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Constitutive activity in receptors and other proteins /

Autres auteurs : Conn, P. Michael.
Collection : Methods in enzymology ; . 484, 485 Détails physiques : 1 online resource (2 volumes) : illustrations (some color) ISBN :9780123812971 (electronic bk.); 0123812976 (electronic bk.); 9780123812995 (electronic bk.); 0123812992 (electronic bk.); 9780123812964 (electronic bk.); 0123812968 (electronic bk.); 9780123812988 (electronic bk.); 0123812984 (electronic bk.).
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Exemplaires : http://www.sciencedirect.com/science/book/9780123812988
Exemplaires : http://www.sciencedirect.com/science/book/9780123812964

Includes bibliographical references and indexes.

volume 484. Constitutive activity at the cannabinoid CB(1) receptor and behavioral responses -- Detecting constitutive activity and protean agonism at cannabinoid-2 receptor -- Modulation of the constitutive activity of the ghrelin receptor by use of pharmacological tools and mutagenesis -- Assessment of constitutive activity and internalization of GPR54 (KISS1-R) -- Assessment of constitutive activity in E-type prostanoid receptors -- [Alpha](1D-adrenergic receptors constitutive activity and reduced expression at the plasma membrane -- Constitutive activity of the histamine H(1) receptor -- Constitutive activity of somatostatin receptor subtypes -- Assessment of homologous internalization of constitutively active N111G mutant of AT(1) receptor -- Methods to detect cell surface expression and constitutive activity of GPR6 -- [beta](3)-adrenoceptor agonists and (antagonists as) inverse agonists history, perspective, constitutive activity, and stereospecific binding -- Constitutive activity of the lutropin receptor and its allosteric modulation by receptor heterodimerization -- Assessing constitutive activity of extracellular calcium-sensing receptors in vitro and in bone -- Constitutive activity of neural melanocortin receptors -- Measurement of constitutive activity of bmp type I receptors -- Probing the constitutive activity among dopamine D1 and D5 receptors and their mutants -- Identification of gain-of-function variants of the human prolactin receptor -- Investigations of activated ACVR1/ALK2, a bone morphogenetic protein type i receptor, that causes fibrodysplasia ossificans progressiva -- Identification and evaluation of constitutively active thyroid stimulating hormone receptor mutations -- Assessment of constitutive activity of a G protein-coupled receptor, CPR2, in cryptococcus neoformans by heterologous and homologous methods -- In vitro and in vivo assessment of mu opioid receptor constitutive activity -- Constitutively active [mu]-opioid receptors -- Protein kinase CK2 is a constitutively active enzyme that promotes cell survival: Strategies to identify CK2 substrates and manipulate its activity in mammalian cells -- Assessment of CK2 constitutive activity in cancer cells -- Structural basis of the constitutive activity of protein kinase CK2 -- Measuring the constitutive activation of C-jun N-terminal kinase isoforms -- Measurement of constitutive mapk and PI3K/AKT signaling activity in human cancer cell lines -- Constitutive activity of GPR40/FFA1 intrinsic or assay dependent? -- Constitutive activity of trp channels methods for measuring the activity and its outcome -- Measurement of orexin (hypocretin) and substance P effects on constitutively active inward rectifier K(+) channels in brain neurons -- Characterization of G protein-coupled receptor kinase 4 and measuring its constitutive activity in vivo -- Voltage-clamp-based methods for the detection of constitutively active acetylcholine-gated I(K, ACH) channels in the diseased heart -- Assaying WAVE and WASH complex constitutive activities toward the Arp2/3 complex -- Methods to assess the mechanism of protein function.

V.485. 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.

Description based on print version record.

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. A. Expert authors who are leaders in the field B. Extensively referenced and useful figures and tables C. Provides hints and tricks to facilitate reproduction of methods.

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