Three component chimeric antisense oligonucleotides

Chemistry: molecular biology and microbiology – Animal cell – per se ; composition thereof; process of... – Method of regulating cell metabolism or physiology

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435 6, 435 911, 536 231, 536 243, 536 2433, 536 245, C07H 2104, C12N 1500, C12Q 168

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active

059899123

ABSTRACT:
This invention relates to antisense oligonucleotides that target mRNAs in cells as substrates for the cellular enzyme RNase H and thereby cause specific degradation of the targeted mRNA. The oligonucleotides have three components: a RNase H activating region, a complementarity region and 3' and 5' ends. The invention optimizes each of the components to resist intracellular nucleases, to increase hybridization to target mRNA, to specifically inactivate target mRNA in cells, and to decrease cytotoxicity.

REFERENCES:
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patent: 5652356 (1997-07-01), Agrawal
De Mesmaeker et al., Current Opinion in Structural Biology, 5:343-355 (1995).
Gerwitz et al., Science, 93:3161-3163 (1966).
Moulds et al., Biochemistry 34:5044-5053 (1995).

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