Novel Method for Quantifying AhR-Ligand Binding Affinities Using Microscale Thermophoresis
The aryl hydrocarbon receptor (AhR) is a highly conserved cellular sensor of a variety of environmental pollutants and dietary-, cell- and microbiota-derived metabolites with important roles in fundamental biological processes. Deregulation of the AhR pathway is implicated in several diseases, inclu...
| Main Authors: | , , , , |
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| Format: | Article |
| Language: | English |
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MDPI AG
2021-02-01
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| Series: | Biosensors |
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| Online Access: | https://www.mdpi.com/2079-6374/11/3/60 |
| _version_ | 1797395412300070912 |
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| author | Anne Stinn Jens Furkert Stefan H. E. Kaufmann Pedro Moura-Alves Michael Kolbe |
| author_facet | Anne Stinn Jens Furkert Stefan H. E. Kaufmann Pedro Moura-Alves Michael Kolbe |
| author_sort | Anne Stinn |
| collection | DOAJ |
| description | The aryl hydrocarbon receptor (AhR) is a highly conserved cellular sensor of a variety of environmental pollutants and dietary-, cell- and microbiota-derived metabolites with important roles in fundamental biological processes. Deregulation of the AhR pathway is implicated in several diseases, including autoimmune diseases and cancer, rendering AhR a promising target for drug development and host-directed therapy. The pharmacological intervention of AhR processes requires detailed information about the ligand binding properties to allow specific targeting of a particular signaling process without affecting the remaining. Here, we present a novel microscale thermophoresis-based approach to monitoring the binding of purified recombinant human AhR to its natural ligands in a cell-free system. This approach facilitates a precise identification and characterization of unknown AhR ligands and represents a screening strategy for the discovery of potential selective AhR modulators. |
| first_indexed | 2024-03-09T00:34:12Z |
| format | Article |
| id | doaj.art-0b37e14ab533421aaaac490023a8cf4e |
| institution | Directory Open Access Journal |
| issn | 2079-6374 |
| language | English |
| last_indexed | 2024-03-09T00:34:12Z |
| publishDate | 2021-02-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Biosensors |
| spelling | doaj.art-0b37e14ab533421aaaac490023a8cf4e2023-12-11T18:16:15ZengMDPI AGBiosensors2079-63742021-02-011136010.3390/bios11030060Novel Method for Quantifying AhR-Ligand Binding Affinities Using Microscale ThermophoresisAnne Stinn0Jens Furkert1Stefan H. E. Kaufmann2Pedro Moura-Alves3Michael Kolbe4Department of Immunology, Max Planck Institute for Infection Biology, Charitéplatz 1, 10117 Berlin, GermanyLeibniz-Institut für Molekulare Pharmakologie (FMP), Robert-Rössle-Strasse 10, 13125 Berlin, GermanyDepartment of Immunology, Max Planck Institute for Infection Biology, Charitéplatz 1, 10117 Berlin, GermanyDepartment of Immunology, Max Planck Institute for Infection Biology, Charitéplatz 1, 10117 Berlin, GermanyDepartment of Structural Infection Biology, Center for Structural Systems Biology (CSSB), Helmholtz-Center for Infection Research (HZI), Notkestrasse 85, 22607 Hamburg, GermanyThe aryl hydrocarbon receptor (AhR) is a highly conserved cellular sensor of a variety of environmental pollutants and dietary-, cell- and microbiota-derived metabolites with important roles in fundamental biological processes. Deregulation of the AhR pathway is implicated in several diseases, including autoimmune diseases and cancer, rendering AhR a promising target for drug development and host-directed therapy. The pharmacological intervention of AhR processes requires detailed information about the ligand binding properties to allow specific targeting of a particular signaling process without affecting the remaining. Here, we present a novel microscale thermophoresis-based approach to monitoring the binding of purified recombinant human AhR to its natural ligands in a cell-free system. This approach facilitates a precise identification and characterization of unknown AhR ligands and represents a screening strategy for the discovery of potential selective AhR modulators.https://www.mdpi.com/2079-6374/11/3/60AhRrecombinant expressionligand bindingMSThigh-throughput screening |
| spellingShingle | Anne Stinn Jens Furkert Stefan H. E. Kaufmann Pedro Moura-Alves Michael Kolbe Novel Method for Quantifying AhR-Ligand Binding Affinities Using Microscale Thermophoresis Biosensors AhR recombinant expression ligand binding MST high-throughput screening |
| title | Novel Method for Quantifying AhR-Ligand Binding Affinities Using Microscale Thermophoresis |
| title_full | Novel Method for Quantifying AhR-Ligand Binding Affinities Using Microscale Thermophoresis |
| title_fullStr | Novel Method for Quantifying AhR-Ligand Binding Affinities Using Microscale Thermophoresis |
| title_full_unstemmed | Novel Method for Quantifying AhR-Ligand Binding Affinities Using Microscale Thermophoresis |
| title_short | Novel Method for Quantifying AhR-Ligand Binding Affinities Using Microscale Thermophoresis |
| title_sort | novel method for quantifying ahr ligand binding affinities using microscale thermophoresis |
| topic | AhR recombinant expression ligand binding MST high-throughput screening |
| url | https://www.mdpi.com/2079-6374/11/3/60 |
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