Aptamer which selectively binds to ERBB2 receptor and uses thereof

Patent metadata

Field	Value
Publication number	US-9309515-B2
Application number	US-201114128152-A
Country	US
Kind code	B2
Filing date	Aug 10, 2011
Priority date	Jun 24, 2011
Publication date	Apr 12, 2016
Grant date	Apr 12, 2016

Abstract

Disclosed are a DNA aptamer specifically binding to the Her2 (ERBB2) receptor involved in the onset of breast cancer, a composition for the suppression of cancer metastasis comprising the same as an active ingredient, and a composition for the diagnosis of cancer comprising the same as an active ingredient. Due to its binding mechanism being different from that of the conventional antibody, the aptamer can be effectively used for suppressing cancer metastasis and diagnosing cancer.

First claim

What is claimed is:

1. An ERBB2 aptamer, which specifically binds to ERBB2, and comprises 40 to 100 nucleotides comprising a nucleotide sequence selected from the group consisting of SEQ ID NOS: 1 to 35.

2. The ERBB2 aptamer of claim 1 , wherein the ERBB2 aptamer comprises of 40 to 100 nucleotides comprising the nucleotide sequence of SEQ ID NO: 7 or SEQ ID NO: 11.

3. The ERBB2 aptamer of claim 1 , wherein the ERBB2 aptamer further comprises 15 to 30 nucleotides at either or both of 5′ and 3′ termini of the nucleotide sequence selected from the group consisting of SEQ ID NOS: 1 to 35.

4. The ERBB2 aptamer of claim 1 , wherein the ERBB2 aptamer is modified by being conjugated with at least one selected from the group consisting of PEG (polyethylene glycol), idT (inverted deoxythymidine), LNA (Locked Nucleic Acid), 2′-methoxy nucleoside, 2′-amino nucleoside, 2′F-nucleoside, an amine linker, a thiol linker, and a cholesterol, at either or both of 5′ and 3′ termini thereof.

5. A pharmaceutical composition, comprising the ERBB2 aptamer of claim 1 as an active ingredient.

6. The pharmaceutical composition of claim 5 , wherein the pharmaceutical composition is for treatment of cancer.

7. The pharmaceutical composition of claim 6 , wherein the cancer is selected from the group consisting of breast cancer, colorectal cancer, lung cancer, gallbladder cancer, pancreatic cancer, and stomach cancer.

8. The pharmaceutical composition of claim 5 , wherein the pharmaceutical composition is for diagnosis of cancer.

9. A method for treating cancer, comprising administering the ERBB2 aptamer of claim 1 to a subject in need of treating cancer.

10. The method of claim 9 , wherein the ERBB2 aptamer comprises 40 to 100 nucleotides comprising the nucleotide sequence of SEQ ID NO: 7 or SEQ ID NO: 11.

11. The method of claim 9 , wherein the ERBB2 aptamer further comprises 15 to 30 nucleotides at either or both of 5′ and 3′ termini of the nucleotide sequence selected from the group consisting of SEQ ID NOS: 1 to 35.

12. The method of claim 9 , wherein the ERBB2 aptamer is modified by being conjugated with at least one selected from the group consisting of PEG (polyethylene glycol), idT (inverted deoxythymidine), LNA (Locked Nucleic Acid), 2′-methoxy nucleoside, 2′-amino nucleoside, 2′F-nucleoside, an amine linker, a thiol linker, and a cholesterol, at either or both of 5′ and 3′ terminus thereof.

13. The method of claim 9 , wherein the cancer is selected from the group consisting of breast cancer, colorectal cancer, lung cancer, gallbladder cancer, pancreatic cancer, and stomach cancer.

14. A method for cancer diagnosis, comprising:
providing a biological specimen of a subject;
reacting the biological specimen with the ERBB2 aptamer of claim 1 ; and
measuring a binding level of the ERBB2 aptamer in the biological specimen,
wherein when the binding level of the ERBB2 aptamer in the biological sample is higher than that in a normal specimen, the subject is determined as a cancer patient.

Assignees

• Lee Jung Hwan
• Chae Young Chan
• Kim Youngdong
• Kang Hyungu
• Im Jong Hun
• Kim Jong In
• Kim Ki Seok
• Jang Sung Key
• Oh Il Ung
• Choi Min Jeong
• Kang Won Jun
• Postech Acad Ind Found
• Korea Food & Drug Admin

Inventors

• Lee Jung Hwan
• Chae Young Chan
• Kim Youngdong
• Kang Hyungu
• Im Jong Hun
• Kim Jong In
• Kim Ki Seok
• Jang Sung Key
• Oh Il Ung
• Choi Min Jeong
• Kang Won Jun

Classifications

• C12N2310/3535

  Nitrogen · CPC title

• C12N2320/30

  Special therapeutic applications · CPC title

• A61P35/00

  Antineoplastic agents · CPC title

• A61K31/7088

  Compounds having three or more nucleosides or nucleotides · CPC title

• G01N2333/71

  for growth factors; for growth regulators · CPC title