Bingjie Zhang; Wenqing Shui
Chin. J. Nat., 2021, 43(1), 32-38
https://doi.org/10.3969/j.issn.0253-9608.2021.01.005

Abstract

Affinity mass spectrometry (affinity MS) based on the detection of protein target-ligand interaction is a powerful technology complementary to conventional high-throughput screening (HTS) assays and has been successfully incorporated into the early-phase lead discovery pipeline. Owing to the special biochemical properties of G protein-coupled receptors (GPCRs), tremendous technical challenges are posed to affinity MS-based ligand screening for GPCR targets. Here we briefly summarize the principle and features of the affinity MS technique adapted to GPCR ligand screening, and review the recent progress in screening both large-scale compound libraries and natural herb extracts with affinity MS for discovery of unreported GPCR ligands and modulators.