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  • Mass spectrometry-based strategies for membrane protein pharmacology. Trends in pharmacological sciences Reiter, A. H., Fehr, A., Florea, R., Floyd, B. M., Schuster, D. 2025

    Abstract

    Membrane proteins are essential for cellular physiology and the target of half of all FDA-approved drugs. However, their hydrophobicity and low abundance make large-scale expression and purification difficult, posing a challenge for drug discovery. Despite these problems, mass spectrometry (MS) has enabled workflows for higher-throughput ligand screening, simplified identification of membrane protein targets and ligandable sites, and direct analysis of drug binding in native environments. In this review, we highlight emerging MS-based strategies, adapted workflows, and novel technological advances in different MS-based fields, including affinity selection, probe-based and probe-free chemoproteomics, and native MS that collectively expand our ability to interrogate membrane proteins for drug discovery, target deconvolution, and mechanistic characterization.

    View details for DOI 10.1016/j.tips.2025.10.012

    View details for PubMedID 41271450