𝔖 Bobbio Scriptorium
✦   LIBER   ✦

Photoaffinity scanning in the mapping of the peptide receptor interface of class II G protein—coupled receptors

✍ Scribed by Vi Pham; Patrick M. Sexton

Publisher
John Wiley and Sons
Year
2004
Tongue
English
Weight
298 KB
Volume
10
Category
Article
ISSN
1075-2617

No coin nor oath required. For personal study only.

✦ Synopsis

Abstract

The family of G protein‐coupled receptors constitutes about 50% of the therapeutic drug targets used in clinical medicine today, although the mechanisms of ligand binding, activation and signal transduction for G protein‐coupled receptors are not yet well defined. This review discusses ongoing research using the photoaffinity scanning method to map the bimolecular interface between class II G protein‐coupled receptors and their ligands. Furthermore the available computer model of class II peptide ligand docking into the receptor, based on the positional constraints imposed by the photoaffinity scanning analyses, will be discussed briefly. The ultimate goal of these efforts is to understand the molecular basis of receptor binding and therefore to generate a template for rational drug design. Copyright © 2003 European Peptide Society and John Wiley & Sons, Ltd.

📜 SIMILAR VOLUMES

Functional interaction of G protein-coup
Functional interaction of G protein-coupled receptors of the adrenomedullin peptide family with accessory receptor-activity-modifying proteins (RAMP)
✍ Walter Born; Roman Muff; Jan A. Fischer 📂 Article 📅 2002 🏛 John Wiley and Sons 🌐 English ⚖ 165 KB

## Abstract Adrenomedullin (AM), α‐ and β‐calcitonin gene‐related peptide (CGRP), calcitonin (CT), and amylin are homologous polypeptides with overlapping biological actions such as vasodilatation and inhibition of bone resorption. They are brought about through receptors that include the CT recept

The NMR-derived conformation of neuropep
The NMR-derived conformation of neuropeptide AF, an orphan G-protein coupled receptor peptide
✍ Mark Miskolzie; George Kotovych 📂 Article 📅 2003 🏛 Wiley (John Wiley & Sons) 🌐 English ⚖ 252 KB

## Abstract The tertiary structure of the pain modulating and anti‐opiate neuropeptide, human neuropeptide AF (NPAF) (the sequence is AGEGLNSQFWSLAAPQRF–NH~2~), was determined by ^1^H‐NMR. The structure of NPAF was determined in two solvent systems, namely 50%/50% trifluoroethanol‐__d__~__3__~/H~2~

Exploratory synthesis of peptide–α-thioe
Exploratory synthesis of peptide–α-thioester segments spanning the polypeptide sequence of the δ-opioid receptor, a G protein-coupled receptor
✍ Erik C. B. Johnson; Stephen B. H. Kent 📂 Article 📅 2007 🏛 Wiley (John Wiley & Sons) 🌐 English ⚖ 350 KB 👁 1 views

## Abstract We have decided to use the δ‐opioid receptor (372 residues) as a model system to develop methods for the total chemical synthesis of G protein‐coupled receptors. The most important feature of this receptor from a chemical synthesis perspective is the wealth of cysteines spread throughou