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  1. B300 農学部/生命農学研究科
  2. B300a 雑誌掲載論文
  3. 学術雑誌

Development of photoaffinity derivatives of the antitumor macrolide aplyronine A, a PPI-inducer between actin and tubulin

http://hdl.handle.net/2237/27403
bf7e1a19-1e57-4a35-b54b-f5b3e940b216
名前 / ファイル ライセンス アクション
ApA_PF_BMC_MS_r1_f.pdf ApA_PF_BMC_MS_r1_f.pdf ファイル公開日:2019/12/15 (4.4 MB)
Item type 学術雑誌論文 / Journal Article(1)
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
著者 Kita, Masaki

× Kita, Masaki

WEKO 75120

Kita, Masaki

Search repository
Yamagishi, Kota

× Yamagishi, Kota

WEKO 75121

Yamagishi, Kota

Search repository
Tsuchiya, Kota

× Tsuchiya, Kota

WEKO 75122

Tsuchiya, Kota

Search repository
Seguchi, Yu

× Seguchi, Yu

WEKO 75123

Seguchi, Yu

Search repository
Nakane, Hiroki

× Nakane, Hiroki

WEKO 75124

Nakane, Hiroki

Search repository
Kigoshi, Hideo

× Kigoshi, Hideo

WEKO 75125

Kigoshi, Hideo

Search repository
権利
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 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.
内容記述タイプ Abstract
出版者
出版者 Elsevier
言語
言語 eng
資源タイプ
資源タイプresource http://purl.org/coar/resource_type/c_6501
タイプ journal article
ISSN
収録物識別子タイプ ISSN
収録物識別子 0968-0896
書誌情報 BIOORGANIC & MEDICINAL CHEMISTRY

巻 25, 号 24, p. 6322-6331, 発行日 2017-12-15
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
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