Functional Expression of Single-Chain Heterodimeric G-Protein-Coupled Receptors for Adenosine and Dopamine

Cell Structure and Function

Hiroyasu Nakata¹  Toshio Kamiya¹  Osamu Saitoh¹ 

[1] Department of Molecular Cell Signaling, Tokyo Metropolitan Institute for Neuroscience

关键词: Adenosine A2A receptor;    dopamine D2 receptor;    G-protein-coupled receptor;    heteromerization;    single-chain;   

DOI  :  10.1247/csf.29.139

学科分类：分子生物学，细胞生物学和基因

来源: Japan Society for Cell Biology

【 摘 要 】

References(23)Cited-By(4)The direct homo- and heteromeric association between G-protein-coupled receptors (GPCRs), adenosine A2A receptor (A2AR) and dopamine D2 receptor (D2R), occurs although little is known about the selectivity of their formation (A2AR/A2AR vs. A2AR/D2R). In order to stimulate the heteromerization of A2AR and D2R, we have designed a single-polypeptide-chain heterodimeric A2AR/D2R complex by fusing the C-terminus of the A2AR 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 A2AR/D2R. This expression system would be useful to exclusively clarify the properties of heteromeric GPCRs irrespective of homomeric receptors.

【 授权许可】

Unknown