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

Xiao-Feng Wang Xian-Tao Yang Yue Chen Yang Liu Lang Zou Zhen-Jun Yang Li-He Zhang

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

    通讯作者: Zhen-Jun Yang,
  • 基金项目:

    assistance with biological assay experiments. This work was supported by the National Natural Science Foundation of China (No. 20932001)  (No. 20932001)

    Technology of China (Nos. 2012CB720604, 2012AA022501). (Nos. 2012CB720604, 2012AA022501)

摘要: 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 () maintained good gene silencing activity, while that of the 3'-antisense strand conjugate decreased somewhat. And the sense strand off-target effect of decreased remarkably.

English

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  • 收稿日期:  2013-04-08
  • 网络出版日期:  2013-05-28
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