| Original document(312 pages) Authorized document(307 pages) 中文版 |
Disclosed herein are constitutively activated, non-endogenous versions of endogenous human G protein-coupled receptors comprising (a) the following amino acid sequence region (C-terminus to N-terminus orientation) and/or (b) the following nucleic acid sequence region (3' to 5' orientation) transversing the transmembrane-6 (TM6) and intracellular loop-3 (IC3) regions of the GPCR: (a) P<1> AA15 X and/or (b) P<codon> (AA-codon)15 Xcodon, respectively. In a most preferred embodiment, P<1> and P<codon> are endogenous proline and an endogenous nucleic acid encoding region encoding proline, respectively, located within TM6 of the non-endogenous GPCR; AA15 and (AA-codon)15 are 15 endogenous amino acid residues and 15 codons encoding endogenous amino acid residues, respectively; and X and Xcodon are non-endogenous lysine and a non-endogenous nucleic acid encoding region encoding lysine, respectively, located within IC3 of the non-endogenous GPCR. Because it is most preferred that the non-endogenous human GPCRs which incorporate these mutations are incorporated into mammalian cells and utilized for the screening of the candidate compounds, the non-endogenous human GPCR incorporating the mutation need not be purified and isolated per se (i.e., these are incorporated within the cellular membrane of a mammalian cell), although such purified and isolated non-endogenous human GPCRs are well within the purview of this disclosure. |
Application Number
申请号 |
99812091 |
Application Date
申请日 |
1999.10.12 |
| Title 名称 |
Non-endogenous, constitutively activated human G protein-coupled receptors |
Publication Number
公开号 |
1398298 |
Publication Date
公开日 |
2003.02.19 |
| Approval Pub. Date |
2007.08.01 |
Granted Pub. Date |
2007.08.01 |
| International Classification 分类号 |
C12N15/12;C07K14/72;G01N33/50;G01N33/566 |
Applicant(s) Name
申请人 |
Arena Pharmaceuticals, Inc |
| Address 地址 |
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| Inventor(s) Name 发明人 |
Dominic P. Behan;Derek T. Chalmers;Liaw W. Chen |
| Attorney & Agent 代理人 |
ding yebeng wang weiyu |
| More information 更 多 信 息 |
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