A Robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands Discovery
The identification of new modulators for Cannabinoid Receptors (CBRs) has garnered significant attention in drug discovery over recent years, owing to their manifold pathophysiological implications. In the context of hit identification, the availability of robust and sensitive high-throughput screen...
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| Format: | Article |
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MDPI AG
2023-12-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/28/24/8107 |
| _version_ | 1797379936917389312 |
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| author | Gemma Navarro Eddy Sotelo Iu Raïch María Isabel Loza Jose Brea Maria Majellaro |
| author_facet | Gemma Navarro Eddy Sotelo Iu Raïch María Isabel Loza Jose Brea Maria Majellaro |
| author_sort | Gemma Navarro |
| collection | DOAJ |
| description | The identification of new modulators for Cannabinoid Receptors (CBRs) has garnered significant attention in drug discovery over recent years, owing to their manifold pathophysiological implications. In the context of hit identification, the availability of robust and sensitive high-throughput screening assays is essential to enhance the likelihood of success. In this study, we present the development and validation of a Tag-lite<sup>®</sup> binding assay designed for screening hCB<sub>1</sub>/hCB<sub>2</sub> binding, employing a dual fluorescent ligand, CELT-335. Representative ligands for CBRs, exhibiting diverse affinity and functional profiles, were utilized as reference compounds to validate the robustness and efficiency of the newly developed Tag-lite<sup>®</sup> binding assay protocol. The homogeneous format, coupled with the sensitivity and optimal performance of the fluorescent ligand CELT-335, establishes this assay as a viable and reliable method for screening in hit and lead identification campaigns. |
| first_indexed | 2024-03-08T20:30:15Z |
| format | Article |
| id | doaj.art-b984db540fcc45b38c1ff849fd3cbb3b |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-08T20:30:15Z |
| publishDate | 2023-12-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-b984db540fcc45b38c1ff849fd3cbb3b2023-12-22T14:27:50ZengMDPI AGMolecules1420-30492023-12-012824810710.3390/molecules28248107A Robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands DiscoveryGemma Navarro0Eddy Sotelo1Iu Raïch2María Isabel Loza3Jose Brea4Maria Majellaro5Department of Biochemistry and Physiology, Faculty of Pharmacy and Food Science, University of Barcelona, 08028 Barcelona, SpainDepartment of Organic Chemistry, Center for Research in Biological Chemistry and Molecular Materials (CiQUS), University of Santiago de Compostela, 15782 Santiago de Compostela, SpainDepartment of Biochemistry and Physiology, Faculty of Pharmacy and Food Science, University of Barcelona, 08028 Barcelona, SpainResearch Center in Molecular Medicine and Chronic Diseases (CIMUS), University of Santiago de Compostela, 15782 Santiago de Compostela, SpainResearch Center in Molecular Medicine and Chronic Diseases (CIMUS), University of Santiago de Compostela, 15782 Santiago de Compostela, SpainCeltarys Research SL, Avda. Mestre Mateo, 2, 15706 Santiago de Compostela, SpainThe identification of new modulators for Cannabinoid Receptors (CBRs) has garnered significant attention in drug discovery over recent years, owing to their manifold pathophysiological implications. In the context of hit identification, the availability of robust and sensitive high-throughput screening assays is essential to enhance the likelihood of success. In this study, we present the development and validation of a Tag-lite<sup>®</sup> binding assay designed for screening hCB<sub>1</sub>/hCB<sub>2</sub> binding, employing a dual fluorescent ligand, CELT-335. Representative ligands for CBRs, exhibiting diverse affinity and functional profiles, were utilized as reference compounds to validate the robustness and efficiency of the newly developed Tag-lite<sup>®</sup> binding assay protocol. The homogeneous format, coupled with the sensitivity and optimal performance of the fluorescent ligand CELT-335, establishes this assay as a viable and reliable method for screening in hit and lead identification campaigns.https://www.mdpi.com/1420-3049/28/24/8107CB<sub>1</sub>RCB<sub>2</sub>RHTRFbindingHTS |
| spellingShingle | Gemma Navarro Eddy Sotelo Iu Raïch María Isabel Loza Jose Brea Maria Majellaro A Robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands Discovery Molecules CB<sub>1</sub>R CB<sub>2</sub>R HTRF binding HTS |
| title | A Robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands Discovery |
| title_full | A Robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands Discovery |
| title_fullStr | A Robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands Discovery |
| title_full_unstemmed | A Robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands Discovery |
| title_short | A Robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands Discovery |
| title_sort | robust and efficient fret based assay for cannabinoid receptor ligands discovery |
| topic | CB<sub>1</sub>R CB<sub>2</sub>R HTRF binding HTS |
| url | https://www.mdpi.com/1420-3049/28/24/8107 |
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