Biologically active conformation of [Met5]- and [Leu5]enkephalin on delta opioid receptor

Eur J Pharmacol. 1989 Dec 5;172(6):417-23. doi: 10.1016/0922-4106(89)90024-2.

Abstract

Investigations of the conformation of endogenous enkephalins are generally based on structural comparisons of enkephalins with other opiates and on experimental pharmacological studies. Based on such investigations, we now propose a novel model of the biologically active (receptor-bound) conformation of [Met5]- and [Leu5]enkephalin on the delta opioid receptor. The model helps with the design of new opioid analgesics.

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Enkephalin, Leucine / metabolism
  • Enkephalin, Leucine / pharmacology*
  • Enkephalin, Methionine / metabolism
  • Enkephalin, Methionine / pharmacology*
  • Guinea Pigs
  • Ileum / drug effects
  • In Vitro Techniques
  • Models, Molecular
  • Molecular Sequence Data
  • Muscle, Smooth / drug effects
  • Phenylalanine / metabolism
  • Protein Conformation
  • Receptors, Opioid / metabolism*
  • Receptors, Opioid, delta

Substances

  • Receptors, Opioid
  • Receptors, Opioid, delta
  • Phenylalanine
  • Enkephalin, Methionine
  • Enkephalin, Leucine