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Novel Method for Quantifying AhR-Ligand Binding Affinities Using Microscale Thermophoresis.
Stinn, Anne Furkert, Jens Kaufmann, Stefan H E Moura-Alves, Pedro Kolbe, Michael
Stinn, Anne
Furkert, Jens
Kaufmann, Stefan H E
Moura-Alves, Pedro
Kolbe, Michael
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2021-02-24
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Abstract
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.
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Biosensors (Basel). 2021 Feb 24;11(3):60. doi: 10.3390/bios11030060.
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en
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2079-6374
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Attribution 4.0 International