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РЖ ВИНИТИ 76 (BI28) 95.12-04Н3.139

Differential effects of paclitaxel (Taxol) analogs modified at positions C-2, C-7, and C-3' on tubulin polymerization and polymer stabilization: Identification of a hyperactive paclitaxel derivative [Text] / Surinder Grover [et al.] // Biochemistry. - 1995. - Vol. 34, N 12. - P3927-3934 . - ISSN 0006-2960
Перевод заглавия: Различное воздействие аналогов паклитакселя (таксола), модифицированных по C=2, C=7 и C=3', на полимеризацию тубулина и стабилизацию полимеров. Идентификация производных паклитакселя с повышенной активностью
Аннотация: Our finding that an analog of paclitaxel (Taxol) modified at position C-2 (2-debenzoyl-2-(m-azidobenzoyl)paclitaxel) was substantially more active than paclitaxel in promoting tubulin assembly [Chaudhary et al. (1994) J. Am. Chem. Soc. 116, 4097-4098] led us to perform an analysis of the modulating effects of microtubule-associated proteins, GTP, and temperature on assembly and polymer stability. The analog always showed superior activity to paclitaxel in inducing polymerization where it fails to occur without drug, probably indicating a greater ability than paclitaxel to "hypernucleate" assembly. In contrast, much smaller differences in effects on polymer stability were observed. The analysis was extended to a large series of derivatives modified at positions C-2, C-7, C-10, and C-3', including docetaxel, a clinically important analog of paclitaxel. While analog stabilization of polymer was frequently observed, neither qualitative nor quantitative analysis of this property reliably predicted whether a compound would have enhanced hypernucleation activity relative to that of paclitaxel. Stabilization was often observed at substoichiometric analog concentrations, while even superstoichiometric concentrations of most compounds failed to induce extensive tubulin polymerization at low temperatures or in the absence of microtubule-associated proteins or GTP. Docetaxel was intermediate in activity between paclitaxel and 2-debenzoyl-2-(m-azidobenzoyl)paclitaxel in promoting assembly reactions. We conclude that the hypernucleation of tubulin assembly and polymer stabilization observed with paclitaxel represent two distinct properties of the drug. Our findings suggest that paclitaxel, docetaxel, and 2-debenzoyl-2-(m-azidobenzoyl)paclitaxel are able to interact with progressively smaller assemblages of tubulin at low temperatures or in the absence of microtubule-associated proteins or GTP. США, Dep. of Chem., Virginia Polytechn. Inst. and St. Univ., Blacksburg, Virginia. Библ. 40

ГРНТИ	76.29.49

ВИНИТИ 761.29.49.55.07.11.11.99
Рубрики: ПАКЛИТАКСЕЛЬ
АНАЛОГИ ВЫСОКОАКТИВНЫЕ
ТУБУЛИН
ПОЛИМЕРИЗАЦИЯ
СТАБИЛИЗАЦИЯ ПОЛИМЕРОВ

Доп.точки доступа:
Grover, Surinder; Rimoldi, John M.; Molinero, anthony A.; Chaudhary, Ashok G.; Kingston, David G.I.; Hamel, Ernest

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