نتایج جستجو برای: vinblastine tubulin
تعداد نتایج: 14858 فیلتر نتایج به سال:
Colchicine and the Vincu alkaloids, vinblastine and vincristine, are commonly used as probes for microtubule-dependent processes in various cell types (see, for example, Oliver et al., 1974; Edelman et al., 1974; Nicolson, 1976; McClure, 1972): both drugs are known to inhibit selectively microtubule assembly in vitro and in uioo and to interact, through separate high-affinity binding sites, wit...
ownload H-indol-2-yl)phenyl)(3,4,5-trimethoxyphenyl)methanone (I-387) is a novel synthetic compound that ts tubulin action and exhibits potent antitumor activity in various preclinical models. I-387 inhibited vitro growth of several human cancer cell lines with IC50 values in the range of 15 to 39 nmol/L. olar concentrations of the compound induced apoptosis and caused phosphorylation of the an...
E7389, which is in phase I and II clinical trials, is a synthetic macrocyclic ketone analogue of the marine sponge natural product halichondrin B. Whereas its mechanism of action has not been fully elucidated, its main target seems to be tubulin and/or the microtubules responsible for the construction and proper function of the mitotic spindle. Like most microtubule-targeted antitumor drugs, it...
Newer therapeutic strategies for the treatment of multiple myeloma have focused on antagonizing the growth-promoting functions of interleukin 6 (IL-6). In this study, we examined the antitumor effects of two mechanistically different microtubule poisons, Taxol and vinblastine, in U266 human myeloma cells and determined whether IL-6 altered these effects. Taxol and vinblastine led to a dose-depe...
Conventional anticancer agents may display antiangiogenic effects, but the underlying mechanism is poorly understood. We determined the antiangiogenic properties of cisplatin, doxorubicin, and the microtubule-targeting agents docetaxel, epothilone B, and vinblastine at concentrations not affecting cell proliferation. We also assessed tubulin and actin morphology and the activity of two key mole...
E7974 is a synthetic analogue of the marine sponge natural product hemiasterlin. Here, we show that E7974, such as parental hemiasterlin, acts via a tubulin-based antimitotic mechanism. E7974 inhibits polymerization of purified tubulin in vitro with IC(50) values similar to those of vinblastine. In cultured human cancer cells, E7974 induces G(2)-M arrest and marked disruption of mitotic spindle...
Inhibition of mitosis by many drugs that bind to tubulin has been attributed to depolymerization of microtubules. However, we found previously that low concentrations of vinblastine and vincristine blocked mitosis in HeLa cells with little or no depolymerization of spindle microtubules, and spindles appeared morphologically normal or nearly normal. In the present study, we characterized the eff...
A series of derivatives of 5,6-diphenylpyridazin-3-one (DPP) was examined for interactions with calf brain tubulin following the demonstration that many members of the class caused significant mitotic effects in intact animals, while others had activity against murine P388 leukemia. In L1210 cells several DPP derivatives caused a rise in the mitotic index which correlated well with the cytotoxi...
Paclitaxel (PTX) and vinblastine (VBL) represent 2 classes of drugs that target tubulin but have separate binding properties and opposing mechanisms of action. To evaluate the potential use of these agents together in a chemotherapeutic regimen, we investigated their effects on the dynamics of tubulin polymerization and cellular cytotoxicity, when administered singly or in combination. In human...
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