US 7,524,638 B1
Methods for identification of modulators of OSGPR114 or OSGPR78 activity, and their use in the treatment of disease
Graeme Griffin, Centereach, N.Y. (US); and Lambertus J. Oehlen, Old Bethpage, N.Y. (US)
Assigned to OSI Pharmaceuticals, Inc., Melville, N.Y. (US)
Filed on Jun. 25, 2004, as Appl. No. 10/877,850.
Claims priority of provisional application 60/482964, filed on Jun. 27, 2003.
Int. Cl. G01N 33/567 (2006.01); C07K 14/705 (2006.01)
U.S. Cl. 435—7.21  [436/501] 36 Claims
 
1. An assay process for identifying a compound that specifically binds to an OSGPR114 receptor, wherein said OSGPR114 receptor comprises an amino acid sequence having at least 95% identity to SEQ ID NO:3, that can induce oleoyl lysophosphatidic acid stimulation of G-protein activity in cells, said process comprising:
providing either
(a) two samples of cells expressing on their cell surface the OSGPR114 receptor, or
(b) two samples of a membrane preparation from said cells;
contacting one sample with a lysophosphatidic acid ligand known to bind to the receptor, under conditions suitable for binding of said ligand to the receptor, in the presence of a test compound;
contacting the second sample with said ligand, under conditions suitable for binding of said ligand to the receptor, in the absence of the test compound;
measuring the specific binding of the ligand to the receptor in the presence of the compound;
measuring the specific binding of the ligand to the receptor in the absence of the compound; and
comparing the binding in the presence and in the absence of the compound being tested, wherein a difference in comparison indicates that the compound binds to the OSGPR114 receptor.