Digging deep--structure-function relationships in the melatonin receptor family

J Pineal Res. 2003 Nov;35(4):221-30. doi: 10.1034/j.1600-079x.2003.00090.x.


The melatonin receptor family is a small group of receptors within the G protein-coupled receptor (GPCR) superfamily. The group comprises of three subtypes which bind melatonin and one member, the melatonin related receptor (MRR), that shares >40% sequence identity with the other melatonin receptors but does not bind melatonin. Identification of two subtypes expressed in the mouse suprachiasmatic nucleus, one of which (MT1) inhibits neuronal firing and the other (MT2) mediating the phase advancing properties of melatonin has given renewed interest to the development of subtype specific compounds for each of the mammalian melatonin receptors. Towards this goal site-directed and chimaeric receptor mutagenesis studies have been performed which have provided some insight into the structure-function relationships of the melatonin receptors. Furthermore, these studies may lead to the identification of the ligand for the orphan MRR.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Humans
  • Mice
  • Molecular Sequence Data
  • Protein Structure, Secondary
  • Receptors, Melatonin / chemistry*
  • Receptors, Melatonin / physiology*
  • Sequence Alignment
  • Signal Transduction / physiology
  • Structure-Activity Relationship


  • Receptors, Melatonin