Biodistribution of phosphodiester and phosphorothioate siRNA

被引:198
作者
Braasch, DA
Paroo, Z
Constantinescu, A
Ren, G
Öz, OK
Mason, RP
Corey, DR
机构
[1] Univ Texas, SW Med Ctr, Dept Pharmacol, Dallas, TX 75390 USA
[2] Univ Texas, SW Med Ctr, Dept Biochem, Dallas, TX 75390 USA
[3] Univ Texas, SW Med Ctr, Dept Radiol, Dallas, TX 75390 USA
关键词
siRNA; phosphorothioate; biodistribution; planar imaging;
D O I
10.1016/j.bmcl.2003.12.074
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Short interfering RNAs (siRNAs) are valuable tools for analyzing protein function in mammalian cell culture. This success has led to high expectations for in vivo and therapeutic applications. However, the pharmacokinetic properties of siRNA are not known. Here we report the biodistribution of a phosphodiester (PO) siRNA duplex and examine the effect of phosphorothioate (PS) linkages. Our findings indicate that biodistribution of siRNA is similar to that for single-stranded antisense oligonucleotides and offer insights for use of siRNA in vivo. (C) 2003 Elsevier Ltd. All rights reserved.
引用
收藏
页码:1139 / 1143
页数:5
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