Solid phase synthesis of peptide-siRNA conjugates containing disulfide bond unit |
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Authors: | Xiao-Feng Wang Xian-Tao Yang Yue Chen Yang Liu Lang Zou Zhen-Jun Yang Li-He Zhang |
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Institution: | State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China |
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Abstract: | A disulfide-modified nucleoside was designed and synthesized. After loading the modified nucleoside on controlled pore glass (CPG), solid phase synthesis strategy was used to prepare peptide-oligonucleotide conjugates (N-3') containing disulfide bond unit. The 3'-sense strand peptide-siRNA conjugate (Ⅶ) maintained good gene silencing activity, while that of the 3'-antisense strand conjugate decreased somewhat. And the sense strand off-target effect of Ⅶ decreased remarkably. |
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Keywords: | siRNA Solid synthesis Disulfide bond Peptide Conjugate |
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