Activity of siRNAs with 2-thio-2'-O-methyluridine modification in mammalian cells

Thazha P Prakash; Nishant Naik; Namir Sioufi; Balkrishen Bhat; Eric E Swayze

doi:10.1080/15257770903316145

Activity of siRNAs with 2-thio-2'-O-methyluridine modification in mammalian cells

Nucleosides Nucleotides Nucleic Acids. 2009 Oct;28(10):902-10. doi: 10.1080/15257770903316145.

Authors

Thazha P Prakash¹, Nishant Naik, Namir Sioufi, Balkrishen Bhat, Eric E Swayze

Affiliation

¹ Department of Medicinal Chemistry, Isis Pharmaceuticals Inc., Carlsbad, California 92008, USA. tprakashn@isisph.com

PMID: 20183560
DOI: 10.1080/15257770903316145

Abstract

In a search to identify chemical modifications to improve the properties of siRNA, we have investigated the effect of the 2 '-O-methyl-2-thiouridine modification on the biological activity of siRNA. Our results indicate that judicious placement of 2 '-O-methyl-2-thiouridine residues could lead to modified siRNA with activity in mammalian cells.

MeSH terms

Cells, Cultured
Drug Design
HeLa Cells
Humans
Oligonucleotides / chemical synthesis
Oligonucleotides / chemistry
Oligonucleotides / metabolism
RNA, Small Interfering / chemistry*
RNA, Small Interfering / genetics
RNA, Small Interfering / metabolism*
Thiouridine / analogs & derivatives*
Thiouridine / chemical synthesis
Thiouridine / chemistry
Thiouridine / metabolism

Substances

2'-O-methyl-2-thiouridine
Oligonucleotides
RNA, Small Interfering
Thiouridine