Constitutive Activity in Receptors and Other Proteins, Part B

Constitutive Activity in Receptors and Other Proteins, Part B

1st Edition - November 15, 2010

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  • Editor: P.Michael Conn
  • Hardcover ISBN: 9780123812964
  • eBook ISBN: 9780123812971

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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

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. ~

Product details

  • No. of pages: 708
  • Language: English
  • Copyright: © Academic Press 2010
  • Published: November 15, 2010
  • Imprint: Academic Press
  • Hardcover ISBN: 9780123812964
  • eBook ISBN: 9780123812971

About the Serial Volume Editor

P.Michael Conn

Affiliations and Expertise

The Salk Institute, La Jolla, CA, USA

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