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Tubulin assembly inhibitor colchicines

Halichondrin B (7), a highly cytotoxic metabolite isolated from the Japanese sponge H. okadai is a tubulin assembly inhibitor,which binds to the colchicine domain. The macrocyclic portion seems to be essential for the activityEribulin (E7389 146) is a drug candidate designed on the basis of the macrocyclic portion of halichondrin B and is now under phase II/III trials for breast cancer conducted by Eisei Co. Ltd., Tokyo. ... [Pg.352]

Vinca alkaloids (vincristine, vinblastine, vinorelbine) are derived from the periwinkle plant (Vinca rosea). These agents work by binding to tubulin at a site different than colchicine or paclitaxel. They block polymerization, which prevents the formation of the mitotic spindle, and are used as antineoplastic agents. Taxanes produce a stabilization of microtubules similar to colchicine, but by a different mechanism, and also halt cells in metaphase. Paclitaxel (taxol) is the taxane used clinically. It is derived from the bark of the pacific yew. Taxol disrupts several microtubule-based functions as completely as inhibitors of polymerization, emphasizing the importance of assembly/disassembly balance in microtubule function. Recently, it has been found that paclitaxel also binds to and inhibits the function of a protein called bcl-2, an inhibitor of one or more pathways involved in mediating apoptosis. PaclitaxeTs interference with this function promotes apoptosis in addition to its microtubule-related inhibition of cell division. [Pg.483]


See other pages where Tubulin assembly inhibitor colchicines is mentioned: [Pg.876]    [Pg.206]    [Pg.357]    [Pg.32]    [Pg.361]    [Pg.114]    [Pg.357]    [Pg.114]    [Pg.44]    [Pg.343]    [Pg.165]    [Pg.166]    [Pg.210]    [Pg.210]    [Pg.92]   
See also in sourсe #XX -- [ Pg.357 ]




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