Studies on aminoisonucleoside modified siRNAs: stability and silencing activity.
A novel class of aminoisonucleoside was synthesized and incorporated into a luciferase gene-targeting siRNA. Structural and functional analyses of such a kind of siRNAs indicated that sense strand modifications with aminoisonucleoside at the 3' or 5' terminal, such as ssIso-1 and ssIso-2, have less effect on RNA duplex thermal and serum stabilities, and their functional activities are also comparable to their native siRNAs. In contrast, antisense strand modifications with aminoisonucleoside at the corresponding positions, such as asIso-2 or asIso-1, bring a striking negative effect on RNA duplex stability but still maintain around 40-50% of gene knockdown.
Li
Zong-Sheng
ZS
State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing, China.
Qiao
Ren-Ping
RP
Du
Quan
Q
Yang
Zhen-Jun
ZJ
Zhang
Liang-Ren
LR
Zhang
Pei-Zhuo
PZ
Liang
Zi-Cai
ZC
Zhang
Li-He
LH
D002460:Cell Line; D006358:Hot Temperature; D006801:Humans; D008156:Luciferases / Q000378:metabolism; D009705:Nucleosides / Q000737:chemistry*; D034622:RNA Interference; D034741:RNA, Small Interfering / Q000138:chemical synthesis* / Q000737:chemistry / Q000502:physiology
D009705:Nucleosides; D034741:RNA, Small Interfering; D008156:Luciferases