2010年1月
Cell permeability of Py-Im-polyamide-fluorescein conjugates: Influence of molecular size and Py/Im content
BIOORGANIC & MEDICINAL CHEMISTRY
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- 巻
- 18
- 号
- 2
- 開始ページ
- 978
- 終了ページ
- 983
- 記述言語
- 英語
- 掲載種別
- 研究論文(学術雑誌)
- DOI
- 10.1016/j.bmc.2009.07.018
- 出版者・発行元
- PERGAMON-ELSEVIER SCIENCE LTD
In order to investigate the influence of molecular size and pyrrole (Py)/imidazole (Im) content on the cell permeability of Py-Im-polyamide-fluorescein conjugates we systematically designed the Py-polyamides and Im-polyamides. Flow cytometric analysis revealed that Py-polyamides, even those with large molecular size, P-15 and P-18, showed good cellular uptake, but Im-polyamides showed very poor uptake. Fluorescence microscopy revealed that conjugate P-6 exhibited nuclear localization, while P-18 showed less nuclear stain but intracellular localization, suggesting that increased molecular size is one of the determinants in reducing nuclear access. Furthermore, results for hairpin polyamide conjugates H-1, H-2, and H-3 containing different Py/Im content indicated that cellular uptake increases as the Im residue is reduced. It appears that Py-Im-polyamide has general properties regardless of whether they have a linear or a hairpin structure. (C) 2009 Elsevier Ltd. All rights reserved.
- リンク情報
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- DOI
- https://doi.org/10.1016/j.bmc.2009.07.018
- J-GLOBAL
- https://jglobal.jst.go.jp/detail?JGLOBAL_ID=201102249420385623
- PubMed
- https://www.ncbi.nlm.nih.gov/pubmed/20022508
- Web of Science
- https://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=JSTA_CEL&SrcApp=J_Gate_JST&DestLinkType=FullRecord&KeyUT=WOS:000273613500053&DestApp=WOS_CPL
- ID情報
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- DOI : 10.1016/j.bmc.2009.07.018
- ISSN : 0968-0896
- eISSN : 1464-3391
- J-Global ID : 201102249420385623
- PubMed ID : 20022508
- Web of Science ID : WOS:000273613500053