# US 7,608,411 B2 · Prostaglandin receptor EP1

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- Number: US 7,608,411 B2
- Document ID: US7608411B2
- Status: Granted
- Kind: B2
- Application number: 11/470,213
- Filed: 2006-09-05
- Published: 2007-01-11
- Granted: 2009-10-27
- Earliest claimed: 2001-03-23
- Assignees: Ono Pharmaceutical Co., Ltd.
- Inventors: Hisao Tajima
- Web page: https://patentgrep.com/patent/US7608411B2

## CPC

- G01N 33/88: involving prostaglandins {or their receptors}
- A61P 13/02: of urine or of the urinary tract, e.g. urine acidifiers
- A61P 25/04: Centrally acting analgesics, e.g. opioids
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07K 14/72: for hormones {(for neuromediators C07K14/70571)}
- C07K 16/2869: {against hormone receptors (for antibodies against neuromediator receptors C07K16/286)}
- 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)
- A61K 2039/505: {comprising antibodies}
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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)

## Abstract

(1) A novel polypeptide prostaglandin E receptor, (2) a cDNA encoding the polypeptide and a fragment selectively hybridized to the sequence of the cDNA, (3) a replication or expression vector carrying the DNA, (4) a host cell transformed with the replication or the expression vector, (5) a method for producing the polypeptide which comprises culturing the host cells, (6) a monoclonal or polyclonal antibody against the polypeptide, (7) a pharmaceutical composition containing the polypeptide or the antibody, in association with pharmaceutically acceptable excipient and/or antibody, (8) a screening method for a compound having agonistic or antagonistic activity against EP1, comprising using the polypeptide or the host cell. The polypeptide of the present invention can be used for treating diseases, which is caused by over production of PGE2, such as pain, fever and pollakiuria.

## Claims

### Claim 1

A method for screening a compound for antagonistic activity against EP1, comprising the steps of:
(1) contacting a test compound with a cell expressing a polypeptide comprising the amino acid sequence of SEQ ID NO: 1 in the presence of at least 10 nM of PGE2;
(2) detecting intracellular Ca2+ concentration in the cell expressing said polypeptide in the presence and absence of said test compound,
wherein when the intracellular Ca2+ concentration in the presence of said test compound is reduced relative to the intracellular Ca2+ concentration in the absence of said test compound, said test compound is an antagonist of EP1.

### Claim 2 (depends on 1)

The method according to claim 1, wherein said cell is transformed with a replication or expression vector comprising the nucleotide sequence of SEQ ID NO: 2.