2017年8月
Ultrasound-dependent cytoplasmic internalization of a peptidesonosensitizer conjugate
BIOORGANIC & MEDICINAL CHEMISTRY
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- 巻
- 25
- 号
- 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.
- リンク情報
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- DOI
- https://doi.org/10.1016/j.bmc.2017.06.024
- PubMed
- https://www.ncbi.nlm.nih.gov/pubmed/28647135
- 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
- URL
- http://europepmc.org/abstract/med/28647135
- URL
- http://orcid.org/0000-0001-9564-6805
- ID情報
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- DOI : 10.1016/j.bmc.2017.06.024
- ISSN : 0968-0896
- eISSN : 1464-3391
- ORCIDのPut Code : 34763356
- PubMed ID : 28647135
- Web of Science ID : WOS:000406022200028