Journal Article

PUBDB-2024-00588

http://join2-wiki.gsi.de/foswiki/pub/Main/Artwork/join2_logo100x88.png Novel Method for Quantifying AhR-Ligand Binding Affinities Using Microscale Thermophoresis

Stinn, A. ; Furkert, J. ; Kaufmann, S. H. E. ; Moura-Alves, P. (Corresponding author) ; Kolbe, M. (Corresponding author)CSSB*EMBL*

2021
MDPI Basel

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Please use a persistent id in citations: doi:10.3390/bios11030060  doi:10.3204/PUBDB-2024-00588

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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Contributing Institute(s):

1. CSSB-HZI-MK (CSSB-HZI-MK)

Research Program(s):

1. 899 - ohne Topic (POF4-899) (POF4-899)
2. iNEXT - Infrastructure for NMR, EM and X-rays for translational research (653706) (653706)

Experiment(s):

1. No specific instrument

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