Incorporation of biaryl units into the 5' and 3' ends of sense and antisense strands of siRNA duplexes improves strand selectivity and nuclease resistance

Kayo Yoshikawa; Aya Ogata; Chiho Matsuda; Michinori Kohara; Hideo Iba; Yukio Kitade; Yoshihito Ueno

doi:10.1021/bc100301w

Incorporation of biaryl units into the 5' and 3' ends of sense and antisense strands of siRNA duplexes improves strand selectivity and nuclease resistance

Bioconjug Chem. 2011 Jan 19;22(1):42-9. doi: 10.1021/bc100301w. Epub 2010 Dec 9.

Authors

Kayo Yoshikawa¹, Aya Ogata, Chiho Matsuda, Michinori Kohara, Hideo Iba, Yukio Kitade, Yoshihito Ueno

Affiliation

¹ Department of Biomolecular Science, Faculty of Engineering, Gifu University, 1-1 Yanagido, Gifu 501-1193, Japan.

PMID: 21141919
DOI: 10.1021/bc100301w

Abstract

Small interfering RNA (siRNA) is a noncoding RNA with considerable potential as a new therapeutic drug for intractable diseases. siRNAs can be rationally designed and synthesized if the sequences of the disease-causing genes are known. In this paper, we describe the synthesis and properties of siRNAs modified with biaryl units. We found that incorporation of biaryl units into the 5' and 3' ends of sense and antisense strands of siRNA duplexes improved strand selectivity and nuclease resistance.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Base Sequence
Gene Silencing
Hepacivirus / physiology
Luciferases / genetics
RNA, Antisense / chemistry*
RNA, Antisense / genetics*
RNA, Antisense / metabolism
RNA, Small Interfering / chemistry*
RNA, Small Interfering / genetics*
RNA, Small Interfering / metabolism
Ribonucleases / metabolism*
Virus Replication / genetics

Substances

RNA, Antisense
RNA, Small Interfering
Luciferases
Ribonucleases