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Constitutive Activity in Receptors and Other Proteins, Part B - 1st Edition - ISBN: 9780123812964, 9780123812971

Constitutive Activity in Receptors and Other Proteins, Part B, Volume 485

1st Edition

Serial Volume Editor: Melvin Simon
Hardcover ISBN: 9780123812964
eBook ISBN: 9780123812971
Imprint: Academic Press
Published Date: 15th November 2010
Page Count: 708
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Table of Contents

    1. Identification and characterization of Steroidogenic Factor-1 inverse agonists.
    2. Mabrouka Doghman, Franck Madoux, Peter Hodder, and Enzo Lalli

    3. Assessment of inverse agonism for the angiotensin II type 1 receptor
    4. Hiroshi Akazawa, Noritaka Yasuda, Shin-ichiro Miura, Issei Komuro

    5. Measurement of inverse agonism in BARs
    6. Carlos Alberto Taira

    7. Inverse agonism of antidepressants: in vitro and in vivo studies
    8. Joel Bockaert

    9. Differential inverse agonism at the human muscarinic M3 receptor
    10. Paola Casarosa

    11. Ghrelin Receptor: High Constitutive Activity and Methods for Developing Inverse Agonists.
    12. Constance Chollet

    13. Constitutive activity and inverse agonism at the α1a and α1b adrenergic receptor subtypes.
    14. Susanna. Cotecchia

    15. Measurement of inverse agonism of the cannabinoid receptor
    16. Tung Fong

    17. Constitutively Active Thyrotropin (TSH) and Thyrotropin-Releasing Hormone (TRH) Receptors and Their Inverse Agonists
    18. Marvin C. Gershengorn

    19. Inverse retinoid agonists and neutral antagonists
    20. Hinrich Gronemeyer

    21. γ-Aminobutyric Acid Type A (GABAA) Receptor Subtype Inverse Agonists as Therapeutic Agents in Cognition
    22. Gabriella Guerrini and Ciciani Giovanna

    23. Assays for inverse agonists in the visual system.
    24. Masahiro Kono

    25. Receptor-driven identification of novel human A3 adenosine receptor antagonists as potential therapeutic agents
    26. Silvia Paoletta, Stephanie Federico, Giampiero Spalluto and Stefano Moro

    27. Inverse agonists of steroidogenic factor SF-1
    28. Fabrice Piu and Andria L. Del Tredici

    29. Methods to Measure G Protein Coupled Receptor Activity for the Identification of Inverse Agonists
    30. Gabriel Barreda-Gómez, M.Teresa Giralt and Rafael Rodríguez-Puertas




      Section II-- Novel Strategies and Techniques for Constitutive Activity and Inverse Agonism

    31. Use of Pharmacoperones to Reveal GPCR Structural Components Associated with Receptor Activation and Trafficking
    32. Jo Ann Janovick and P. Michael Conn

    33. Application of large-scale transiently transfected cells to functional assays of ion channels and other proteins.
    34. Jun Chen, Sujatha Gopalakrishnan, Marc R Lake, and Bruce R Bianchi

    35. Quantification of RNA Editing of the Serotonin 2C Receptor (5-HT2CR) Ex Vivo
    36. Maria Fe Lanfranco, Noelle C. Anastasio, Patricia K. Seitz, and Kathryn A. Cunningham

    37. Strategies for isolating constitutively-active and dominant-negative pheromone receptor mutants in yeast.
    38. Mercedes Dosil and James B. Konopka

    39. Development of a GPR23 Cell-based β-Lactamase Reporter Assay
    40. Paul H. Lee and Bonnie J. Hanson

    41. Computational Modeling of Constitutively Active Mutants of GPCRs: C5a Receptor.
    42. Gregory V. Nikiforovich and Thomas J. Baranski

    43. TSH receptor monoclonal antibodies with agonist, antagonist and inverse agonist activities
    44. Jane Sanders, Ricardo Núñez Miguel, Jadwiga Furmaniak, Bernard Rees Smith

    45. Current standards, variations and pitfalls for the determination of constitutive TSHR activity in vitro
    46. Sandra Mueller, Holger Jaeschke, Ralf Paschke

    47. Towards the Rational Design of Constitutively Active KCa3.1 Mutant Channels
    48. Line Garneau, Hélène Klein, Lucie Parent, Rémy Sauvé

    49. Fusion proteins as model systems for the analysis of constitutive GPCR activity
    50. Erich H. Schneider, Roland Seifert

    51. Screening for Novel Constitutively Active CXCR2 Mutants and Their Cellular Effects
    52. Giljun Park, Tom Masi, Chang K. Choi, Heejung Kim, Jeffrey M. Becker, and Tim E. Sparer

    53. A method for parallel solid-phase synthesis of iodinated analogues of the cannabinoid receptor type I (CB1) inverse agonist rimonabant
    54. Alan C. Spivey and Chih-Chung Tseng

    55. Coexpression systems as models for the analysis of constitutive GPCR activity
    56. Roland Seifert and Erich H. Schneider

    57. Modelling and simulation of inverse agonism dynamics
    58. Lloyd J. Bridge

    59. Design and Use of Constitutively Active STAT5 Constructs
    60. Michael A. Farrar

    61. In vitro and in vivo assays of protein kinase CK2 activity

    Renaud Prudent, Céline F. Sautel, Virginie Moucadel, Béatrice Laudet, Odilhe Filhol, and Claude Cochet

  1. ~


This volume of Methods in Enzymology covers the current methodology for the detection and assessment of constitutively active proteins. The chapters written by expert authors who are leaders in the field, provide hints and tricks not available in primary research publications.It is extensively referenced, with useful figures and tables throughout the volume.

Key Features

  • Expert authors who are leaders in the field
  • Extensively referenced and useful figures and tables
  • Provides hints and tricks to facilitate reproduction of methods


Researchers and students in cell, molecular and developmental biology


No. of pages:
© Academic Press 2010
15th November 2010
Academic Press
Hardcover ISBN:
eBook ISBN:

Ratings and Reviews

About the Serial Volume Editor

Melvin Simon

Affiliations and Expertise

The Salk Institute, La Jolla, CA, USA