2. Academic Validation
  3. A G protein-coupled receptor for UDP-glucose

A G protein-coupled receptor for UDP-glucose

  • J Biol Chem. 2000 Apr 14;275(15):10767-71. doi: 10.1074/jbc.275.15.10767.
J K Chambers 1,  L E Macdonald,  H M Sarau,  R S Ames,  K Freeman,  J J Foley,  Y Zhu,  M M McLaughlin,  P Murdock,  L McMillan,  J Trill,  A Swift,  N Aiyar,  P Taylor,  L Vawter,  S Naheed,  P Szekeres,  G Hervieu,  C Scott,  J M Watson,  A J Murphy,  E Duzic,  C Klein,  D J Bergsma,  S Wilson,  G P Livi
Affiliations

Affiliation

  • 1 Department of Vascular Biology, New Frontiers Science Park, SmithKline Beecham Pharmaceuticals, Southern Way, Harlow, Essex CM19 5AW, United Kingdom. Jon_Chambers-1@sbphrd.com
PMID: 10753868 DOI: 10.1074/jbc.275.15.10767
Abstract

Uridine 5'-diphosphoglucose (UDP-glucose) has a well established biochemical role as a glycosyl donor in the enzymatic biosynthesis of Carbohydrates. It is less well known that UDP-glucose may possess pharmacological activity, suggesting that a receptor for this molecule may exist. Here, we show that UDP-glucose, and some closely related molecules, potently activate the orphan G protein-coupled receptor KIAA0001 heterologously expressed in yeast or mammalian cells. Nucleotides known to activate P2Y receptors were inactive, indicating the distinctly novel pharmacology of this receptor. The receptor is expressed in a wide variety of human tissues, including many regions of the brain. These data suggest that some sugar-nucleotides may serve important physiological roles as extracellular signaling molecules in addition to their familiar role in intermediary metabolism.

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