Actions for Constitutive activity in receptors and other proteins. Part A [electronic resource]

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Constitutive activity in receptors and other proteins. Part A [electronic resource] / volume editor, Melvin I. Simon

Published
San Diego : Academic Press, 2010.
Physical Description
1 online resource (xxv, 747 pages)
Additional Creators
Simon, Melvin I.
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Contents
Machine generated contents note: Section I Identification and Measurement of Constitutive Activity -- 1.Constitutive Activity at the Cannabinoid CB1 Receptor and Behavioral Responses / Todd W. Vanderah -- 1.Introduction -- 2.Modifying CB1 Activity -- 3.Behavioral Models -- References -- 2.Detecting Constitutive Activity and Protean Agonism at Cannabinoid-2 Receptor / Paola Scandroglio -- 1.Introduction -- 2.General Considerations -- 3.Evaluation of Constitutive Activity Using GTPγS Assay -- 4.Evaluation of Constitutive Activity Using cAMP Assay -- 5.Evaluation of Constitutive Activity Using RT-CES -- 6.Evaluation of Protean Agonism with cAMP Assay -- 7.Comparison of the Methods -- References -- 3.Modulation of the Constitutive Activity of the Ghrelin Receptor by Use of Pharmacological Tools and Mutagenesis / Birgitte Holst -- 1.Introduction -- 2.The Ghrelin Receptor and its Constitutive Activity -- 3.Structural Basis of Constitutive Activity -- 4.Residues Responsible for the Inverse Agonism and Efficacy Swap -- 5.Physiological Relevance of Constitutive Activity -- 6.Experimental Procedures -- References -- 4.Assessment of Constitutive Activity and Internalization of GPR54 (KISS1-R) / Andy V. Babwah -- 1.Introduction -- 2.Materials -- 3.Methods -- Acknowledgment -- References -- 5.Assessment of Constitutive Activity in E-Type Prostanoid Receptors / John W. Regan -- 1.Introduction -- 2.Assays Used to Assess EP3 Receptor Constitutive Activity -- 3.Assays Used to Assess EP4 Receptor Constitutive Activity -- References -- 6.α1D-Adrenergic Receptors: Constitutive Activity and Reduced Expression at the Plasma Membrane / Luz del Carmen Medina -- 1.Introduction -- 2.Methods -- 3.Constitutive Activity -- 4.Plasma Membrane α1D-Adrenergic Receptors -- 5.Possible Physiological Implications -- Acknowledgments -- References -- 7.Constitutive Activity of the Histamine H1 Receptor / Henry F. Vischer -- 1.Introduction -- 2.Methods to Study Constitutive H1R Signaling -- 3.Constitutive Activity as Tool to Elucidate Receptor Activation and Crosstalk -- 4.Conclusion -- Acknowledgments -- References -- 8.Constitutive Activity of Somatostatin Receptor Subtypes / Shlomo Melmed -- 1.Introduction -- 2.Choosing Cells to be Studied -- 3.Modifying SSTR Density -- 4.Summary -- References -- 9.Assessment of Homologous Internalization of Constitutively Active N111G Mutant of AT1 Receptor / Takafumi Nagatomo -- 1.Introduction -- 2.Preparation of Receptor Plasmid and Protein -- 3.Radioligand Binding Assay -- 4.Inositol Phosphate Accumulation Assay -- 5.Internalization Assay -- 6.Western Blot Analysis -- 7.Data Analysis -- 8.Concluding Remark -- References -- 10.Methods to Detect Cell Surface Expression and Constitutive Activity of GPR6 / Nevin A. Lambert -- 1.Introduction -- 2.GPR6 is Expressed in Intracellular Compartments -- 3.Comparison of the Cell Surface Protein Detection Methods -- 4.Comparison of the Constitutive Gs-Activity Detection Methods -- 5.Conclusions -- References -- 11.β3-Adrenoceptor Agonists and (Antagonists as) Inverse Agonists: History, Perspective, Constitutive Activity, and Stereospecific Binding / Antonio Scilimati -- 1.Introduction -- 2.