Constitutive Activity in Receptors and Other Proteins, Part B

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.

1. Identification and characterization of Steroidogenic Factor-1 inverse agonists.

Mabrouka Doghman, Franck Madoux, Peter Hodder, and Enzo Lalli

2. Assessment of inverse agonism for the angiotensin II type 1 receptor

Hiroshi Akazawa, Noritaka Yasuda, Shin-ichiro Miura, Issei Komuro

3. Measurement of inverse agonism in BARs

Carlos Alberto Taira

4. Inverse agonism of antidepressants: in vitro and in vivo studies

Joel Bockaert

5. Differential inverse agonism at the human muscarinic M₃ receptor

Paola Casarosa

6. Ghrelin Receptor: High Constitutive Activity and Methods for Developing Inverse Agonists.

Constance Chollet

7. Constitutive activity and inverse agonism at the α1a and α1b adrenergic receptor subtypes.

Susanna. Cotecchia

8. Measurement of inverse agonism of the cannabinoid receptor

Tung Fong

9. Constitutively Active Thyrotropin (TSH) and Thyrotropin-Releasing Hormone (TRH) Receptors and Their Inverse Agonists

Marvin C. Gershengorn

10. Inverse retinoid agonists and neutral antagonists

Hinrich Gronemeyer

11. γ-Aminobutyric Acid Type A (GABA_A) Receptor Subtype Inverse Agonists as Therapeutic Agents in Cognition

Gabriella Guerrini and Ciciani Giovanna

12. Assays for inverse agonists in the visual system.

Masahiro Kono

13. Receptor-driven identification of novel human A3 adenosine receptor antagonists as potential therapeutic agents

Silvia Paoletta, Stephanie Federico, Giampiero Spalluto and Stefano Moro

14. Inverse agonists of steroidogenic factor SF-1

Fabrice Piu and Andria L. Del Tredici

15. Methods to Measure G Protein Coupled Receptor Activity for the Identification of Inverse Agonists

Gabriel Barreda-Gómez, M.Teresa Giralt and Rafael Rodríguez-Puertas

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

16. Use of Pharmacoperones to Reveal GPCR Structural Components Associated with Receptor Activation and Trafficking

Jo Ann Janovick and P. Michael Conn

17. Application of large-scale transiently transfected cells to functional assays of ion channels and other proteins.

Jun Chen, Sujatha Gopalakrishnan, Marc R Lake, and Bruce R Bianchi

18. Quantification of RNA Editing of the Serotonin 2C Receptor (5-HT2CR) Ex Vivo

Maria Fe Lanfranco, Noelle C. Anastasio, Patricia K. Seitz, and Kathryn A. Cunningham

19. Strategies for isolating constitutively-active and dominant-negative pheromone receptor mutants in yeast.

Mercedes Dosil and James B. Konopka

20. Development of a GPR23 Cell-based β-Lactamase Reporter Assay

Paul H. Lee and Bonnie J. Hanson

21. Computational Modeling of Constitutively Active Mutants of GPCRs: C5a Receptor.

Gregory V. Nikiforovich and Thomas J. Baranski

22. TSH receptor monoclonal antibodies with agonist, antagonist and inverse agonist activities

Jane Sanders, Ricardo Núñez Miguel, Jadwiga Furmaniak, Bernard Rees Smith

23. Current standards, variations and pitfalls for the determination of constitutive TSHR activity in vitro

Sandra Mueller, Holger Jaeschke, Ralf Paschke

24. Towards the Rational Design of Constitutively Active KCa3.1 Mutant Channels

Line Garneau, Hélène Klein, Lucie Parent, Rémy Sauvé

25. Fusion proteins as model systems for the analysis of constitutive GPCR activity

Erich H. Schneider, Roland Seifert

26. Screening for Novel Constitutively Active CXCR2 Mutants and Their Cellular Effects

Giljun Park, Tom Masi, Chang K. Choi, Heejung Kim, Jeffrey M. Becker, and Tim E. Sparer

27. A method for parallel solid-phase synthesis of iodinated analogues of the cannabinoid receptor type I (CB1) inverse agonist rimonabant

Alan C. Spivey and Chih-Chung Tseng

28. Coexpression systems as models for the analysis of constitutive GPCR activity

Roland Seifert and Erich H. Schneider

29. Modelling and simulation of inverse agonism dynamics

Lloyd J. Bridge

30. Design and Use of Constitutively Active STAT5 Constructs

Michael A. Farrar

31. 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