GPCRTargets

GPCRTargets is a catalog of G protein-coupled receptor targets used in pharmacology and drug discovery. It aggregates receptor identities, ligands, signaling pathways, and disease associations, enabling researchers to compare receptor families and prioritize targets for modulation.

G protein-coupled receptors constitute the largest family of cell surface receptors, characterized by seven transmembrane helices. They transduce signals through G proteins and arrestins, regulating cAMP, calcium, and other pathways. GPCRs mediate senses, neurotransmission, immunity, and hormonal signaling; they account for a substantial share of approved drugs.

A typical GPCRTargets entry includes receptor name and gene symbol, pharmacological class (e.g., class A, B, C), endogenous or synthetic ligands, agonist/antagonist profiles, signaling bias, tissue distribution, and disease associations. Structural data, such as available crystal or cryo-EM structures, may be included.

Data sources for GPCRTargets commonly include public resources like IUPHAR/BPS Guide to Pharmacology, GPCRdb, ChEMBL, and PubChem. Cross-referencing across species and isoforms helps translational research and target validation.

Applications include prioritizing targets for lead discovery, guiding selectivity and bias screening, deorphanization efforts for orphan receptors, and supporting pharmacovigilance by capturing adverse signaling profiles.

Limitations include incomplete ligand data, evolving receptor taxonomy, challenges of biased signaling and allosteric modulation, and variability in tissue expression data. Ongoing curation integrates new structural insights and functional studies.