| US 7,611,832 B2 | ||
| Human G protein-coupled receptor and modulators thereof for the treatment of ischemic heart disease and congestive heart failure | ||
| John W. Adams, San Diego, Calif. (US); and Daniel T. Connolly, Solana Beach, Calif. (US) | ||
| Assigned to Arena Pharmaceuticals, Inc., San Diego, Calif. (US) | ||
| Appl. No. 10/523,100 PCT Filed Jul. 25, 2003, PCT No. PCT/US03/23296 § 371(c)(1), (2), (4) Date Jan. 31, 2005, PCT Pub. No. WO2004/013285, PCT Pub. Date Feb. 12, 2004. |
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| Claims priority of provisional application 60/400774, filed on Aug. 01, 2002. | ||
| Prior Publication US 2005/0238579 A1, Oct. 27, 2005 | ||
| Int. Cl. C12Q 1/00 (2006.01); C07K 14/705 (2006.01) | ||
| U.S. Cl. 435—4 [530/350] | 14 Claims |
| 1. A method of identifying a compound as having cardioprotective activity comprising:
(a) contacting a candidate compound with a G protein-coupled receptor (GPCR) comprising an amino acid sequence having at least
95% identity to SEQ ID NO:3, wherein said GPCR is present on a cell or isolated membrane thereof and wherein overexpression
of the GPCR promotes survival of cardiomyocytes;
(b) determining whether said compound stimulates the GPCR;
(c) identifying a compound as having an activity that stimulates said GPCR;
(d) determining whether said compound of step (c) has cardioprotective activity by:
(i) administering said compound of step (c) to a mammal; and
(ii) determining whether said compound of step (c) modulates cardiac function in the mammal; or
(iii) contacting said compound of step (c) with a cardiomyocyte cell in vitro; and
(iv) determining whether said compound modulates survival of said cardiomyocyte cell; and
(e) identifying a compound as having cardioprotective activity.
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