Citation: Xiao-Feng Wang, Xian-Tao Yang, Yue Chen, Yang Liu, Lang Zou, Zhen-Jun Yang, Li-He Zhang. Solid phase synthesis of peptide-siRNA conjugates containing disulfide bond unit[J]. Chinese Chemical Letters, ;2013, 24(10): 873-876. shu

Solid phase synthesis of peptide-siRNA conjugates containing disulfide bond unit

1.
State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China

Corresponding author: Zhen-Jun Yang,
Received Date: 8 April 2013
Available Online: 28 May 2013
Fund Project:

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.
- siRNA,
- Solid synthesis,
- Disulfide bond,
- Peptide,
- Conjugate
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