First fatty acylated dipeptides to affect muscarinic receptor ligand binding

Authors
Krishnan, V Pham, WN Messer, WS Peseckis, SM
Citation
V. Krishnan et al., First fatty acylated dipeptides to affect muscarinic receptor ligand binding, BIOORG MED, 9(23), 1999, pp. 3363-3368
Citations number
6
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
23
Year of publication
1999
Pages
3363 - 3368
Database
ISI
SICI code
0960-894X(199912)9:23<3363:FFADTA>2.0.ZU;2-X
Abstract
Fatty acylated dipeptides homologous to G(i)alpha N-termini affect ligand b inding to muscarinic acetylcholine receptors. Myristylglycine-serine contai ning dipeptides decrease antagonist binding at both M-i, and M-2, muscarini c receptors. Palmitate on the serine analogous to native palmitoylated cyst eine affords dipeptide which selectively decreases the number of high affin ity agonist binding sites at M-2, but not M-1 receptor. (C) 1999 Elsevier S cience Ltd. All rights reserved.