GPCR Omics & Ligand Discovery

  • I. High-throughput identification of functional modulators for GPCR targets.
  • II. Discovery of brain disease-related biomarkers or potential drug targets from the GPCR superfamily.
  • III. Bioinformatics tool development for efficient mining of GPCR omics data.



The superfamily of G-protein-coupled receptors (GPCRs) play essential roles in various pathophysiological conditions and represent a prominent family of therapeutic targets which 30-40% of marketed drugs act on. Innumerable efforts have been made to identify novel ligands that can modulate the activity of specific GPCRs and characterize GPCR-ligand interactions at the molecular level. However, the limitations of most commonly used techniques for GPCR ligand screen and global proteomics highlight the need for more sensitive, selective and robust technologies that can accelerate GPCR drug discovery and functional study.

The central theme of Shui group research is GPCR Omics and Ligand Discovery. Shui group is dedicated to developing versatile mass spectrometry (MS)-based approaches to be integrated with biochemical, structural, pharmacological and computational approaches for GPCR research in three specific directions:

I. GPCR ligand screen and drug discovery. We develop affinity MS techniques for high-throughput GPCR ligand screen, which generates new ligands to serve as chemical tools/probes for elucidating GPCR signaling mechanism or as potential leads for drug development.

II. Functional proteomics targeting GPCR proteins in the brain. Through profiling the transmembrane proteome, especially the GPCR family, in the brain with advanced proteomics technology, we aim to expand the understanding of transmembrane protein organization and dynamics as well as accelerate the discovery of therapeutic targets for neurological disease treatment.

III. Bioinformatics tool development to support GPCR proteomics and ligand screen.


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