G Protein Coupled Receptors: Modeling, Activation, Interactions and Virtual Screening

Overview

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.


  • Continues the legacy of this premier serial with quality chapters authored by leaders in ...
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G Protein Coupled Receptors: Modeling, Activation, Interactions and Virtual Screening

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Overview

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.


  • 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.
Read More Show Less

Product Details

  • ISBN-13: 9780124078659
  • Publisher: Elsevier Science
  • Publication date: 3/1/2013
  • Pages: 528
  • Product dimensions: 6.00 (w) x 9.10 (h) x 1.00 (d)

Meet the Author

P. Michael Conn is the Senior Vice President for Research and Associate Provost, Texas Tech Health Sciences Center. 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. 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 served on the National Board of Medical Examiners, including two years as chairman of the reproduction and endocrinology committee. The work of his laboratory has been recognized with a MERIT award from the NIH, the J.J. Abel Award of the American Society for Pharmacology and Experimental Therapeutics, the Weitzman, Oppenheimer and Ingbar Awards of the Endocrine Society, the National Science Medal of Mexico (the Miguel Aleman Prize) and the Stevenson Award of Canada. He is the recipient of the Oregon State Award for Discovery, the Media Award of the American College of Neuropsychopharmacology and was named a distinguished Alumnus of Baylor College of Medicine in 2012. He is an elected member of the Mexican Institute of Medicine and a fellow of the American Association for the Advancement of Science.

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Table of Contents

GPCR Modeling

  1. The Protein Local Optimization Program and G-Protein Coupled Receptors: Loop Restoration and Applications to Homology Modeling
  2. Modeling Active GPCR Conformations
  3. Molecular Modeling of Adenosine Receptors
  4. Predicting G Protein-Coupled Receptors Families using Different Physiochemical Properties and Pseudo Amino Acid Composition
  5. Computational Design and Experimental Characterization of GPCR Segment Models

    GPCR Interactions with Other Molecules and Cross-Talk

  6. G Protein-Coupled Receptor Interaction with Small GTPases
  7. Quantification of Receptor Tyrosine Kinase Activation and Transactivation by G Protein Coupled Receptors Using Spatial Intensity Distribution Analysis (SpIDA)
  8. NMR Methods for Detection of Small Molecule Binding to RGS4
  9. Group II Activators of G-protein Signaling: Monitoring the Interaction of Ga with the G-Protein Regulatory Motif in the Intact Cell
  10. Homogeneous Time-Resolved Fluorescence Assay to Probe Folded G Protein-Coupled Receptors
  11. cAMP Biosensors Applied in Molecular Pharmacological Studies of G Protein-Coupled Receptors
  12. Rhodopsin-Lipid Interactions Studied by NMR
  13. GPCR Bias

  14. Biasing the Parathyroid Hormone Receptor: Relating In Vitro Ligand Efficacy to In Vivo Biological Activity
  15. Virtual Screening

  16. Application of Monte Carlo-based Receptor-Ensemble Docking to Virtual Screening for GPCR Ligands
  17. From Heptahelical Bundle to Hits from the Haystack: Structure-Based Virtual Screening for GPCR Ligands
  18. GPCR Activation

  19. Kinetics and Dynamics in the G-Protein Coupled Receptor Signaling Cascade
  20. Magic Angle Spinning Nuclear Magnetic Resonance Spectroscopy of G Protein-Coupled Receptors
  21. Post-Translation Modification of G Protein-Coupled Receptor in Relationship to Biased Agonism
  22. Protein S-Nitrosylation Measurement
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