Integrated Approaches for Genome-wide Interrogation of the Druggable Non-olfactory G Protein-coupled Receptor Superfamily

J Biol Chem. 2015 Aug 7;290(32):19471-7. doi: 10.1074/jbc.R115.654764. Epub 2015 Jun 22.

Abstract

G-protein-coupled receptors (GPCRs) are frequent and fruitful targets for drug discovery and development, as well as being off-targets for the side effects of a variety of medications. Much of the druggable non-olfactory human GPCR-ome remains under-interrogated, and we present here various approaches that we and others have used to shine light into these previously dark corners of the human genome.

Keywords: G-protein-coupled receptor (GPCR); chemical biology; cheminformatics; disease; druggable genome; functional genomics; molecular pharmacology; neurological disease.

Publication types

  • Research Support, N.I.H., Extramural
  • Review

MeSH terms

  • Binding Sites
  • Databases, Bibliographic
  • Databases, Chemical
  • Databases, Pharmaceutical
  • Drugs, Investigational / chemical synthesis
  • Drugs, Investigational / pharmacology*
  • Genome, Human*
  • Humans
  • Ligands
  • Protein Binding
  • Proteome / chemistry*
  • Proteome / metabolism
  • Receptors, G-Protein-Coupled / agonists
  • Receptors, G-Protein-Coupled / antagonists & inhibitors
  • Receptors, G-Protein-Coupled / genetics
  • Receptors, G-Protein-Coupled / metabolism*
  • Small Molecule Libraries / chemical synthesis
  • Small Molecule Libraries / pharmacology*

Substances

  • Drugs, Investigational
  • Ligands
  • Proteome
  • Receptors, G-Protein-Coupled
  • Small Molecule Libraries