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bioRxiv · 10.1101/2021.01.26.428246

Novel method for quantifying AhR-ligand binding affinities using Microscale Thermophoresis

Moura Alves, P.·Kaufmann, S. H. E.·Stinn, A.·Kolbe, M.·Furkert, J.
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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 signalling 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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Moura Alves, P., Kaufmann, S. H. E., Stinn, A., Kolbe, M., Furkert, J.. 2021-01-27. Novel method for quantifying AhR-ligand binding affinities using Microscale Thermophoresis. https://doi.org/10.1101/2021.01.26.428246

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