Endogenous and non-endogenous versions of human G protein-coupled receptors

• US 7,119,190 B2
• Filed: 02/26/2002
• Issued: 10/10/2006
• Est. Priority Date: 04/14/1997
• Status: Expired due to Fees

• Current Assignee: Arena Pharmaceuticals Incorporated (Pfizer Inc.)
• Original Assignee: Arena Pharmaceuticals Incorporated (Pfizer Inc.)
• Inventors: Ortuño, Daniel, Liaw, Chen W., Lin, I-Lin, Leonard, James N., Chalmers, Derek T., Behan, Dominic P., Maciejewski-Lenior, Dominique
• Primary Examiner(s): Andres, Janet L.
• Assistant Examiner(s): BASI, NIRMAL SINGH
• Application Number:
  US10/083,168
• Publication Number:
  US 20030023069A1
• Time in Patent Office: 1,687 Days
• Field of Search: 435/69.1, 435/252.3, 435/325, 435/7.1, 530/300, 530/350, 536/23.1, 536/24.31
• US Class Current: 536/23.5
• CPC Class Codes: 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
• CPC Class Codes: C07D 231/12 with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
• CPC Class Codes: C07D 231/16 Halogen atoms or nitro radicals
• CPC Class Codes: C07D 409/12 linked by a chain containing hetero atoms as chain links
• CPC Class Codes: C07K 14/705 Receptors; Cell surface antigens; Cell surface determinants tumour specific antigens C07K14/4748
• CPC Class Codes: C07K 14/70571 for neuromediators, e.g. serotonin receptor, dopamine receptor
• CPC Class Codes: C07K 14/723 G protein coupled receptor, e.g. TSHR-thyrotropin-receptor, LH/hCG receptor, FSH receptor
• CPC Class Codes: G01N 2333/70571 for neuromediators, e.g. serotonin receptor, dopamine receptor
• CPC Class Codes: G01N 2333/726 G protein coupled receptor, e.g. TSHR-thyrotropin-receptor, LH/hCG receptor, FSH
• CPC Class Codes: G01N 33/566 using specific carrier or receptor proteins as ligand binding reagents where possible specific carrier or receptor proteins are classified with their target compounds

Abstract

The invention disclosed in this patent document relates to transmembrane receptors, more particularly to a human G protein-coupled receptor and to mutated (non-endogenous) versions of the human GPCRs for evidence of constitutive activity.

Claims

1. An isolated polynucleotide encoding a non-endogenous, constitutively activated version of a wild-type G protein-coupled receptor, wherein the wild-type G protein-coupled receptor comprises SEQ. ID.:

16 and wherein said non-endogenous constitutively activated version contains a mutation of an amino acid residue located 16 amino acid residues from a proline residue in TM6.

4. A vector comprising a polynucleotide according to any one of claims 1 to 3.

5. A vector according to claim 4, wherein said vector is an expression vector.

6. A host cell comprising an expression vector according to claim 5.

7. A process for making a recombinant host cell comprising the steps of:

(a) transfecting an expression vector according to claim 5 into a suitable host cell; and

(b) culturing the host cell under conditions which allow expression of a G protein-coupled receptor from the expression vector.

8. A membrane of a recombinant host cell produced by the process of claim 7 comprising said G protein-coupled receptor.

2. An isolated polynucleotide encoding a non-endogenous, constitutively activated version of a wild-type G protein-coupled receptor, wherein the wild-type G protein-coupled receptor comprises SEQ. ID. NO.:

16, and wherein said polynucleotide encodes an amino avid sequence that comprises.

3. An isolated polynucleotide according to claim 2, wherein the polynucleotide comprises.