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Nucleic Acid Ther. 2016 Oct;26(5):327-334. Epub 2016 Jul 25.

Inhibition of miR-21 by 3'/5'-Serinyl-Capped 2'-O-Methyl RNA Interspersed with 2'-O-(2-Amino-3-Methoxypropyl) Uridine Units.

Author information

1
1 Academy of Scientific and Innovative Research (AcSIR) , New Delhi, India .
2
2 CSIR-Institute of Genomics and Integrative Biology , Delhi, India .
3
3 Department of Chemistry, Binghamton University, State University of New York , Binghamton, New York.
4
4 Organic Chemistry Division, CSIR-National Chemical Laboratory , Pune, India .

Abstract

miRNAs are highly conserved class of small ncRNAs whose involvement in human pathophysiologies is extensively investigated. MiR-21 is a well established oncogenic miRNA whose deregulation plays a significant role in onset and progression of cancer. The need of novel approaches to downregulate miR-21 is rapidly expanding. Potent inhibition of miR-21 is achieved by chemically modified 2'-O-methyl RNA oligonucleotide. The serinol capping at 3' and 5'ends and the interspersed 2'-O-(R-2-amino-3-methoxypropyl) uridine units enhance the nuclease resistance and efficacy of 2'-O-methyl RNA for the inhibition of miR-21. This represents a simple and novel modification for developing oligonucleotide-based therapeutics.

KEYWORDS:

antagomirs; cancer; microRNA; noncoding RNA; oligonucleotides

PMID:
27454558
DOI:
10.1089/nat.2015.0591
[Indexed for MEDLINE]

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