发明名称 |
METHODS AND COMPOSITIONS FOR IDENTIFYING MODULATORS OF G PROTEIN-COUPLED RECEPTORS |
摘要 |
The subject invention provides methods for making ligand upregulatable G-protein coupled receptors (GPCRs). Ligand upregulatable GPCRs contain a modified TM5-IC3-TM6 segment, which provides for increased levels of the ligand upregulatable GPCR in a host cell in the presence of a ligand as compared to the absence of the ligand. The subject invention also provides assays for screening test compounds for a ligand of a GPCR using a ligand upregulatable GPCR. In these assays, a ligand upregulatable GPCR is contacted with a test compound, and an increase in the detectable amount of the ligand upregulatable GPCR in the host cell indicates that the test compound is a ligand of the GPCR. Said indicated ligands encompass modulators of the GPCR. Said modulators of the GPCR are particularly useful in treating GPCR-related conditions. |
申请公布号 |
WO2004099419(A3) |
申请公布日期 |
2005.01.27 |
申请号 |
WO2004US13543 |
申请日期 |
2004.04.29 |
申请人 |
ARENA PHARMACEUTICALS, INC.;ZENG, FU-YUE;BEHAN, DOMINIC |
发明人 |
ZENG, FU-YUE;BEHAN, DOMINIC |
分类号 |
C07K14/705 |
主分类号 |
C07K14/705 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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