# US 7,612,043 B2 · Method of reducing or inhibiting ObR signaling using a leptin antagonist consisting of SEQ id No: 2

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- Number: US 7,612,043 B2
- Document ID: US7612043B2
- Status: Granted
- Kind: B2
- Application number: 12/157,127
- Filed: 2008-06-06
- Published: 2009-01-29
- Granted: 2009-11-03
- Earliest claimed: 2004-05-07
- Assignees: Boston Biomedical Research Institute
- Inventors: Ruben Rene Gonzalez; Paul C. Leavis
- Web page: https://patentgrep.com/patent/US7612043B2

## CPC

- C07K 14/5759: {Products of obesity genes, e.g. leptin, obese (OB), tub, fat}
- A61K 38/2264: {Obesity-gene products, e.g. leptin}
- G01N 33/5041: {involving analysis of members of signalling pathways}
- G01N 33/74: involving hormones {or other non-cytokine intercellular protein regulatory factors such as growth factors, including receptors to hormones and growth factors}
- C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00)
- 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)
- G01N: INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES (measuring or testing apparatus or processes other than immunoassay, involving enzymes or microorganisms C12M, C12Q)

## Abstract

Disclosed herein are peptides comprising a leptin sequence and methods for their use in preventing ObR signaling in a leptin-responsive cell. A leptin peptide of the present invention binds to but does not activate ObR signaling in a leptin-responsive cell, thereby inhibiting the up-regulatory effects of leptin on ObR signaling in the leptin-responsive cell. Administration of the peptide effectively prevents embryo implantation in a mammal to which the peptide has been administered. Also disclosed herein is a method for identifying a peptide antagonist of ObR, wherein the peptide comprises a leptin sequence.

## Claims

### Claim 1

A method for reducing or inhibiting ObR signaling in a leptin-responsive cell, the method comprising administering to a mammal a therapeutically effective amount of a peptide consisting of SEQ ID NO.: 2.

### Claim 2 (depends on 1)

The method of claim 1 wherein the mammal is selected from the group consisting of humans, mice, and rabbits.

### Claim 3 (depends on 1)

The method of claim 1 wherein the administration of the peptide results in the reduction of the likelihood of embryo implantation.

### Claim 4 (depends on 1)

The method of claim 1 wherein the reduction or inhibition of ObR signaling in the cell results in a reduction or inhibition of the up-regulatory effects of leptin on a signaling event downstream of ObR.

### Claim 5 (depends on 4)

The method of claim 4 wherein the signaling event downstream of the leptin receptor consists of p-Stat-3, β3-integrin, IL-1 and LIF signaling.

### Claim 6 (depends on 1)

The method of claim 1 wherein the reduction or inhibition of ObR signaling results in a reduction or inhibition of the up-regulatory effects of leptin on the expression of a leptin-sensitive target.

### Claim 7 (depends on 6)

The method of claim 6 wherein the leptin-sensitive target is selected from the group consisting of p-Stat-3, β3-integrin, IL-1R tI, LIF-R, LIF, IL-1β, and IL-1Ra.