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E-grāmata: Constitutive Activity in Receptors and Other Proteins, Part B

Volume editor Melvin I. Simon (The Salk Institute, La Jolla, CA, USA)

Formāts: PDF+DRM
Sērija : Methods in Enzymology
Izdošanas datums: 24-Nov-2010
Izdevniecība: Academic Press Inc
Valoda: eng
ISBN-13: 9780123812971

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Proteins

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Formāts: PDF+DRM
Sērija : Methods in Enzymology
Izdošanas datums: 24-Nov-2010
Izdevniecība: Academic Press Inc
Valoda: eng
ISBN-13: 9780123812971

Citas grāmatas par šo tēmu:

Proteins

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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

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

Papildus informācija

This volume of Methods in Enzymology covers the current methodology for the detection and assessment of constitutively active proteins.

Contributors

Preface

xxiil

Volumes in Series

xxv

Section I Inverse Agonism and Inverse Agonists

(274)

1 Identification and Characterization of Steroidogenic Factor-1 Inverse Agonists

(22)

Mabrouka Doghman

Franck Madoux

Peter Hodder

Enzo Lalli

1 Introduction

(2)

2 Characterization of Inverse Agonists of SF-1 by uHTS

(11)

3 Effect of SF-1 Inverse Agonists on Adrenocortical Tumor Cell Proliferation and Sterold Production

(3)

4 Conclusion

(2)

Acknowledgments

(1)

References

(3)

2 Assessment of Inverse Agonism for the Angiotensin II Type 1 Receptor

(12)

Hiroshi Akazawa

Noritaka Yasuda

Shin-Ichiro Miura

Issei Komuro

1 Introduction

(1)

2 Protocol for Cell Culture and Transfection

(1)

3 Radioligand Assay for AT1 Receptor

(1)

4 Protocol for Cell Stretching

(2)

5 Assessment of AT1 Receptor Activation

(3)

6 Conclusion

(1)

Acknowledgments

(1)

References

(3)

3 Measurement of Inverse Agonism in β-Adrenoceptors

(24)

Carlos A. Taira

Federico Monczor

Christian Hocht

1 Introduction: Basal Spontaneous Receptor Activity. The Rise of the Concept of Inverse Agonism

(4)

2 β-Adrenoceptors: Main Features

(3)

3 Methodological Aspects of the Assessment of Inverse Agonist Properties at βAR

(6)

4 Clinical Potential Uses of βAR Inverse Agonists

(2)

References

(8)

4 Techniques for Studying Inverse Agonist Activity of Antidepressants at Recombinant Nonedited 5-HT2C-INI Receptor and Native Neuronal 5-HT2C Receptors

(20)

Mathieu Seimandi

Joel Bockaert

Philippe Marin

1 Introduction

(3)

2 Constitutive Activity Toward the Gαq-PLC Effector Pathway of 5-HT2C-INI Receptors Transiently Expressed in HEK-293 Cells

(6)

3 Plasma Membrane Insertion of 5-HT2C-INI Receptors

(2)

4 Enhanced Responsiveness of Constitutively Active 5-HT2C Receptors Upon Prolonged Treatment with Inverse Agonists

(4)

Acknowledgments

(1)

References

(4)

5 Differential Inverse Agonism at the Human Muscarinic M3 Receptor

(22)

Paola Casarosa

Tobias Kiechle

Remko A. Bakker

1 Introduction to Muscarinic Receptors

(2)

2 Role of M3R in Regulating Smooth Muscle Function and Clinical Use of Anticholinergics

(1)

3 In Vitro Assays to Monitor hM3R Activation and Constitutive Activity

(10)

4 Constitutive Activity and Receptor Upregulation Studies

(3)

5 Physiological Relevance of hM3R Constitutive Activity

(2)

References

100

(3)

6 Ghrelin Receptor: High Constitutive Activity and Methods for Developing Inverse Agonists

103

(20)

Sylvia Els

Annette G. Beck-Sickinger

Constance Chollet

1 Introduction

104

(1)

2 Constitutive Activity and Development of Ghrelin Receptor Inverse Agonists

105

(2)

3 Synthesis of Ghrelin Receptor Inverse Agonists: Solid-Phase Peptide Synthesis (SPPS)

107

(6)

4 Functional Assays for Ghrelin Receptor Inverse Agonists

113

(6)

References

119

(4)

7 Constitutive Activity and Inverse Agonism at the α1a and α1b Adrenergic Receptor Subtypes

123

(16)

Susanna Cotecchia

1 Introduction

124

(3)

2 Combination of Computational Modeling and Site-Directed Mutagenesis of the Receptor to Identify Constitutively Activating Mutations

127

(3)

3 Measuring Constitutive Activity of Receptor-Mediated Gq Activation

130

(2)

4 Inverse Agonism at the α1-ARs

132

(3)

5 Conclusions

135

(1)

Acknowledgments

136

(1)

References

136

(3)

