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Development of photoaffinity derivatives of the antitumor macrolide aplyronine A, a PPI-inducer between actin and tubulin
http://hdl.handle.net/2237/27403
http://hdl.handle.net/2237/27403bf7e1a19-1e57-4a35-b54b-f5b3e940b216
名前 / ファイル | ライセンス | アクション |
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ApA_PF_BMC_MS_r1_f.pdf ファイル公開日:2019/12/15 (4.4 MB)
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Item type | 学術雑誌論文 / Journal Article(1) | |||||
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公開日 | 2018-02-13 | |||||
タイトル | ||||||
タイトル | Development of photoaffinity derivatives of the antitumor macrolide aplyronine A, a PPI-inducer between actin and tubulin | |||||
言語 | en | |||||
著者 |
Kita, Masaki
× Kita, Masaki× Yamagishi, Kota× Tsuchiya, Kota× Seguchi, Yu× Nakane, Hiroki× Kigoshi, Hideo |
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アクセス権 | ||||||
アクセス権 | open access | |||||
アクセス権URI | http://purl.org/coar/access_right/c_abf2 | |||||
権利 | ||||||
言語 | en | |||||
権利情報 | © 2017. This manuscript version is made available under the CC-BY-NC-ND 4.0 license http://creativecommons.org/licenses/by-nc-nd/4.0/ | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | Photoaffinity probe | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | Protein–protein interaction | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | Antitumor natural products | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | Actin | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | Tubulin | |||||
抄録 | ||||||
内容記述タイプ | Abstract | |||||
内容記述 | The antitumor and actin-depolymerizing marine macrolide aplyronine A (ApA) synergistically binds to tubulin in association with actin, and prevents spindle formation and mitosis. While the crystal structure of the actin ApA complex was solved in 2006, its interaction with the tubulin heterodimer has not been clarified. To investigate the binding modes of ApA as a unique protein–protein interaction (PPI)-inducer between these two cytoskeletal proteins, we prepared its photoaffinity acetylene and fluorescent derivatives with the aid of molecular modeling studies for probe design. Among these three derivatives, the ApA–PPA–TAMRA probe specifically photoreacted with both actin and tubulin in vitro. However, the photolabeling yield of tubulin was quite low (up to ∼1%), and one of the major side-reactions was the addition of a water molecule to the carbene species generated from an aryldiazirine moiety on the hydrophilic surface of actin. | |||||
言語 | en | |||||
出版者 | ||||||
出版者 | Elsevier | |||||
言語 | en | |||||
言語 | ||||||
言語 | eng | |||||
資源タイプ | ||||||
資源タイプ識別子 | http://purl.org/coar/resource_type/c_6501 | |||||
資源タイプ | journal article | |||||
出版タイプ | ||||||
出版タイプ | AM | |||||
出版タイプResource | http://purl.org/coar/version/c_ab4af688f83e57aa | |||||
DOI | ||||||
関連タイプ | isVersionOf | |||||
識別子タイプ | DOI | |||||
関連識別子 | https://doi.org/10.1016/j.bmc.2017.09.044 | |||||
ISSN | ||||||
収録物識別子タイプ | PISSN | |||||
収録物識別子 | 0968-0896 | |||||
書誌情報 |
en : BIOORGANIC & MEDICINAL CHEMISTRY 巻 25, 号 24, p. 6322-6331, 発行日 2017-12-15 |
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著者版フラグ | ||||||
値 | author | |||||
URI | ||||||
識別子 | http://doi.org/10.1016/j.bmc.2017.09.044 | |||||
識別子タイプ | DOI | |||||
URI | ||||||
識別子 | http://hdl.handle.net/2237/27403 | |||||
識別子タイプ | HDL |