β3-Adrenoceptor -- 3.Methodologies -- Acknowledgments -- References -- 12.Constitutive Activity of the Lutropin Receptor and Its Allosteric Modulation by Receptor Heterodimerization / Deborah L. Segaloff -- 1.Introduction -- 2.General Principles for Quantifying Receptor Activation -- 3.Modifying Cell Surface Expression Levels of Recombinant hLHR and Mutants Thereof -- 4.Quantifying Cell Surface hLHR Expression -- 5.Quantifying cAMP Production in Cells Expressing the hLHR -- 6.Experimental Strategies for Characterizing the Attenuating Effects of a Signaling Inactive hLHR on a Coexpressed wt or CAM hLHR -- Acknowledgment -- References -- 13.Assessing Constitutive Activity of Extracellular Calcium-Sensing Receptors in Vitro and in Bone / Dolores Shoback -- 1.Introduction -- 2.Materials and Methods -- 3.Results -- 4.Conclusions -- Acknowledgments -- References -- 14.Constitutive Activity of Neural Melanocortin Receptors / Gregory V. Nikiforovich -- 1.Introduction -- 2.Signaling Assay for the Neural Melanocortin Receptors -- 3.Naturally Occuring Constitutively Active MC4R Mutants -- 4.Inverse Agonism of AgRP at the MC3R -- 5.Computational Modeling of the Constitutively Active MC4R Mutants -- Acknowledgments -- References -- 15.Measurement of Constitutive Activity of BMP Type I Receptors / Peter ten Dijke -- 1.Introduction -- 2.Determining ALK2 Constitutive Activity -- 3.Determining the Effects of ALK2 Constitutive Activity on Osteoblast Differentiation -- 4.Concluding Remarks -- Acknowledgments -- References -- 16.Probing the Constitutive Activity Among Dopamine D1 and D5 Receptors and Their Mutants / Mario Tiberi -- 1.Introduction -- 2.Design of Genetically Modified D1-Like Receptor Constructs and Cloning Strategy -- 3.Transfection of D1R and D5R Expression Constructs in HEK293 Cells -- 4.Radioligand-Binding Assays -- 5.Whole Cell cAMP Assays -- 6.Results Validating Experimental Approaches -- 7.Concluding Remarks -- Acknowledgments -- References -- 17.Identification of Gain-of-Function Variants of the Human Prolctin Receptor / Philippe Touraine -- 1.Introduction -- 2.Experimental Procedures -- 3.Identification of Constitutive Activity: Results and Discussion -- 4.Conclusions -- Acknowledgments -- References -- 18.Investigations of Activated ACVR1/ALK2, a Bone Morphogenetic Protein Type I Receptor, That Causes Fibrodysplasia Ossificans Progressiva / Eileen M. Shore -- 1.Introduction -- 2.Patient Methodologies -- 3.Cellular Methodologies -- 4.Tissue Methodologies -- 5.In Vivo Methodologies -- Acknowledgments -- References -- 19.Identification and Evaluation of Constitutively Active Thyroid Stimulating Hormone Receptor Mutations / Isabel Castro-Piedras -- 1.Introduction -- 2.TSHR Gene Mutational Screening -- 3.Determination of TSHR Constitutive Activity In Vitro -- 4.Measurement of TSHR Expression at Cell Surface by Flow Cytometry Analysis -- 5.TSH-TSHR Binding Assays -- 6.TSHR Phosphorylation Analysis -- Acknowledgments -- References -- 20.Assessment of Constitutive Activity of a G Protein-Coupled Receptor, Cpr2, in Cryptococcus neoformans by Heterologous and Homologous Methods / Yen-Ping Hsueh -- 1.Introduction of Receptors and Constitutive Receptors -- 2.Identification of Cpr2 as a Natural Occuring Constitutively Active Receptor -- 3.Additional Constitutively Active Receptors Identified in Fungi -- Acknowledgments -- References -- 21.In Vitro and In Vivo Assessment of Mu Opioid Receptor Constitutive Activity / Richard B. Rothman -- 1.Introduction -- 2.Measuring Opioid Receptor Constitutive Activity in Vitro -- 3.cAMP Quantification Assay in CHO Cells Expressing Cloned Opioid Receptors -- 4.In Vivo Assessment of Antagonist Potency in Opioid Naive Subjects -- 5.In Vivo Assessment of Antagonist Potency to Precipitate Withdrawal -- 6.Summary -- Acknowledgments -- References -- 22.Constitutively Active μ-Opioid Receptors / John Traynor -- 1.Introduction -- 2.Methods for Measuring Constitutive Activity -- 3.Conclusions -- Acknowledgments -- References -- 23.Protein Kinase CK2 is a Constitutively Active Enzyme that Promotes Cell Survival: Strategies to Identify CK2 Substrates and Manipulate its Activity in Mammalian Cells / David W. Litchfield -- 1.Introduction -- 2.Purification of CK2 for In Vitro Studies -- 3.Assays for CK2 Activity -- 4.Modulation of CK2 in Mammalian Cells -- 5.Conclusions -- Acknowledgments -- References -- 24.Assessment of CK2 Constitutive Activity in Cancer Cells / Lorenzo A. Pinna -- 1.Introduction -- 2.Assay of CK2 in Crude Biological Samples -- 3.In-Cell Assay of Endogenous CK2 Activity -- 4.Identification/Validation of in Vivo CK2 Targets with Specific Inhibitors -- Acknowledgments.
Subject(s)
ISBN
9780123812988 (Cloth)
0123812984 (Cloth)
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AVAILABLE ONLINE TO AUTHORIZED PSU USERS.
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