IP Library › Granted Patent US 10,669,312
Granted Patent B2
US 10,669,312 · App. 15/875,669 · Granted Jun 2, 2020

Peptide for suppressing osteoclast differentiation and use thereof

Inventors: Yong-Ji Chung (Yongin-si, KR); Eun-Mi Kim (Gunpo-si, KR); Eung-Ji Lee (Anyang-si, KR); Tae-Hoon Lee (Sangju-si, KR); A-Reum Han (Icheon-si, KR)
Assignee: CAREGEN CO., LTD.
C07K7/08C07K14/5403A61K38/00
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Quick Facts
Patent No.
US 10,669,312
App. No.
15/875,669
Granted
Jun 2, 2020
Kind
B2
Abstract

The peptide of the present invention performs a function, which is the same as or similar to that of natural interleukin (IL)-3, and has superior skin permeability due to the small size thereof. In addition, the peptide of the present invention suppresses the activation of NF-κB and nuclear transition by inhibiting the receptor activator of nuclear factor kappa-B ligand (RANKL)-RANK signaling pathway, and suppresses the expression of a RANKL or an inflammatory cytokine-induced tartrate-resistant acid phosphatase (TRAP), cathepsin K, or TNF receptor type 1 or type 2, thereby inhibiting osteoclast differentiation depending on the treatment concentration. Moreover, the peptide of the present invention can contribute to osteoblast differentiation by promoting the expression of osteoblast differentiation markers such as osteocalcin (OCN), osteoprotegerin (OPG), bone sialoprotein (BSP), or osteopontin (OPN). Therefore, the superior activity and stability of the peptide of the present invention are useful for medicines, sanitary aids, or cosmetics.

Claims (12)

1. A peptide consisting of the amino acid sequence of SEQ ID NO: 2.

2. The peptide of claim 1 , wherein the peptide inhibits the receptor activator of nuclear factor kappa-B ligand (RANKL)-RANK signaling pathway.

3. The peptide of claim 1 , wherein the peptide inhibits RANKL- or inflammatory cytokine-induced osteoclast differentiation.

4. The peptide of claim 1 , wherein the peptide inhibits the RANKL- or inflammatory cytokine-induced expression of tartrate-resistant acid phosphatase (TRAP), cathepsin K, or type 1 or type 2 TNF receptor.

5. The peptide of claim 3 , wherein the inflammatory cytokine includes tumor necrosis factor-α (TNF-α), macrophage colony-stimulating factor (M-CSF), interleukin-1β (IL-1β), IL-6 or IL-7.

6. The peptide of claim 1 , wherein the peptide promotes osteoblast differentiation.

7. The peptide of claim 1 , wherein the N- or C-terminal of the peptide is linked to a protective group selected from the group consisting of an acetyl group, a fluorenyl methoxy carbonyl group, a formyl group, a palmitoyl group, a myristyl group, a stearyl group and polyethylene glycol (PEG).

8. A peptide consisting of the amino acid sequence of SEQ ID NO: 2, wherein a protective group selected from the group consisting of an acetyl group, a fluorenyl methoxy carbonyl group, a formyl group, a palmitoyl group, a myristyl group, a stearyl group, and polyethylene glycol (PEG), is linked to C-terminus of the peptide.

9. A peptide consisting of the amino acid sequence of SEQ ID NO: 2, wherein a protective group selected from the group consisting of an acetyl group, a fluorenyl methoxy carbonyl group, a formyl group, a palmitoyl group, a myristyl group, a stearyl group, and polyethylene glycol (PEG), is linked to the N-terminus of the peptide.

10. A pharmaceutical composition comprising the peptide of claim 1 .

11. A pharmaceutical composition comprising the peptide of claim 8 .

12. A pharmaceutical composition comprising the peptide of claim 9 .

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 8, 2018
From: CHUNG, YONG JI; KIM, EUN MI; LEE, EUNG-JI; LEE, TAE-HOON; HAN, A REUM
To: CAREGEN CO., LTD.
Reel/Frame 044875/0904 →
Priority Claims (1)
KR 10-2013-0086939 · Jul 23, 2013 · national
Continuity (2)
Division 14906829
Related Publication 20180170966A1 · Jun 21, 2018