G Protein Coupled Receptors, Volume 520

1st Edition


Serial Volume Editors: P. Michael Conn
Hardcover ISBN: 9780123918611
eBook ISBN: 9780123918727
Imprint: Academic Press
Published Date: 8th February 2013
Page Count: 440
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Table of Contents

Series Page



Methods in Enzymology

Chapter One. Expression of GPCRs in Pichia pastoris for Structural Studies

1 Introduction

2 Generation of Expression Clones

3 Screening Transformants

4 Characterization and Optimization of Initial Target Receptor Production

5 Large-Scale Production

6 Prospects for Large-Scale GPCR Production in P. pastoris


Chapter Two. Conformational Ensemble View of G Protein-Coupled Receptors and the Effect of Mutations and Ligand Binding

1 Introduction

2 Overview of the Conformational Ensemble Prediction

3 Generating Starting Structures Based on Templates

4 BiHelix: TM Bundle Conformational Sampling of Helix Rotation Angles

5 SuperBiHelix TM Bundle Sampling of All Helix Orientation Angles

6 Effect of Mutations on the WT Conformational Ensemble

7 Ensemble Docking of Ligands to WT or Mutant Receptors

8 Summary


Chapter Three. Structural Evolution of G-Protein-Coupled Receptors


1 Introduction

2 The Puzzle of GPCR Evolution

3 The Evolution of Class A GPCRs Viewed by MDS

4 Evolutionary Trends

5 Structural Evolution of GPCRs

6 Summary


Chapter Four. Directed Evolution of G-Protein-Coupled Receptors for High Functional Expression and Detergent Stability

1 Introduction

2 Methods


Chapter Five. The Role of Hydrophobic Amino Acids in the Structure and Function of the Rhodopsin Family of G Protein-Coupled Receptors

1 Introduction

2 The Structure of GPCRs

3 Sequence Analyses of the 7TM Segments of the Rhodopsin Family of GPCRs

4 Importance of the Highly Conserved Hydrophobic Amino Acid at Position 3.40 in the Process of Agonist-Induced Receptor Activation

5 The Hydro


This new volume of Methods in Enzymology continues the legacy of this premier serial by containing quality chapters authored by leaders in the field. This volume covers G protein coupled receptors and includes chapters on such topics as post-translation modification of GPCR in relationship to biased agonism, structure-based virtual screening, and GPCR oligomerization in the brain.

Key Features

  • Continues the legacy of this premier serial with quality chapters authored by leaders in the field
  • Covers G protein coupled receptors
  • Contains chapters on such topics as post-translation modification of GPCR in relationship to biased agonism, structure-based virtual screening, and GPCR oligomerization in the brain


Biochemists, biophysicists, molecular biologists, analytical chemists, and physiologists


No. of pages:
© Academic Press 2013
Academic Press
eBook ISBN:
Hardcover ISBN:

About the Serial Volume Editors

P. Michael Conn Serial Volume Editor

P. Michael Conn is the Senior Vice President for Research and Associate Provost, Texas Tech Health Sciences Center. He is The Robert C. Kimbrough, Professor of Internal Medicine and Cell Biology/Biochemistry. He was previously Director of Research Advocacy and Professor of Physiology and Pharmacology, Cell Biology and Development and Obstetrics and Gynecology at Oregon Health and Science University and Senior Scientist of the Oregon National Primate Research Center (ONPRC). He served for twelve years as Special Assistant to the President and Associate Director of the ONPRC. After receiving a B.S. degree and teaching certification from the University of Michigan (1971), a M.S. from North Carolina State University (1973), and a Ph.D. degree from Baylor College of Medicine (1976), Conn did a fellowship at the NIH, then joined the faculty in the Department of Pharmacology, Duke University Medical Center where he was promoted to Associate Professor in 1982. In 1984, he became Professor and Head of Pharmacology at the University of Iowa College of Medicine, a position he held for eleven years. Conn is known for his research in the area of the cellular and molecular basis of action of gonadotropin releasing hormone action in the pituitary and therapeutic approaches that restore misfolded proteins to function. His work has led to drugs that have benefitted humans and animals. Most recently, he has identified a new class of drugs, pharmacoperones, which act by regulating the intracellular trafficking of receptors, enzymes and ion channels. He has authored or co-authored over 350 publications in this area and written or edited over 200 books, including texts in neurosciences, molecular biology and endocrinology. Conn has served as the editor of many professional journals and book series (Endocrinology, Journal of Clinical Endocrinology and Metabolism, Endocrine, Methods, Progress in Molecular Biology and Translational Science and Contemporary Endocrinology). Conn serve

Affiliations and Expertise

Texas Tech University Health Sciences Center, Lubbock, USA