Synthesis, RNAi activity and nuclease-resistant properties of apolar carbohydrates siRNA conjugates

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:23

Article

Vengut-Climent, Empar¹  Terrazas, Montserrat²  Lucas, Ricardo¹  Arevalo-Ruiz, Matilde¹  Eritja, Ramon²  Carlos Morales, Juan¹ 

[1] CSIC Univ Sevilla, Inst Invest Quim, Dept Bioorgan Chem, Seville 41092, Spain

[2] CIBER BBN Networking Ctr Bioengn Biomat & Nanomed, CSIC, IQAC, E-08034 Barcelona, Spain

关键词: siRNA;    Modified siRNA;    Phosphoramidite;    Carbohydrate;    Lipophilic vector;   

DOI  :  10.1016/j.bmcl.2013.05.065

来源: Elsevier

【 摘 要 】

Oligoribonucleotide conjugates carrying apolar carbohydrates at the 5'-end and the corresponding siRNA duplexes have been prepared using phosphoramidite chemistry. All the carbohydrate-siRNA derivatives were compatible with RNA interference machinery if transfected with oligofectamine. In the absence of a transfection agent, some of them exerted certain reduction of gene expression. Double-tailed permethylated glucose conjugated to siRNA through a long spacer inhibited gene expression up to 26% compared to the scrambled duplex. Such modifications contribute positively to the stability of oligoribonucleotides against 5'-exonuclease degradation. (C) 2013 Elsevier Ltd. All rights reserved.

【 授权许可】

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