8 Measurement of Inverse Agonism of the Cannabinoid Receptors

139

(8)

Tung M. Fong

1 Introduction

139

(1)

2 Gi-cAMP Assay

140

(2)

3 GTPγS Binding Assay

142

(1)

4 Electrophysiological Assays

143

(1)

5 Summary

143

(1)

References

144

(3)

9 Constitutively Active Thyrotropin and Thyrotropin-Releasing Hormone Receptors and Their Inverse Agonists

147

(14)

Susanne Neumann

Bruce M. Raaka

Marvin C. Gershengorn

1 Introduction

148

(1)

2 TRH-R2 and Its Inverse Agonist Midazolam

149

(4)

3 TSHR and Its Inverse Agonist NCGC00161856

153

(6)

Acknowledgments

159

(1)

References

159

(2)

10 Inverse Agonists and Antagonists of Retinoid Receptors

161

(36)

William Bourguet

Angel R. de Lera

Hinrich Gronemeyer

1 Introduction

162

(2)

2 Functional Classification of Retinoid Receptor Ligands

164

(1)

3 Structural Basis of Retinoid Receptor Action

165

(4)

4 Synthetic Routes and Toolbox for Rational Retinoid Design

169

(8)

5 Protocols for the Study of Ligand Function

177

(13)

6 Chemical Syntheses

190

(1)

Acknowledgments

191

(1)

References

192

(5)

11 γ-Aminobutyric Acid Type A (GABAA) Receptor Subtype Inverse Agonists as Therapeutic Agents in Cognition

197

(16)

Guerrini Gabriella

Ciciani Giovanna

1 Introduction

198

(5)

2 Inverse Agonism: Definition

203

(1)

3 Negative Allosteric Regulators of GABAA-R in Cognitive Impairment

204

(2)

4 Methods for Evaluating the Affinity and Efficacy at GABAA Receptor Subtypes

206

(2)

5 Conclusion

208

(1)

References

208

(5)

12 Assays for Inverse Agonists in the Visual System

213

(12)

Masahiro Kono

1 Introduction

214

(4)

2 Opsin Preparation

218

(1)

3 Transducin Preparation

219

(1)

4 Transducin Activation Assay

219

(2)

Acknowledgments

221

(1)

References

221

(4)

13 Receptor-Driven Identification of Novel Human A3 Adenosine Receptor Antagonists as Potential Therapeutic Agents

225

(20)

Silvia Paoletta

Stephanie Federico

Giampiero Spalluto

Stefano Moro

1 Introduction

226

(1)

2 Newer Potential Therapeutic Role of A3 Adenosine Receptors

226

(2)

3 A3 Adenosine Receptor Antagonists

228

(3)

4 Receptor-Based Antagonist Design

231

(12)

Acknowledgments

243

(1)

References

243

(2)

14 Inverse Agonist Activity of Steroidogenic Factor SF-1

245

(16)

Fabrice Piu

Andria L. Del Tredici

1 Introduction

246

(1)

2 SF-1 Inverse Agonism in the R-SAT® Assay of Cellular Proliferation

247

(4)

3 SF-1 Inverse Agonism in Luciferase Transcriptional Assay

251

(3)

4 SF-1 Inverse Agonism in Adrenocortical Cultures

254

(3)

Acknowledgments

257

(1)

References

257

(4)

15 Methods to Measure G-Protein-Coupled Receptor Activity for the Identification of Inverse Agonists

261

(14)

Gabriel Barreda-Gomez

M. Teresa Giralt

Rafael Rodriguez-Puertas

1 Introduction

262

(4)

2 [ 35S]GTPγS Binding Assay in Membrane Homogenates

266

(4)

3 [ 35S]GTPγS Autoradiography in Brain Sections

270

(2)

Acknowledgments

272

(1)

References

273

(2)

Section II Novel Strategies and Techniques for Constitutive Activity and Inverse Agonism

275

(336)

16 Use of Pharmacoperones to Reveal GPCR Structural Changes Associated with Constitutive Activation and Trafficking

277

(16)

Jo Ann Janovick

P. Michael Conn

1 Introduction

278

(1)

2 Methods for Measuring Receptors and Receptor Activity

279

(4)

3 Assessment of Results

283

(7)

4 Conclusions

290

(1)

Acknowledgments

290

(1)

References

290

(3)

17 Application of Large-Scale Transient Transfection to Cell-Based Functional Assays for Ion Channels and GPCRs

293

(18)

Jun Chen

Sujatha Gopalakrishnan

Marc R. Lake

Bruce R. Bianchi

John Locklear

Regina M. Reilly

1 Introduction

294

(1)

2 Large-Scale Transient Transfection

295

(1)

3 Cryopreservation of Cells

296

(1)

4 Application to Ion Channel Assays

297

(8)

5 Application to GPCR Assays

305

(3)

6 Conclusion

308

(1)

Acknowledgment

309

(1)

References

309

(2)

18 Quantification of RNA Editing of the Serotonin 2C Receptor (5-HT2CR) Ex Vivo

311

(18)

