文章基本信息

标题：Novel Method for Quantifying AhR-Ligand Binding Affinities Using Microscale Thermophoresis
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作者：Anne Stinn ; Jens Furkert , Stefan H.E. Kaufmann ; Pedro Moura-Alves 等
期刊名称：Biosensors
电子版ISSN：2079-6374
出版年度：2021
卷号：11
期号：3
页码：60
DOI：10.3390/bios11030060
出版社：MDPI Publishing
摘要：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.
关键词：AhR; recombinant expression; ligand binding; MST; high-throughput screening AhR ; recombinant expression ; ligand binding ; MST ; high-throughput screening