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Lysophosphatidic acid receptor

Foreign code F110005198
File No. A141-03US
Posted date Aug 25, 2011
Country United States of America
Application number 54221703
Gazette No. 20060264361
Gazette No. 7666611
Date of filing Dec 17, 2003
Gazette Date Nov 23, 2006
Gazette Date Feb 23, 2010
International application number JP2003016176
International publication number WO2004063224
Date of international filing Dec 17, 2003
Date of international publication Jul 29, 2004
Priority data
  • P2003-007657 (Jan 15, 2003) JP
  • 2003WO-JP16176 (Dec 17, 2003) WO
Title Lysophosphatidic acid receptor
Abstract (US7666611)
It is intended to provide a novel receptor of LPA and a method of screening a drug such as an LPA receptor antagonist using the same.
Use as a lysophosphatidic acid (LPA) receptor comprising a G protein-coupled protein p2y9.
More specifically, use of the G protein-coupled protein p2y9 as a lysophosphatidic acid (LPA) receptor.
A method of screening an agonist or an antagonist to the LPA receptor as described above by using the receptor.
Scope of claims [claim1]
1. A method of screening for a candidate compound that acts as an agonist of a G protein-coupled receptor p2y9, comprising: (a) preparing a first group and a second group of cells that express the G protein-coupled receptor p2y9 on the cell surfaces;
(b) adding LPA to the cell surfaces of the first group of cells;
(c) monitoring an intracellular activity in the first group of cells, said intracellular activity being associated with binding of LPA to p2y9;
(d) adding said candidate compound to the second group of cells;
(e) monitoring an intracellular activity in the second group of cells, said intracellular activity being the same as the intracellular activity of step (c);
(f) comparing the intracellular activity in step (c) with the intracellular activity in step (e); and
(g) determining whether said candidate compound is an agonist of the G protein-coupled receptor p2y9 based on the comparison in step (f),
wherein said G protein-coupled receptor p2y9 comprises seven transmembrane regions, and
wherein said G protein-coupled receptor p2y9 comprises an amino acid sequence represented by SEQ ID NO: 1.
[claim2]
2. The method according to claim 1, wherein the monitoring the intracellular activity in steps (c) and (e) comprises detecting calcium concentration in the cells.
[claim3]
3. The method according to claim 1, wherein the monitoring the intracellular activity in steps (c) and (e) comprises detecting cAMP concentration in the cells.
[claim4]
4. A method of screening for a candidate compound that acts as an antagonist of a G protein-coupled receptor p2y9, comprising: (a) preparing a first group and a second group of cells that express the G protein-coupled receptor p2y9 on the cell surfaces;
(b) adding LPA to the cell surfaces of the first group of cells;
(c) monitoring an intracellular activity in the first group of cells, said intracellular activity being associated with binding of LPA to p2y9;
(d) adding said candidate compound and LPA to the second group of cells;
(e) monitoring an intracellular activity in the second group of cells, said intracellular activity being the same as the intracellular activity of step (c);
(f) comparing the intracellular activity in step (c) with the intracellular activity in step (e); and
(g) determining whether said candidate compound is an antagonist of the G protein-coupled receptor p2y9 based on the comparison in step (f),
wherein said G protein-coupled receptor p2y9 comprises seven transmembrane regions. and
wherein said G protein-coupled receptor p2y9 comprises an amino acid sequence represented by SEQ ID NO: 1.
[claim5]
5. The method according to claim 4, wherein the monitoring the intracellular activity in steps (c) and (e) comprises detecting calcium concentration in the cells.
[claim6]
6. The method according to claim 4, wherein the monitoring the intracellular activity in steps (c) and (e) comprises detecting cAMP concentration in the cells.
[claim7]
7. The method according to claim 4, wherein the candidate compound is an inhibitor of carcinoma cell invasion.
[claim8]
8. A method of screening for a candidate compound that acts as an inhibitor of binding of LPA to G protein-coupled receptor p2y9, comprising: (a) preparing a plurality of groups of cells that express the G protein-coupled receptor p2y9 on the cell surfaces;
(b) adding (1) the candidate compound and (2) labeled LPA to each of said plurality of groups of cells that express the G protein-coupled receptor p2y9 on the cell surfaces, said candidate compound being added in a different concentration to each of said plurality of groups of cells that express the G protein-coupled receptor p2y9 on the cell surfaces,
(c) detecting activity of said labeled LPA bound to the G protein-coupled receptor p2y9 in each of said plurality of groups of cells that express the G protein-coupled receptor p2y9 on the cell surfaces, and
(d) determining that said candidate compound is an inhibitor of binding of LPA to G protein-coupled receptor p2y9 when the activity detected in step (c) decreases dose-dependently with the candidate compound among said plurality of groups of cells that express the G protein-coupled receptor p2y9 on the cell surfaces,
wherein said G protein-coupled receptor p2y9 comprises seven transmembrane regions, and
wherein said G protein-coupled receptor p2y9 comprises an amino acid sequence represented by SEQ ID NO: 1.
[claim9]
9. The method according to claim 8, wherein said inhibitor of binding of LPA to G protein-coupled receptor p2y9 is an agonist candidate of G protein-coupled receptor p2y9.
[claim10]
10. The method according to claim 8, wherein said inhibitor of binding of LPA to G protein-coupled receptor p2y9 is an antagonist candidate of G protein-coupled receptor p2y9.
  • Inventor, and Inventor/Applicant
  • SHIMIZU TAKAO
  • ISHII SATOSHI
  • NOGUCHI KYOKO
  • JAPAN SCIENCE AND TECHNOLOGY AGENCY
IPC(International Patent Classification)
Reference ( R and D project ) CREST Understanding the Brain AREA
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