• Novel Method for Quantifying AhR-Ligand Binding Affinities Using Microscale Thermophoresis.

      Stinn, Anne; Furkert, Jens; Kaufmann, Stefan H E; Moura-Alves, Pedro; Kolbe, Michael; CSSB, Centre for Structural Systembiologie, Notkestr.85, 22607 Hamburg. Germany. (MDPI, 2021-02-24)
      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.