Desoxyepothilone B: An efficacious microtubule-targeted antitumor agent with a promising in vivo profile relative to epothilone B
نویسندگان
چکیده
منابع مشابه
Desoxyepothilone B: an efficacious microtubule-targeted antitumor agent with a promising in vivo profile relative to epothilone B.
A new class of 16-membered macrolides, the epothilones (Epos), has been synthesized and evaluated for antitumor potential in vitro and in vivo. Recent studies in these and other laboratories showed that epothilones and paclitaxel (paclitaxel) share similar mechanisms of action in stabilizing microtubule arrays as indicated by binding-displacement studies, substitution for paclitaxel in paclitax...
متن کاملPseudolaric acid B, a novel microtubule-destabilizing agent that circumvents multidrug resistance phenotype and exhibits antitumor activity in vivo.
PURPOSE Pseudolaric acid B (PAB) is the major bioactive constituent in the root bark of Pseudolarix kaempferi that has been used as an antifungal remedy in traditional Chinese medicine. Previous studies showed that PAB exhibited substantial cytotoxicity. The aims of this study were to elucidate the molecular target of PAB, to examine its mechanism of action, and to evaluate the efficacy of this...
متن کاملSuppression of microtubule dynamics by epothilone B is associated with mitotic arrest.
The epothilones are a group of novel microtubule-targeted, antimitotic compounds that have a paclitaxel-like, assembly enhancing effect on tubulin in vitro as well as in cultured cells. We hypothesize that epothilones induce mitotic arrest by suppressing microtubule dynamics. To test this hypothesis, we used MCF7 cells stably transfected with GFP-alpha-tubulin to analyze microtubule dynamics at...
متن کاملThe microtubule stabilizer patupilone (epothilone B) is a potent radiosensitizer in medulloblastoma cells.
Concurrent radiochemotherapy for medulloblastoma includes the microtubule disrupting agent vincristine; however, vincristine alone or as part of a combined treatment regimen is highly toxic. A major goal is therefore to replace vincristine with novel potent chemotherapeutic agents-in particular, with microtubule stabilizing and destabilizing compounds-with a larger therapeutic window. Here, we ...
متن کاملIndolo[2,3-b]quinoline Derivatives as Novel Promising Antitumor Agents
Chemistry Dept., Pharmaceutical Research Institute, Rydygiera St. 8, 01-793 Warszawa; Faculty of Biotechnology, Wrocław University, Fryderyk Joliot-Curie St. 14a, 50-383 Wrocław; Faculty of Chemistry, Wroclaw University of Technology, C.K. Norwid St.4/6, 50373 Wrocław; Experimental Acticancer Therapy Laboratory, Institute of Immunology and Experimental Therapy of Polish Academy of Sciences, Rud...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
ژورنال
عنوان ژورنال: Proceedings of the National Academy of Sciences
سال: 1998
ISSN: 0027-8424,1091-6490
DOI: 10.1073/pnas.95.16.9642