Functional expression of single-chain heterodimeric G-protein-coupled receptors for adenosine and dopamine

被引：5

作者：

Kamiya, T

Saitoh, O

Nakata, H

机构：

[1] Tokyo Metropolitan Inst Neurosci, Dept Mol Cell Signaling, Tokyo 1838526, Japan

[2] Kinki Univ, Sch Pharmaceut Sci, Cell Biol Lab, Higashiosaka, Osaka 5778502, Japan

[3] Nagahama Inst Biosci & Technol, Mol Biol Lab, Shiga 5260829, Japan

来源：

CELL STRUCTURE AND FUNCTION | 2005年 / 29卷 / 5-6期

关键词：

adenosine A(2A) receptor; dopamine D-2 receptor; G-protein-coupled receptor; heteromerization; single-chain;

D O I：

10.1247/csf.29.139

中图分类号：

Q2 [细胞生物学];

学科分类号：

071009 ; 090102 ;

摘要：

The direct homo- and heteromeric association between G-protein-coupled receptors (GPCRs), adenosine A(2A) receptor (A(2A)R) and dopamine D-2 receptor (D2R), occurs although little is known about the selectivity of their formation (A(2A)R/A(2A)R vs. A(2A)R/D2R). In order to stimulate the heteromerization of A(2A)R and D2R, we have designed a single-polypeptide-chain heterodimeric A(2A)R/D2R complex by fusing the C-terminus of the A(2A)R via transmembrane (TM) of a type II TM protein with the N-terminus of D2R in tandem. This was successfully expressed on the cell surface as a full-length protein with specific binding to the respective ligands and functional coupling to G-proteins comparable to wild-type receptors, suggesting the possible creation of physiologically relevant heteromeric A(2A)R/D2R. This expression system would be useful to exclusively clarify the properties of heteromeric GPCRs irrespective of homomeric receptors.

引用

页码：139 / 145

页数：7

共 23 条

[1] A fusion protein of the human P2Y1 receptor and NTPDase1 exhibits functional activities of the native receptor and ectoenzyme and reduced signaling [J].