# US 2010/0167390 A1 · Novel Oligonucleotide and NF-kB Decoy Comprising the Same

> Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt

- Number: US 2010/0167390 A1
- Document ID: US20100167390A1
- Status: Published application
- Kind: A1
- Application number: 12/086,923
- Filed: 2006-12-21
- Published: 2010-07-01
- Earliest claimed: 2005-12-22
- Inventors: Toshohiro Nakajima; Akiko Temma; Naho Suzuki
- Web page: https://patentgrep.com/patent/US20100167390A1

## CPC

- C12N 15/115: Aptamers, i.e. nucleic acids binding a target molecule specifically and with high affinity without hybridising therewith {; Nucleic acids binding to non-nucleic acids, e.g. aptamers}
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 3/04: Anorexiants; Antiobesity agents
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 11/06: Antiasthmatics
- A61P 13/00: Drugs for disorders of the urinary system
- A61P 13/12: of the kidneys
- A61P 17/00: Drugs for dermatological disorders
- A61P 17/02: for treating wounds, ulcers, burns, scars, keloids, or the like
- A61P 17/06: Antipsoriatics
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 19/08: for bone diseases, e.g. rachitism, Paget's disease
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 35/00: Antineoplastic agents
- A61P 35/04: specific for metastasis
- A61P 37/00: Drugs for immunological or allergic disorders
- A61P 37/02: Immunomodulators
- A61P 37/08: Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14)
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- 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)}
- C12N 2310/13: Decoys
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

A novel oligonucleotide useful as an NF-κB decoy having a higher binding ability to NF-κB than known NF-κB decoy as well as the medical uses thereof, is disclosed. The oligonucleotide of the invention has a base sequence having a consensus sequence and specific 5′-flanking and 3′-flanking sequences ligated to both ends of the consensus sequence, respectively. The NF-κB decoy is constituted by an oligonucleotide which is the above-described oligonucleotide of the invention and which is substantially double-stranded wherein the strands are complementary to each other.

## Claims

### Claim at position 1

1-28. (canceled)

### Claim 29

An oligonucleotide having a base sequence represented by Formula (I):
A-X—B (I)
wherein X is a consensus sequence comprising either gggatttccc (SEQ ID NO:1) or gggactttcc (SEQ ID NO:2);
A is a 5′-flanking sequence selected from the group consisting of: cgc; ccc; gga; cgca; ccct; and ggct; and
B is a 3′-flanking sequence selected from the group consisting of: agc; acc; ggg: gcg; gcc; and gcgg.

### Claim 30 (depends on 29)

The oligonucleotide of claim 29, wherein said consensus sequence is gggatttccc (SEQ ID NO:1).

### Claim 31 (depends on 30)

The oligonucleotide of claim 30, wherein said base sequence is selected from the group consisting of: cgcgggatttcccagc (SEQ ID NO:3); cccgggatttcccacc (SEQ ID NO:4); ggagggatttcccggg (SEQ ID NO:5); cgcagggatttcccgcg (SEQ ID NO:6); ccctgggatttcccgcc (SEQ ID NO:7); and ggctgggatttcccgcgg (SEQ ID NO:8).

### Claim 32 (depends on 29)

The oligonucleotide of claim 29, wherein said oligonucleotide is double-stranded and the strands in said oligonucleotide are complementary to each other.

### Claim 33 (depends on 29)

The oligonucleotide of claim 29, wherein the bond between at least two adjacent nucleotides is modified by a nuclease-resistant modification.

### Claim 34 (depends on 33)

The oligonucleotide of claim 33, wherein said oligonucleotide is double-stranded, the strands in said oligonucleotide are complementary to each other, and both of the strands in said oligonucleotide are modified by said nuclease-resistant modification.

### Claim 35 (depends on 33)

The oligonucleotide of claim 33, wherein at least the bonds between all of the nucleotides constituting said consensus sequence are modified by said nuclease-resistant modification.

### Claim 36 (depends on 35)

The oligonucleotide of claim 35, wherein the bonds between all nucleotides are modified by said nuclease-resistant modification.

### Claim 37 (depends on 35)

The oligonucleotide of claim 35, wherein the bonds between all of the nucleotides constituting said consensus sequence are modified by said nuclease-resistant modification, and the bonds between all of other nucleotides are not modified.

### Claim 38 (depends on 33)

The oligonucleotide of claim 33, wherein said nuclease-resistant modification is phosphorothioation.

### Claim 39

An oligonucleotide decoy for a transcription factor, comprising an oligonucleotide which is substantially double-stranded, wherein the strands in said oligonucleotide are complementary to each other and said oligonucleotide comprises a core sequence and one or more flanking sequences ligated to one or both ends of said core sequence, wherein the bonds between only all of the nucleotides constituting said core sequence are modified by a nuclease-resistant modification and the bonds between all of other nucleotides are not modified.

### Claim 40 (depends on 39)

The oligonucleotide decoy of claim 39, wherein said nuclease-resistant modification is phosphorothioation.

### Claim 41 (depends on 29)

A method for inhibiting NF-κB, said method comprising bringing the oligonucleotide of claim 29 into contact with NF-κB, said oligonucleotide being substantially double-stranded and wherein the strands of said oligonucleotide are complementary to each other.

### Claim 42

A method for inhibiting a transcription factor, comprising contacting said transcription factor with an effective amount of an oligonucleotide decoy for the transcription factor, said oligonucleotide decoy comprising an oligonucleotide having a core sequence and one or more flanking sequences ligated to one or both ends of said core sequence, wherein the bonds between all of the nucleotides constituting said core sequence are modified by a nuclease-resistant modification, and the bonds between all of other nucleotides are not modified.

### Claim 43 (depends on 42)

The method of claim 42, wherein said oligonucleotide is completely double-stranded.

### Claim 44 (depends on 43)

The method of claim 43, wherein said oligonucleotide binds to at least one molecular species selected from the group consisting of p65, p50, p52 and Rel-B proteins.