4.4 Article Proceedings Paper

Functions of heteromeric association between adenosine and P2Y receptors

期刊

JOURNAL OF MOLECULAR NEUROSCIENCE
卷 26, 期 2-3, 页码 233-238

出版社

HUMANA PRESS INC
DOI: 10.1385/JMN:26:2-3:233

关键词

GPCR dimer; oligomerization; purinergic; adenosine receptor; P2 receptor; BRET; ATP; inhibitory neurotransmission

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It is now well accepted that G protein-coupled receptors (GPCRs) can be directly associated, as either homo- or hetero-oligomers, to alter their functions. G protein-coupled purinergic receptors, classified as adenosine receptors, and P2Y receptors (ATP receptors) are also found to oligomerize each other to alter their pharmacology. Specifically, adenosine receptor of A(1) subtype (A,R) is able to form a heteromeric complex with P2Y receptor of P2Y(1) type (P2Y(1)R) either in heterologously transfected cells or in rat brain tissues, as demonstrated by coimmunoprecipitation or bioluminescence resonance energy transfer methods in addition to double immunocytochemistry. It is shown that the heteromerization between A,R and P2Y,R generates an adenosine receptor with P2Y-like agonistic pharmacology, i.e., a potent P2Y,R agonist, adenosine 5'-O-(2-thiodiphosphate), binds the A(1)R binding pocket of the A(1)R/P2Y(1)R complex and inhibits adenylyl cyclase activity via G(i/o) protein. This hetero-oligomerization between adenosine receptor and P2Y receptor might be one of the mechanisms for the adenine nucleotide-mediated inhibition of neurotransmitter release. The oligomerization of purinergic receptors is thus considered as an important regulation system in the central nervous system.

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