# US 5,707,866 A · DNA oligomers for inhibition of HIV by decreasing ribosomal frameshifting

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- Number: US 5,707,866 A
- Document ID: US5707866A
- Status: Granted
- Kind: A
- Application number: 08/651,835
- Filed: 1996-05-21
- Granted: 1998-01-13
- Earliest claimed: 1994-03-30
- Assignees: Universite de Montreal
- Inventors: Lea Brakier-Gingras; Pierre Melan.cedilla.on; Marc Cote; Catherine Payant
- Web page: https://patentgrep.com/patent/US5707866A

## CPC

- C12N 15/113: Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; {Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing (when used in plants C12N15/8218)}
- A61K 38/00: Medicinal preparations containing peptides (peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00)
- C12N 2310/3125: Methylphosphonates
- C12N 2310/321: 2'-O-R Modification
- C12N 2310/322: 2'-R Modification
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)

## Abstract

The invention relates to the use of antisense DNA oligomers to decrease the occurrence of ribosomal frameshifting required for the production of HIV enzymatic proteins when translating HIV messenger RNA, which should interfere with the production of virions and disrupt HIV life cycle. The antisense DNA oligomers are complementary to regions of the RNA of the small ribosomal subunit of mammalian cells, which are involved in the control of translation fidelity.

## Claims

### Claim 1

An antisense DNA oligomer which is complementary to the region of the human 18 S rRNA consisting of nucleotides 595 to 641, wherein said oligomer decreases the occurrence of ribosomal frameshifting and inhibits the expression of HIV enzymatic proteins.

### Claim 2 (depends on 1)

The antisense DNA oligomer of claim 1 having a sequence selected from the group consisting of SEQ ID NO:3, SEQ D NO:4, SEQ ID NO:5, SEQ ID NO:6, and SEQ ID NO:7.

### Claim 3

An antisense oligomer having the sequence of SEQ ID NO:9.

### Claim 4 (depends on 1)

A composition which inhibits HIV in cell culture comprising an antisense DNA oligomer of claim 1 and a pharmaceutically acceptable carrier.

### Claim 5 (depends on 4)

A method of inhibiting HIV in cell culture comprising administering the composition of claim 4.