| Synthesis and silencing properties of siRNAs possessing lipophilic groups at their 3'-termini. | |
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MedLine Citation:
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PMID: 18644731 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Short-interfering RNAs (siRNAs) conjugated with lipophilic groups at their 3'-termini were synthesized. The properties of the synthesized siRNAs were examined in detail, and it was found that at low concentrations, their silencing abilities were dependent on the positions of the modifications and the types of organic molecules attached. Although the modification of siRNAs with palmitic acid or oleic acid at the 3'-end slightly reduced their silencing activities, siRNAs had enough abilities to induce RNAi at 10 nM concentrations. On the other hand, the modification of siRNAs with cholesterol at the 3'-end of the passenger strand was tolerated; however, the modification at the guide strand significantly reduces its silencing activity. The siRNAs modified with the lipophilic groups did not possess ability to penetrate the plasma membranes of HT-1080 cells without the transfection reagent. However, the results described in this report will aid in designing novel siRNAs with cell membrane-permeable molecules. |
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Authors:
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Yoshihito Ueno; Koshi Kawada; Tomoharu Naito; Aya Shibata; Kayo Yoshikawa; Hye-Sook Kim; Yusuke Wataya; Yukio Kitade |
Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't Date: 2008-07-09 |
Journal Detail:
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Title: Bioorganic & medicinal chemistry Volume: 16 ISSN: 1464-3391 ISO Abbreviation: Bioorg. Med. Chem. Publication Date: 2008 Aug |
Date Detail:
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Created Date: 2008-08-18 Completed Date: 2008-10-29 Revised Date: 2011-06-17 |
Medline Journal Info:
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Nlm Unique ID: 9413298 Medline TA: Bioorg Med Chem Country: England |
Other Details:
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Languages: eng Pagination: 7698-704 Citation Subset: IM |
Affiliation:
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Department of Biomolecular Science, Faculty of Engineering, Gifu University, Medical Information Sciences, Gifu University, 1-1 Yanagido, Gifu 501-1193, Japan. uenoy@gifu-u.ac.jp |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Blotting, Western Cholesterol / chemistry, pharmacology Endoribonucleases / metabolism Hela Cells Humans Lipids / chemical synthesis, chemistry*, pharmacology Magnetic Resonance Spectroscopy Oleic Acids / chemistry, pharmacology Palmitic Acids / chemistry, pharmacology RNA Interference RNA, Small Interfering / chemical synthesis*, chemistry*, genetics, pharmacology Transfection |
| Chemical | |
Reg. No./Substance:
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0/Lipids; 0/Oleic Acids; 0/Palmitic Acids; 0/RNA, Small Interfering; 57-88-5/Cholesterol; EC 3.1.-/Endoribonucleases; EC 3.1.26.-/2-5A-dependent ribonuclease |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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