Constitutive activity in receptors and other proteins, part B - Conn, P. Michael (Amsterdam Elsevier /Academic Press, 2010)
Identification and characterization of steroidogenic factor-1 inverse agonists -- Assessment of inverse agonism for the angiotensin II type 1 receptor -- Measurement of inverse agonism in [beta]-adrenoceptors -- Techniques for studying inverse agonist activity of antidepressants at recombinant nonedited 5-HT(C-INI) receptor and native neuronal 5-HT(2C) receptors -- 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 [alpha](A) and [alpha](B) adrenergic receptor subtypes -- Measurement of inverse agonism of the cannabinoid receptors -- Constitutively active thyrotropin and thyrotropin-releasing hormone receptors and their inverse agonists -- Inverse agonists and antagonists of retinoid receptors -- [gamma]-aminobutyric acid type A (GABA(A)) receptor subtype inverse agonists as therapeutic agents in cognition -- Assays for inverse agonists in the visual system -- Receptor-driven identification of novel human a adenosine receptor antagonists as potential therapeutic agents -- Inverse agonist activity of steroidogenic factor SF-1 -- Methods to measure G-protein-coupled receptor activity for the identification of inverse agonists -- Use of pharmacoperones to reveal GPCR structural changes associated with constitutive activation and trafficking -- Application of large-scale transient transfection to cell-based functional assays for ion channels and GPCRs -- Quantification of RNA editing of the serotonin 2C receptor (5-HT(C)R) ex vivo -- Strategies for isolating constitutively active and dominant-negative pheromone receptor mutants in yeast -- Development of a GPR23 cell-based [beta]-lactamase reporter assay -- Computational modeling of constitutively active mutants of GPCRs C5A receptor -- TSH receptor monoclonal antibodies with agonist, antagonist, and inverse agonist activities -- Current standards, variations, and pitfalls for the determination of constitutive TSHR activity in vitro -- Toward the rational design of constitutively active KCA3.1 mutant channels -- Fusion proteins as model systems for the analysis of constitutive GPCR activity -- Screening for novel constitutively active CXCR2 mutants and their cellular effects -- A method for parallel solid-phase synthesis of iodinated analogs of the cannabinoid receptor type I (CB) inverse agonist rimonabant -- Coexpression systems as models for the analysis of constitutive GPCR activity -- Modeling and simulation of inverse agonism dynamics -- Design and use of constitutively active STAT5 constructs -- In vitro and in vivo assays of protein kinase CK2 activity.
Includes bibliographical references and indexes.
Keywords: Proteins; Proteins -- Metabolism; Cell receptors; G proteins; Electronic books