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Comparison of microtubules stabilized with the anticancer drugs cevipabulin and paclitaxel

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Title: Comparison of microtubules stabilized with the anticancer drugs cevipabulin and paclitaxel
Authors: Nasrin, Syeda Rubaiya Browse this author
Ishihara, Tsukasa Browse this author
Kabir, Arif Md Rashedul Browse this author
Konagaya, Akihiko Browse this author
Sada, Kazuki Browse this author
Kakugo, Akira Browse this author →KAKEN DB
Issue Date: 6-Apr-2020
Publisher: Nature Publishing Group
Journal Title: Polymer journal
Volume: 52
Start Page: 969
End Page: 976
Publisher DOI: 10.1038/s41428-020-0334-9
Abstract: Microtubules, one of the major components of the cytoskeleton, play important roles as pathways for neuronal transport of cellular traffic. The loss of structural stability of microtubules causes detrimental effects on neurons and may contribute to several neurodegenerative diseases, such as Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, etc. The triazolopyrimidine class compound cevipabulin is a synthetic microtubule-stabilizing agent that has recently emerged as a drug for the treatment of Alzheimer's disease. However, the mechanism of microtubule stabilization by cevipabulin has not yet been revealed. Here, we explored the effect of cevipabulin on stabilizing microtubules polymerized from purified tubulins in vitro. We observed the effects of the concentration of microtubule-stabilizing drugs, incubation time, and modification of the cevipabulin structure on the stabilization of microtubules in comparison to those of the most commonly used anticancer drug, paclitaxel. This study will provide insight into the action of cevipabulin in the treatment of neurodegenerative diseases. Stabilization of microtubules occurs by paclitaxel bound to the taxoid site and cevipabulin (and its derivative) bound to the taxoid site and/or vinca alkaloid domain of the beta-tubulin in tubulin heterodimer.
Type: article (author version)
Appears in Collections:理学院・理学研究院 (Graduate School of Science / Faculty of Science) > 雑誌発表論文等 (Peer-reviewed Journal Articles, etc)

Submitter: 角五 彰

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