BiasDB

A manually curated database of biased GPCR ligands

BiasDB[1] is a manually curated database containing all published biased GPCR ligands. BiasDB currently contains 617 bias cases of signaling bias representing 481 individual ligands for 61 receptors. We provide information about the chemical structure, target receptor, type of bias, assay categories used for bias determination, reference ligand and literature source. BiasDB is a resource for medicinal chemists, pharmacologists and researchers interested in biased GPCR signaling.


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What is biased GPCR signaling?

G protein-coupled receptors (GPCRs) represent important drug targets with complex pharmacological characteristics. Biased signaling represents one important dimension of this complexity describing ligand-dependent shifts of naturally imprinted signaling profiles. Since biased GPCR modulators provide potential therapeutic benefits including higher efficiencies and reduced adverse effects, the identification of such ligands as drug candidates is highly desirable [2,3].

References:

  1. C. Omieczynski, T. N. Nguyen, D. Sribar, L. Deng, D. Stepanov, D. Schaller, G. Wolber, M. Bermudez. BiasDB: A Comprehensive Database for Biased GPCR Ligands, BioRxiv, first published August 24, 2019.
  2. Bermudez, M., Nguyen, T.N., Omieczynski,C., Wolber, G., Strategies for the discovery of biased GPCR ligands. Drug Discov Today, 24(4): 1031-1037, 2019
  3. Tan, L., Yan, W., McCorvy, J.D., Cheng, J., Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential. J Med Chem, 61(22): 9841-9878, 2018