First Fatty Acylated Dipeptides to Affect Muscarinic Receptor Ligand Binding

Bioorg Med Chem Lett. 1999 Dec 6;9(23):3363-8. doi: 10.1016/s0960-894x(99)00604-6.

Abstract

Fatty acylated dipeptides homologous to Gi alpha N-termini affect ligand binding to muscarinic acetylcholine receptors. Myristylglycine-serine containing dipeptides decrease antagonist binding at both M1 and M2 muscarinic receptors. Palmitate on the serine analogous to native palmitoylated cysteine affords dipeptide which selectively decreases the number of high affinity agonist binding sites at M2 but not M1 receptor.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acylation
  • Animals
  • Binding Sites
  • CHO Cells
  • Cricetinae
  • Dipeptides / chemistry
  • Dipeptides / pharmacology*
  • Fatty Acids / chemistry*
  • Ligands
  • Muscarinic Antagonists / chemistry
  • Muscarinic Antagonists / pharmacology*
  • Receptors, Muscarinic / metabolism*

Substances

  • Dipeptides
  • Fatty Acids
  • Ligands
  • Muscarinic Antagonists
  • Receptors, Muscarinic