論文

2017年8月

Ultrasound-dependent cytoplasmic internalization of a peptidesonosensitizer conjugate

BIOORGANIC & MEDICINAL CHEMISTRY
  • Yuki Inaba
  • ,
  • Kazunori Watanabe
  • ,
  • Mizuki Kitamatsu
  • ,
  • Eiji Nakata
  • ,
  • Atsushi Harada
  • ,
  • Takashi Ohtsuki

25
15
開始ページ
4212
終了ページ
4217
記述言語
英語
掲載種別
研究論文(学術雑誌)
DOI
10.1016/j.bmc.2017.06.024
出版者・発行元
PERGAMON-ELSEVIER SCIENCE LTD

A method to induce cytoplasmic peptide delivery, using ultrasound, was demonstrated using a molecular conjugate of a cell-penetrating peptide (CPP), a functional peptide, and a sonosensitizer. As a model of such molecular conjugates, TatBim-RB, consisting of the Tat CPP, the Bim apoptosis inducing peptide, and the sonosensitizer rose bengal was synthesized. CPPs have been widely used for intracellular delivery of various cargos; however, CPP-fused molecules tend to become entrapped in endosomes, as was observed for TatBim-RB molecules applied to cells. To promote escape of the entrapped TatBim-RB molecules, cells were irradiated with ultrasound, which successfully induced endosomal escape and cytoplasmic dispersion of TatBim-RB, and subsequently apoptosis. Our results suggest that this peptidesonosensitizer conjugate strategy may facilitate numerous kinds of medicinal chemistry studies, and furthermore, this specific conjugate may exhibit potential as a novel therapeutic agent for the promotion of apoptosis. (C) 2017 Elsevier Ltd. All rights reserved.

Web of Science ® 被引用回数 : 2

リンク情報
DOI
https://doi.org/10.1016/j.bmc.2017.06.024
Web of Science
https://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=JSTA_CEL&SrcApp=J_Gate_JST&DestLinkType=FullRecord&KeyUT=WOS:000406022200028&DestApp=WOS_CPL

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