Bioluminescence Resonance Energy Transfer as a Method to Study Protein-Protein Interactions: Application to G Protein Coupled Receptor Biology
The bioluminescence resonance energy transfer (BRET) approach involves resonance energy transfer between a light-emitting enzyme and fluorescent acceptors. The major advantage of this technique over biochemical methods is that protein-protein interactions (PPI) can be monitored without disrupting th...
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| Format: | Article |
| Language: | English |
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MDPI AG
2019-02-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/24/3/537 |
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| author | Chayma El Khamlichi Flora Reverchon-Assadi Nadège Hervouet-Coste Lauren Blot Eric Reiter Séverine Morisset-Lopez |
| author_facet | Chayma El Khamlichi Flora Reverchon-Assadi Nadège Hervouet-Coste Lauren Blot Eric Reiter Séverine Morisset-Lopez |
| author_sort | Chayma El Khamlichi |
| collection | DOAJ |
| description | The bioluminescence resonance energy transfer (BRET) approach involves resonance energy transfer between a light-emitting enzyme and fluorescent acceptors. The major advantage of this technique over biochemical methods is that protein-protein interactions (PPI) can be monitored without disrupting the natural environment, frequently altered by detergents and membrane preparations. Thus, it is considered as one of the most versatile technique for studying molecular interactions in living cells at “physiological„ expression levels. BRET analysis has been applied to study many transmembrane receptor classes including G-protein coupled receptors (GPCR). It is well established that these receptors may function as dimeric/oligomeric forms and interact with multiple effectors to transduce the signal. Therefore, they are considered as attractive targets to identify PPI modulators. In this review, we present an overview of the different BRET systems developed up to now and their relevance to identify inhibitors/modulators of protein⁻protein interaction. Then, we introduce the different classes of agents that have been recently developed to target PPI, and provide some examples illustrating the use of BRET-based assays to identify and characterize innovative PPI modulators in the field of GPCRs biology. Finally, we discuss the main advantages and the limits of BRET approach to characterize PPI modulators. |
| first_indexed | 2024-12-13T02:43:04Z |
| format | Article |
| id | doaj.art-88adc43caa0d441b93e7bfbfa3033e4e |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-12-13T02:43:04Z |
| publishDate | 2019-02-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-88adc43caa0d441b93e7bfbfa3033e4e2022-12-22T00:02:15ZengMDPI AGMolecules1420-30492019-02-0124353710.3390/molecules24030537molecules24030537Bioluminescence Resonance Energy Transfer as a Method to Study Protein-Protein Interactions: Application to G Protein Coupled Receptor BiologyChayma El Khamlichi0Flora Reverchon-Assadi1Nadège Hervouet-Coste2Lauren Blot3Eric Reiter4Séverine Morisset-Lopez5Centre de Biophysique Moléculaire, CNRS, UPR 4301, University of Orléans and INSERM, 45071 Orléans, FranceCentre de Biophysique Moléculaire, CNRS, UPR 4301, University of Orléans and INSERM, 45071 Orléans, FranceCentre de Biophysique Moléculaire, CNRS, UPR 4301, University of Orléans and INSERM, 45071 Orléans, FranceCentre de Biophysique Moléculaire, CNRS, UPR 4301, University of Orléans and INSERM, 45071 Orléans, FrancePRC, INRA, CNRS, Université François Rabelais-Tours, 37380 Nouzilly, FranceCentre de Biophysique Moléculaire, CNRS, UPR 4301, University of Orléans and INSERM, 45071 Orléans, FranceThe bioluminescence resonance energy transfer (BRET) approach involves resonance energy transfer between a light-emitting enzyme and fluorescent acceptors. The major advantage of this technique over biochemical methods is that protein-protein interactions (PPI) can be monitored without disrupting the natural environment, frequently altered by detergents and membrane preparations. Thus, it is considered as one of the most versatile technique for studying molecular interactions in living cells at “physiological„ expression levels. BRET analysis has been applied to study many transmembrane receptor classes including G-protein coupled receptors (GPCR). It is well established that these receptors may function as dimeric/oligomeric forms and interact with multiple effectors to transduce the signal. Therefore, they are considered as attractive targets to identify PPI modulators. In this review, we present an overview of the different BRET systems developed up to now and their relevance to identify inhibitors/modulators of protein⁻protein interaction. Then, we introduce the different classes of agents that have been recently developed to target PPI, and provide some examples illustrating the use of BRET-based assays to identify and characterize innovative PPI modulators in the field of GPCRs biology. Finally, we discuss the main advantages and the limits of BRET approach to characterize PPI modulators.https://www.mdpi.com/1420-3049/24/3/537BRETreceptor-protein interactionsG protein-coupled receptorsGPCR signalingGPCR-interacting proteinsdrug discoveryscreening |
| spellingShingle | Chayma El Khamlichi Flora Reverchon-Assadi Nadège Hervouet-Coste Lauren Blot Eric Reiter Séverine Morisset-Lopez Bioluminescence Resonance Energy Transfer as a Method to Study Protein-Protein Interactions: Application to G Protein Coupled Receptor Biology Molecules BRET receptor-protein interactions G protein-coupled receptors GPCR signaling GPCR-interacting proteins drug discovery screening |
| title | Bioluminescence Resonance Energy Transfer as a Method to Study Protein-Protein Interactions: Application to G Protein Coupled Receptor Biology |
| title_full | Bioluminescence Resonance Energy Transfer as a Method to Study Protein-Protein Interactions: Application to G Protein Coupled Receptor Biology |
| title_fullStr | Bioluminescence Resonance Energy Transfer as a Method to Study Protein-Protein Interactions: Application to G Protein Coupled Receptor Biology |
| title_full_unstemmed | Bioluminescence Resonance Energy Transfer as a Method to Study Protein-Protein Interactions: Application to G Protein Coupled Receptor Biology |
| title_short | Bioluminescence Resonance Energy Transfer as a Method to Study Protein-Protein Interactions: Application to G Protein Coupled Receptor Biology |
| title_sort | bioluminescence resonance energy transfer as a method to study protein protein interactions application to g protein coupled receptor biology |
| topic | BRET receptor-protein interactions G protein-coupled receptors GPCR signaling GPCR-interacting proteins drug discovery screening |
| url | https://www.mdpi.com/1420-3049/24/3/537 |
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