Evolving pharmacology of orphan GPCRs: IUPHAR Commentary

Br J Pharmacol. 2013 Oct;170(4):693-5. doi: 10.1111/bph.12339.


The award of the 2012 Nobel Prize in Chemistry to Robert Lefkowitz and Brian Kobilka for their work on the structure and function of GPCRs, spanning a period of more than 20 years from the cloning of the human β2 -adrenoceptor to determining the crystal structure of the same protein, has earned both researchers a much deserved place in the pantheon of major scientific discoveries. GPCRs comprise one of the largest families of proteins, controlling many major physiological processes and have been a major focus of the International Union of Basic and Clinical Pharmacology Committee on Receptor Nomenclature and Drug Classification (NC-IUPHAR) since its inception in 1987. We report here recent efforts by the British Pharmacological Society and NC-IUPHAR to define the endogenous ligands of 'orphan' GPCRs and to place authoritative and accessible information about these crucial therapeutic targets online.

Keywords: chemerin receptor; chemokine receptors; free fatty acid receptors; hydroxycarboxylic acid receptors; lysophosphatidic acid receptors; oxoglutarate receptor; succinate receptor.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Access to Information
  • Animals
  • Cooperative Behavior
  • High-Throughput Screening Assays
  • Humans
  • International Cooperation
  • Ligands
  • Orphan Nuclear Receptors / classification
  • Orphan Nuclear Receptors / drug effects*
  • Orphan Nuclear Receptors / metabolism
  • Pharmacology* / methods
  • Signal Transduction / drug effects*
  • Societies, Scientific
  • Terminology as Topic


  • Ligands
  • Orphan Nuclear Receptors