G Protein-Coupled Receptors: Structure, Function, and Ligand Screening

Series:
Methods in Signal Transduction Series
Published:
August 04, 2005 by CRC Press - 336 Pages
Editor(s):
Tatsuya Haga, Gakushuin University, Toyko, Japan; Shigeki Takeda, Gunma University, Japan

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$209.95
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ISBN 9780849327711
Cat# 2771
 

Features

  • Concerns itself with the methods for screening novel ligands for GPCRs, particularly endogenous ligands for orphan GPCRs including odorant receptors
  • Includes a simple ligand screening method using the fusion protein of GPCRs with G protein alpha subunits
  • Presents a method of systematic mutagenesis of muscarinic receptors to reveal the structure–function relationship, as well as a method to generate and analyze knockout mice using muscarinic receptors as a model
  • Discusses desensitization, particularly internalization of muscarinic receptors, valuable to those researching other GPCRs
  • Includes discussion on oligomerization of GPCRs, particularly of purinergic receptors
  • Shares highly useful information on the crystallization of rhodopsin, the only GPCR that has had its atomic structure revealed.
  • Offers a unique approach— the single molecule detection technique — that is applied to cAMP receptors involved in the chemotactic response of Dictyostelium cells
  • Investigates the structure of ligands bound to GPCRs and computer models for the interaction of GPCRs and their ligands

    • Summary

    This book provides a broad base of knowledge of G-protein-coupled receptors. Useful at both the university and industrial levels, this book is of particular interest to those who are developing therapeutic approaches to diseases using drugs that influence receptor activation.

    Table of Contents

    Screening of Ligands for GPCRs


    Screening of Endogenous Ligands for Orphan GPCRs, M. Mori, S. Hinuma, T. Ohtaki, and M. Fujino
    Screening of Ligands for Human GPCRs by the Use of Receptor-Ga ( Fusion Proteins, S. Takeda, H. Suga, and T. Haga
    Screening and Identification of Ghrelin, an Endogenous Ligand for the Growth-Hormone-Secretagogue Receptor, M. Kojima and K. Kangawa
    Ligand Screening of Olfactory Receptors, K. Touhara, S. Katada, T. Nakagawa, and Y. Oka
    Functions and Regulations of GPCRs
    Generation and Phenotypical Analysis of Muscarinic Acetylcholine Receptor Knockout Mice, J. Wess, D. Gautam, S.-J. Han, J. Jeon, C. Li, and C. Deng
    Systematic Mutagenesis of M1 Muscarinic Acetylcholine Receptors, E.C. Hulme
    Analysis of the Regulation of Muscarinic Acetylcholine Receptors, C.J. Van Koppen
    Single-Molecule Analysis of Chemotactic Signaling Mediated by cAMP Receptor on Living Cells, M. Ueda, Y. Miyanaga, and T. Yanagida
    Oligomerization of G Protein-Coupled Purinergic Receptors, H. Nakata, K. Yoshioka, and T. Kamiya

    Tertiary Structure of GPCRs and Their Ligands


    Methods and Results in X-Ray Crystallography of Bovine Rhodopsin, T. Okada, R. Tsujimoto, M. Muraoka, and C. Funamoto
    Determination of Steric Structure of Muscarinic Ligands Bound to Muscarinic Acetylcholine Receptors: Approaches by TRNOE (Transferred Nuclear Overhauser Effect), H. Furukawa, T. Hamada, H. Hirota, M. Ishiguro, and T. Haga
    Modeling of G Protein-Coupled Receptors for Drug Design, M. Ishiguro
    Index

    Editorial Reviews

    “… offers an excellent exhibition of the appropriate methodology to advance in this line of investigation. Experts on this area of work, most of them Japanese scientists, provide the methods and the results obtained on their topic of study. … A book that will be an invaluable resource to scientists dedicated to the cellular signs, as well to the researchers interested in the design of new pharmaceutical drugs.”
    — In the Journal of Physiology and Biochemistry, Vol. 62, No. 1, March 2006

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