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 |
US2008009551(A1) |
申请公布日期 |
2008.01.10 |
申请号 |
US20040554521 |
申请日期 |
2004.04.29 |
申请人 |
ARENA PHARMACEUTICALS, INC. |
发明人 |
ZENG FU-YUE;BEHAN DOMINIC |
分类号 |
A61K35/00;A61P43/00;C07H21/00;C07K14/00;C07K14/705;C12Q1/02;C12Q1/68 |
主分类号 |
A61K35/00 |
代理机构 |
|
代理人 |
|
主权项 |
|
地址 |
|