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TheScientificWorldJOURNAL (ISSN 1537-744X) |
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Title: |
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Detection of Heteromers Formed by Cannabinoid CB1, Dopamine D2, and Adenosine A2A G-Protein-Coupled Receptors by Combining Bimolecular Fluorescence Complementation and Bioluminescence Energy Transfer |
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Authors: |
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Navarro, Gemma ; Carriba, Paulina ; Gandía, Jorge ; Ciruela, Francisco ; Casadó, Vicent ; Cortés, Antoni ; Mallol, Josefa ; Canela, Enric I.; Lluis, Carmen ; Franco, Rafael |
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Journal: |
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TheScientificWorldJOURNAL |
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Year: |
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2008 |
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Volume: |
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8 |
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Page Range: |
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1088-1097 |
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Article Type: |
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Research Article |
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Handling Editor: |
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Sergi Ferre |
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Domains: |
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Neuroscience
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Endocrinology
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Drug Dependence
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Methods & Protocols
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Cell Signaling
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Proteins & Proteomics
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Intercellular Communication
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Biochemistry & Molecular Biology
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DOI: |
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10.1100/tsw.2008.136 |
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Synopsis: |
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There are a number of techniques to detect G-protein-coupled receptor (GPCR) dimers. However, it is suspected that GPCRs may form oligomers. This paper reports a technique to detect trimers of GPCRs. Hetero-oligomers of cannabinoid CB1, dopamine D2, and adenosine A2A receptors, which are crucial in order to understand striatal neurotransmission, are detected. The technique is, therefore, instrumental in order to detect the topology of GPCR molecular interactions, which is fundamental to the understanding of neurotransmission and endocrine regulation. |
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Keywords: |
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G-protein-coupled receptors, adenosine A2A receptor, cannabinoid CB1 receptor, dopamine D2 receptor, heterotrimers, oligomers of three different protomers, bimolecular fluorescence complementation, bioluminescence energy transfer, BRET |
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Abstract |
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Functional interactions in signaling occur between dopamine D2 (D2R) and cannabinoid CB1 (CB1R) receptors, between CB1R and adenosine A2A (A2AR) receptors, and between D2R and A2AR. Furthermore, direct molecular interactions have been reported for the pairs CB1R-D2R, A2AR-D2R, and CB1R-A2AR. Here a combination of bimolecular fluorescence complementation and bioluminescence energy transfer techniques was used to identify the occurrence of D2R-CB1R-A2AR hetero-oligomers in living cells. |
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