Mcgill University

Boehringer Ingelheim (Canada) Ltd.

Michael A Parniak

Masad Jose Damha

Kyung-Lyum Min

Nicolas Paul Sluis-Cremer

Alex Pelletier

Chun-Nam Lok

Ekaterina Vlazovkina

Ekaterina Viazovkina

The invention relates to oligonucleotides having alternating segments of sugar-modified nucleosides and 2'-deoxynucleosides, and uses thereof. The invention further related to oligonucleotides having alternating segments of sugar-modified nucleotides and 2&#x2032;-deoxynucleotides, and uses thereof. Such uses include the preparation of antisense oligonucleotides and their use for the prevention or depletion of function of a target nucleic acid of interest, such as an RNA, in a system. Accordingly, and oligonucleotide of the invention is useful for therapeutic, analytical and diagnostic methods and uses, as well as component of compositions and commercial packages corresponding to such methods and uses.

Oligonucleotides comprising alternating segments and uses thereof

The invention relates to oligonucleosides having alternating segments of sugar-modified nucleosides and 2'-deoxynucleosides, and uses thereof. The invention further relates to oligonucleotides having alternating segments of sugar-modified nucleotides and 2&#x2032;-deoxynucleotides, and uses thereof. Such uses include the preparation of antisense oligonucleotides and their use for the prevention or depletion of function of a target nucleic acid of interest, such as an RNA, in a system. Accordingly, an oligonucleotide of the invention is useful for therapeutic, analytical and diagnostic methods and uses, as well as a component of compositions and commercial packages corresponding to such methods and uses.

The present invention relates to novel oligonucleotide chimera used as therapeutic agents to selectively prevent gene transcription and expression in a sequence-specific manner. In particular, this invention is directed to the selective inhibition of protein biosynthesis via antisense strategy using oligonucleotides constructed from arabinonucleotide or modified arabinonucleotide residues, flanking a series of deoxyribose nucleotide residues of variable length. Particularly this invention relates to the use of antisense oligonucleotides constructed from arabinonucleotide or modified arabinonucleotide residues, flanking a series of deoxyribose nucleotide residues of variable length, to hybridize to complementary RNA such as cellular messenger RNA, viral RNA, etc. More particularly this invention relates to the use of antisense oligonucleotides constructed from arabinonucleotide or modified arabinonucleotide residues, flanking a series of deoxyribose nucleotide residues of variable length, to hybridize to and induce cleavage of (via RNaseH activation) the complementary RNA.

Chimeric antisense oligonucleotides of arabinofuranose analogue and deoxyribose nucleotides

The invention relates to a substrate and method for the assay of ribonuclease H activity. The substrate comprises a DNA/RNA heteroduplex molecule having fluorophore and quencher molecules in close proximity, which emit a background level of fluorescence in the absence of ribonuclease H activity due to quenching of the fluorophore as a result of fluorescence resonance energy transfer. Ribonuclease H cleavage of the heteroduplex results in an increase in fluorescence emission due to the destabilization and separation of the DNA and RNA molecules and their associated fluorophore and quencher molecules. The assay method of the present invention is suitable for use in screening (e.g. high throughput screening) for modulators, e.g. inhibitors, of the ribonuclease H activity associated with, for example, reverse transcriptase and ribonuclease H enzymes.

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Pittsburgh, PA, United States of America

Michael A Parniak