Work

Comparative Evaluation and Profiling of Chemical Tools for the Nuclear Hormone Receptor Family 2

Year: 2025

Type: article

Abstract: Nuclear receptors regulate transcription in response to ligand signals and enable the pharmacological control of gene expression. However, many nuclear receptors are still poorly explored and are not accessible to ligand-based target identification studies. In particular, most members of the NR2 family are among the least studied proteins of the class, and apart from the retinoid X receptors (RXR), validated NR2 ligands are very rare. Here, we gathered the NR2 modulators reported in the literature for comparative profiling in uniform test systems. Most candidate compounds displayed insufficient on-target activity or selectivity to be used as chemical tools for NR2 receptors, underscoring the urgent need for further NR2 ligand development. Nevertheless, a small NR2 modulator set could be assembled for application in a chemogenomic fashion.

Source: ACS Pharmacology & Translational Science

DOI: 10.1021/acsptsci.4c00719

Authors: Max Lewandowski, Romy Busch, Julian A. Marschner, Daniel Merk

Institution: Ludwig-Maximilians-Universität München

Language: English

Topic: Nuclear Receptors and Signaling

Subfield: Cellular and Molecular Neuroscience

Field: Neuroscience

Domain: Life Sciences

SDG: Good health and well-being

Open Access status: green

Funders: Innovative Medicines Initiative, European Research Council