发明名称 |
Non-endogenous, constitutively activated human G protein-coupled receptors |
摘要 |
Disclosed 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) P1 AA15 X and/or (b) Pcodon (AA-codon)15 Xcodon, respectively. In a most preferred embodiment, P1 and Pcodon 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. As it is most preferred that the non-endogenous human GPCRs which incorporate these mutations are incorporated into mammalian cells and utilised 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. |
申请公布号 |
NZ510331(A) |
申请公布日期 |
2004.07.30 |
申请号 |
NZ19990510331 |
申请日期 |
1999.10.12 |
申请人 |
ARENA PHARMACEUTICALS, INC |
发明人 |
BEHAN, DOMINIC P;CHALMERS, DEREK T;LIAW, CHEN W |
分类号 |
G01N33/50;A61K38/00;A61K45/00;A61P43/00;C07D231/12;C07D231/16;C07D409/12;C07K5/08;C07K7/06;C07K14/705;C07K14/72;C12N1/15;C12N1/19;C12N1/21;C12N5/10;C12N15/09;C12N15/12;C12N15/16;C12Q1/02;G01N33/15;G01N33/566 |
主分类号 |
G01N33/50 |
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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