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Lysophosphatidic acid receptor

外国特許コード F110005198
整理番号 A141-03US
掲載日 2011年8月25日
出願国 アメリカ合衆国
出願番号 54221703
公報番号 20060264361
公報番号 7666611
出願日 平成15年12月17日(2003.12.17)
公報発行日 平成18年11月23日(2006.11.23)
公報発行日 平成22年2月23日(2010.2.23)
国際出願番号 JP2003016176
国際公開番号 WO2004063224
国際出願日 平成15年12月17日(2003.12.17)
国際公開日 平成16年7月29日(2004.7.29)
優先権データ
  • 特願2003-007657 (2003.1.15) JP
  • 2003WO-JP16176 (2003.12.17) WO
発明の名称 (英語) Lysophosphatidic acid receptor
発明の概要(英語) (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.
特許請求の範囲(英語) [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.
  • 発明者/出願人(英語)
  • SHIMIZU TAKAO
  • ISHII SATOSHI
  • NOGUCHI KYOKO
  • JAPAN SCIENCE AND TECHNOLOGY AGENCY
国際特許分類(IPC)
米国特許分類/主・副
  • 435/7.2
  • 435/4
  • 435/7.1
参考情報 (研究プロジェクト等) CREST Understanding the Brain AREA
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