G Protein Coupled Receptors: Modeling, Activation, Interactions and Virtual Screening Volume 522

ISBN-13: 9780124078659 / Angielski / Twarda / 2013 / 528 str.

P Michael Conn

Opis

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

Spis treści

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

Computational Design and Experimental Characterization of GPCR Segment Models

GPCR Interactions with Other Molecules and Cross-Talk

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

GPCR Bias

12. Biasing the Parathyroid Hormone Receptor: Relating In Vitro Ligand Efficacy to In Vivo Biological Activity

Virtual Screening

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

GPCR Activation

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

O autorze

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 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. Conn is a previous member of Council for the American Society for Cell Biology and the Endocrine Society and is a prior President of the Endocrine Society, during which time he founded the Hormone Foundation and worked with political leadership to heighten the public's awareness of diabetes. Conn's students and fellows have gone on to become leaders in industry and academia. He is an elected member of the Mexican Institute of Medicine and a fellow of the American Association for the Advancement of Science. He is the co-author of The Animal Research War (2008) and many articles for the public and academic community on the value of animal research and the dangers posed by animal extremism. His op/eds have appeared in The Washington Post, The LA Times, The Wall Street Journal, the Des Moines Register, and elsewhere. Conn consults with organizations that are influenced by animal extremism and with universities and companies facing challenges from these groups.