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Tubulin assembly inhibition

Halichondrin B (204) Macrocyclic polyether Eribulin (E7389, NSC-707389) (205) Oncology Tubulin assembly inhibition Phase II/III (advanced or metastatic breast cancer) Eisai 937-943... [Pg.84]

Hemiasterlin (206) Oligopeptide E7974 (207) Oncology Tubulin assembly inhibition Phase I (against a variety of human tumor xenografts) Eisai 944... [Pg.84]

Dolastatin 10 (215) Depsipeptide Soblidotin (YHI-501, TZT-1027, Auristatin PE) (216) Oncology Tubulin assembly inhibition Phase II Yakult Honsha (ASKA Pharmaceutical) 955... [Pg.85]

Microtubules can be reconstituted in vitro at 37 °C from a solution that contains a physiological mixture of brain tubulin, MAPs, small amounts of guanosine 5 -triphosphate (GTP), magnesium ions, and the calcium-chelating agent EGTA [ethylene glycol-bis(2-aminoethyl ether) N, N -tetraacetic acid]. Tubulin assembly is inhibited by low temperature and by the presence of calcium ions. [Pg.5]

The role of microtubules in secretion is more clearly defined. Colchicine and vinblastine inhibit secretion, even in cytochalasin-B-treated cells, and D2O (which promotes tubulin assembly) enhances secretion in cytochalasin-treated cells. Microtubules may also be necessary for the translocation of phagocytic vesicles from the neutrophil periphery into the central region of the cytoplasm. Drugs affecting microtubule assembly may inhibit particle-induced oxidase activation or else increase oxidase activation in response to soluble agents such as fMet-Leu-Phe. [Pg.140]

Dolastatin 15 (213) Depsipeptide Tasidotin (Synthadotin, ILX-651) (214) Oncology Induces G2/M phase cell cycle arrest by inhibiting tubulin assembly Phase II Genzyme 952-954... [Pg.85]

S4b jHjteb e causes degenerative alterations m tti tegument and intestinal sells cf the worm by binding to tn eoiehroins-s of tubulin, thus inhibiting its polymerization or assembly into microtubules. ... [Pg.147]

The tubulin-binding properties of (-)-rhazinilam were discovered through screening of a number of Malaysian plant extracts [60]. Natural (-)-rhazinilam induces tubulin spiralization, inhibiting tubulin assembly in the same way as vinblastine-like alkaloids, and protects microtubules from cold disassembly such as with paclitaxel [67]. This effect has never been observed with other microtubule poisons. For this reason, and despite the in vivo inactivity of (-)-rhazinilam [67], a number of analogues have been prepared by semi-synthesis and total synthesis (see Sections 3.1.3. and 3.2.3.) in order to improve the pharmacological properties of this molecule. [Pg.364]

All benzimidazole fungicides (benomyl, carbendazim, fuberidazole, thiabendazole) and thiophanate fungicides are cross-resistant. However, the reeently diseovered fungicide, zoxamide, which also inhibits the B-tubulin assembly, is not cross-resistant in oomycetes... [Pg.79]

The mechanism by which tubulin assembles and disassembles itself continues to be a major problem in this field, and taxol, by virtue of its unique ability to inhibit disassembly, remains the tool of choice for this study 134). As for the... [Pg.230]

The primary mechanism nf action nf vinorcibine is binding In tubulin, which inhibits microtubule assembly. It may be more specific than other vinca alkaloids for mitotic microtubules. Vinorcibine has been approved by the FDA for treatment of iinrescclablc advanced non-small cell lung cancer. The must important side effect is granulocytopenia. [Pg.427]

Similar to paclitaxel, promotes microtubule assembly inhibits depolymerization of tubulin inhibits cell division... [Pg.2301]

The mechanism of action of the vinca alkaloids is that of the inhibition of the polymerization of tubulin to microtubules. The cellular protein tubulin, which occurs in a- and /3-forms, is essential for proper cellular function. During mitosis tubulin polymerizes to form microtubules, which are long tube-shaped protein polymers. The equilibrium between unpolymerized a- and /3-tubulin and microtubules is an important one and any disruption of this equilibrium can send dividing cells into mitotic block and apoptosis. The vinca alkaloids bind to /3-tubulin at a different site from paclitaxel (Taxol) and act to prevent tubulin assembly. [Pg.7]

Fig. (6). Natural compounds which inhibit tubulin assembly. Fig. (6). Natural compounds which inhibit tubulin assembly.
Fig. (11). Structures of the non-benzimidazole fungicides, diethofencarb (15) and zarilamide (65a) which inhibit tubulin assembly, 5-hydroxy-7-methoxychromone (64), an antagonist of benzimidazole antidotes, and centaureidin (65), a tubulin-interactive flavone. Fig. (11). Structures of the non-benzimidazole fungicides, diethofencarb (15) and zarilamide (65a) which inhibit tubulin assembly, 5-hydroxy-7-methoxychromone (64), an antagonist of benzimidazole antidotes, and centaureidin (65), a tubulin-interactive flavone.
See other pages where Tubulin assembly inhibition is mentioned: [Pg.146]    [Pg.141]    [Pg.53]    [Pg.253]    [Pg.84]    [Pg.876]    [Pg.236]    [Pg.357]    [Pg.358]    [Pg.360]    [Pg.367]    [Pg.53]    [Pg.678]    [Pg.361]    [Pg.1143]    [Pg.1144]    [Pg.253]    [Pg.114]    [Pg.161]    [Pg.2302]    [Pg.357]    [Pg.358]    [Pg.360]    [Pg.367]    [Pg.259]    [Pg.307]    [Pg.8]    [Pg.33]    [Pg.482]   
See also in sourсe #XX -- [ Pg.360 ]

See also in sourсe #XX -- [ Pg.360 ]



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