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.
- Expert authors who are leaders in the field
- Extensively referenced and useful figures and tables
- Provides hints and tricks to facilitate reproduction of methods
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Mabrouka Doghman, Franck Madoux, Peter Hodder, and Enzo Lalli
- Assessment of inverse agonism for the angiotensin II type 1 receptor
Hiroshi Akazawa, Noritaka Yasuda, Shin-ichiro Miura, Issei Komuro
- Measurement of inverse agonism in BARs
Carlos Alberto Taira
- Inverse agonism of antidepressants: in vitro and in vivo studies
- Differential inverse agonism at the human muscarinic M3 receptor
- Ghrelin Receptor: High Constitutive Activity and Methods for Developing Inverse Agonists.
- Constitutive activity and inverse agonism at the ?1a and ?1b adrenergic receptor subtypes.
- Measurement of inverse agonism of the cannabinoid receptor
- Constitutively Active Thyrotropin (TSH) and Thyrotropin-Releasing Hormone (TRH) Receptors and Their Inverse Agonists
Marvin C. Gershengorn
- Inverse retinoid agonists and neutral antagonists
- ?-Aminobutyric Acid Type A (GABAA) Receptor Subtype Inverse Agonists as Therapeutic Agents in Cognition
Gabriella Guerrini and Ciciani Giovanna
- Assays for inverse agonists in the visual system.
- Receptor-driven identification of novel human A3 adenosine receptor antagonists as potential therapeutic agents
Silvia Paoletta, Stephanie Federico, Giampiero Spalluto and Stefano Moro
- Inverse agonists of steroidogenic factor SF-1
Fabrice Piu and Andria L. Del Tredici
- 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
- Use of Pharmacoperones to Reveal GPCR Structural Components Associated with Receptor Activation and Trafficking
Jo Ann Janovick and P. Michael Conn
- 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
- 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
- Strategies for isolating constitutively-active and dominant-negative pheromone receptor mutants in yeast.
Mercedes Dosil and James B. Konopka
- Development of a GPR23 Cell-based ?-Lactamase Reporter Assay
Paul H. Lee and Bonnie J. Hanson
- Computational Modeling of Constitutively Active Mutants of GPCRs: C5a Receptor.
Gregory V. Nikiforovich and Thomas J. Baranski
- TSH receptor monoclonal antibodies with agonist, antagonist and inverse agonist activities
Jane Sanders, Ricardo Núñez Miguel, Jadwiga Furmaniak, Bernard Rees Smith
- Current standards, variations and pitfalls for the determination of constitutive TSHR activity in vitro
Sandra Mueller, Holger Jaeschke, Ralf Paschke
- Towards the Rational Design of Constitutively Active KCa3.1 Mutant Channels
Line Garneau, Hélène Klein, Lucie Parent, Rémy Sauvé
- Fusion proteins as model systems for the analysis of constitutive GPCR activity
Erich H. Schneider, Roland Seifert
- 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
- 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
- Coexpression systems as models for the analysis of constitutive GPCR activity
Roland Seifert and Erich H. Schneider
- Modelling and simulation of inverse agonism dynamics
Lloyd J. Bridge
- Design and Use of Constitutively Active STAT5 Constructs
Michael A. Farrar
- 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