuura N, Onose R, Osada H.: Morphology reversion activity of phosmidosine and phosmidosine B, a newly isolated derivative, on src transformed NRK cells.
J Antibiot, 49(4): 361-365 (1996)- Tomoda H, Tabata N, Yang DJ, Takayanagi H, Omura S.: Terpendoles, novel ACAT inhibitors produced by Albophoma yamanashiensis. III. Production, isolation and structure elucidation of new components.
J Antibiot, 48(8): 793-804 (1995)biological activities as a new roles- Nakazawa J, Yajima J, Usui T, Ueki M, Takatsuki A, Imoto M, Toyoshima YY, Osada H.: A novel action of terpendole E on the motor activity of mitotic Kinesin Eg5.
Chem Biol, 10(2): 131-137 (2003) - Huang XH, Tomoda H, Nishida H, Masuma R, Omura S.: Terpendoles, novel ACAT inhibitors produced by Albophoma yamanashiensis. I. Production, isolation and biological properties.