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Differential in vitro action of S-12363, a new vinblastine derivative, and of its epimer on microtubule proteins (1991)

Wright, Michel ; Garès, Michèle ; Verdier-Pinard, Pascal ; [et al.]

Springer

Cancer chemotherapy and pharmacology 28 (1991), S. 434-440

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ISSN: 1432-0843

Source: Springer Online Journal Archives 1860-2000

Topics: Medicine

Notes: Summary The action of two epimers of a new vinblastine derivative that differ in their in vivo antitumor activity and their cytotoxicity was studied in vitro in brain microtubule proteins. These two compounds, called S-12363 and S-12362, could not be distinguished from one another or from other active vinca alkaloids by their ability to prevent microtubule assembly. However, they differed strongly both from one another and from vincristine and vinblastine in their ability to induce the formation of tubulin paracrystals and in the stability of the paracrystals following temperature shifts from 0° to 37°C and vice versa. The most potent drugs, S-12363, induced considerable tubulin aggregation, which was even more pronounced than that observed in the presence of vincristine. Previous results have shown that S-12363, in contrast to vincristine, induces no neurotoxic effects. This observation is in disagreement with a direct relationship between tubulin aggregation and neurotoxicity.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00685819

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Rhazinilam mimics the cellular effects of taxol by different mechanisms of action (1994)

David, Bruno ; Sévenet, Thierry ; Morgat, Michel ; [et al.]

New York, NY : Wiley-Blackwell

Cell Motility and the Cytoskeleton 28 (1994), S. 317-326

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ISSN: 0886-1544

Keywords: maytansine ; vinblastine ; diphenylpyridazone ; colchicine ; taxol ; tubulin ; microtubule ; Life and Medical Sciences ; Cell & Developmental Biology

Source: Wiley InterScience Backfile Collection 1832-2000

Topics: Biology , Medicine

Notes: We have investigated the effects of the microtubule poison rhazinilam on microtubule assembly in vivo and in vitro. In mammalian cells, rhazinilam mimics the effects of taxol and leads to microtubule bundles, multiple asters, and microtubule cold stability. In vitro, rhazinilam protected preassembled microtubules from cold-induced disassembly, but not from calcium ion-induced disassembly. Moreover, both at 0°C and at 37°C, rhazinilam induced the formation of anomalous tubulin assemblies (spirals). This process was prevented by maytansine and vinblastine, but not by colchicine. Preferential saturable and stoichiometric binding of radioactive rhazinilam to tubulin in spirals was observed with a dissociation constant of 5 μM. This binding was abolished in the presence of vinblastine and maytansine. In contrast, specific binding of radioactive rhazinilam to tubulin assembled in microtubules was undetectable. These results demonstrate that rhazinilam alters microtubule stability differently than taxol, and that the overall similar effects of rhazinilam and taxol on the cellular cytoskeleton are the consequence of two distinct mechanisms of action at the molecular level. © 1994 Wiley-Liss, Inc.

Additional Material: 6 Ill.