Description

This new volume of Methods in Enzymology continues the legacy of this premier serial with quality chapters authored by leaders in the field. This volume covers G protein coupled receptors, and includes chapters on such topics as GPCR modelling, interactions with other molecules, virtual screening and GPCR activation.

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 GPCR modelling, interactions with other molecules, virtual screening and GPCR activation

Readership

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

Table of Contents

Contributors

Preface

Methods in Enzymology

Chapter One. The Protein Local Optimization Program and G-Protein-Coupled Receptors: Loop Restoration and Applications to Homology Modeling

1 Introduction

2 PLOP Performance for Loop Prediction

3 PLOP and GPCRs

4 Loop Prediction with the Single-Residue Library

5 Loop Prediction with the Dipeptide Library

6 Hierarchical Loop Prediction with Surrounding Side Chain Optimization

7 Additional Sampling Methods

8 VSGB 2.0: The Newest Energy Model Incorporated into PLOP

9 Conclusions

References

Chapter Two. Modeling Active GPCR Conformations

1 Introduction

2 General Approaches

3 Agonist-Induced Activation

4 Simulation Methods

5 Microswitches

6 Biophysical Restraints

7 Virtual Screening

8 Class B GPCRs

References

Chapter Three. Molecular Modeling of Adenosine Receptors

1 Introduction

2 Adenosine A2a Receptor

3 Receptor Modeling

4 Summary

References

Chapter Four. Predicting G-Protein-Coupled Receptors Families Using Different Physiochemical Properties and Pseudo Amino Acid Composition

1 Introduction

2 GPCRs Prediction

3 Performance Evaluation of GPCR Predictor

4 Webserver for GPCR Predictor

5 Concluding Remarks

References

Chapter Five. Computational Design and Experimental Characterization of GPCR Segment Models

1 Introduction

2 Design of GPCR Segment Models

3 Experimental Characterization of GPCR Segment Models

4 Integration of GPCR Segment Models into GPCR Homology Models

5 Summary

References

Chapter Six. G-Protein-Coupled Receptor Interaction with Small GTPases

1 Introduction

2 Assays for GPCR Interaction with Small GTPases

3 Function of GPCR–Small GTPa

Details

No. of pages:
528
Language:
English
Copyright:
© 2013
Published:
Imprint:
Academic Press
eBook ISBN:
9780124079441
Print ISBN:
9780124078659

About the serial-volume-editor

P. Michael Conn

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

Reviews

This new volume of Methods in Enzymology continues the legacy of this premier serial with quality chapters authored by leaders in the field. This volume covers G protein coupled receptors, and includes chapters on such topics as GPCR modelling, interactions with other molecules, virtual screening and GPCR activation.