Constitutive Activity in Receptors & Oth

Covers the methodology for the detection and assessment of constitutively active proteins.

List of contents

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 ?1a and ?1b 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. ?-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 ?-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) inve

Product details

• Authors: P.michael Conn
• Assisted by: P. Michael Conn (Editor), Melvin I. Simon (Editor)
• Publisher: Academic Press London
• Languages: English
• Product format: Hardback
• Release: 15.12.2010, delayed
• EAN: 9780123812964
• ISBN: 978-0-12-381296-4
• No. of pages: 250
• Series: Academic Press; Academic Press; Methods in Enzymology
• Subjects: Natural sciences, medicine, IT, technology > Biology > General, dictionaries; SCIENCE / Life Sciences / Biochemistry, biochemistry, proteins