Maria Fe Lanfranco

Noelle C. Anastasio

Patricia K. Seitz

Kathryn A. Cunningham

1 RNA Editing of the 5-HT2CR

312

(2)

2 Functional Properties of 5-HT2CR Edited Isoforms

314

(1)

3 Current Methods for Quantification of 5-HT2CR Editing Events Ex Vivo

315

(3)

4 Quantification of 5-HT2CR Editing Events Ex Vivo with qRT-PCR

318

(7)

Acknowledgments

325

(1)

References

325

(4)

19 Strategies for Isolating Constitutively Active and Dominant-Negative Pheromone Receptor Mutants in Yeast

329

(20)

Mercedes Dosil

James B. Konopka

1 Introduction

330

(2)

2 Selecting a Yeast Strain and Expression Vector

332

(3)

3 Transforming Plasmids into Yeast

335

(2)

4 "Gap-Repair" Approach for Targeting Mutagenesis to Genes on Plasmids

337

(1)

5 Isolation of Constitutively Active Mutants

338

(4)

6 Isolation of Dominant-Negative Mutants

342

(2)

7 Further Methods for Analysis of Mutant Receptors

344

(3)

Acknowledgments

347

(1)

References

347

(2)

20 Development of a GPR23 Cell-Based β-Lactamase Reporter Assay

349

(20)

Paul H. Lee

Bonnie J. Hanson

1 Introduction

350

(2)

2 GPCR Cell-Based Assays

352

(5)

3 Development of a Cell-Based β-Lactamase Reporter Assay for Constitutively Active GPR23

357

(5)

4 Identification of GPR23 Inverse Agonists Using a β-Lactamase Reporter Screen

362

(3)

5 Concluding Remarks

365

(1)

Acknowledgments

366

(1)

References

366

(3)

21 Computational Modeling of Constitutively Active Mutants of GPCRs: C5a Receptor

369

(24)

Gregory V. Nikiforovich

Thomas J. Baranski

1 Introduction

370

(1)

2 Modeling CAMs Based on Experimental Data for the Ground and Activated States of GPCRs

371

(6)

3 Rotational Sampling of the TM Regions of GPCRs

377

(5)

4 Modeling Structural Mechanisms of Constitutive Activity in C5aRs

382

(5)

5 Conclusions and Perspectives

387

(1)

Acknowledgments

387

(1)

References

387

(6)

22 TSH Receptor Monoclonal Antibodies with Agonist, Antagonist, and Inverse Agonist Activities

393

(28)

Jane Sanders

Ricardo Nunez Miguel

Jadwiga Furmaniak

Bernard Rees Smith

1 Introduction

394

(3)

2 Production of Monoclonal Antibodies to the TSHR with the Characteristics of Patient Serum Autoantibodies

397

(2)

3 Characterization of 5C9 a Human Autoantibody with TSH Antagonist and TSHR Inverse Agonist Activity

399

(6)

4 Effects of TSHR Mutations on the Activity of MAb 5C9

405

(7)

5 Structure of MAb 5C9 Fab

412

(3)

6 Conclusions

415

(1)

Acknowledgment

416

(1)

References

417

(4)

23 Current Standards, Variations, and Pitfalls for the Determination of Constitutive TSHR Activity In Vitro

421

(16)

Sandra Mueller

Holger Jaeschke

Ralf Paschke

1 Introduction

422

(3)

2 Detection of Constitutive TSHR Activity

425

(4)

3 Methods and Required Materials for LRA

429

(3)

4 Conclusion

432

(1)

Acknowledgment

433

(1)

References

433

(4)

24 Toward the Rational Design of Constitutively Active KCa3.1 Mutant Channels

437

(22)

Line Garneau

Helene Klein

Lucie Parent

Remy Sauve

1 Introduction

438

(3)

2 Production of Constitutively Active KCa3.1 Mutant Channels

441

(13)

3 Concluding Remarks

454

(1)

References

455

(4)

25 Fusion Proteins as Model Systems for the Analysis of Constitutive GPCR Activity

459

(22)

Erich H. Schnelder

Roland Seifert

1 Introduction

460

(2)

2 Expression of Fusion Proteins: hH4R-Gα12 and hH4R-GAIP as Paradigms

462

(4)

3 Investigation of GPCR Constitutive Activity with Fusion Proteins: H4R as Paradigm

466

(10)

4 Application of the Fusion Protein Approach to other GPCRs

476

(2)

Acknowledgments

478

(1)

References

479

(2)

26 Screening for Novel Constitutively Active CXCR2 Mutants and Their Cellular Effects

481

(18)

Giljun Park

Tom Masi

Chang K. Choi

Heejung Kim

Jeffrey M. Becker

Tim E. Sparer

1 Introduction

482

(1)

2 Establishment of a Yeast System to Identify CXCR2 CAMs

483

(7)

3 Establishment of a Mammalian System to Characterize CXCR2 CAMs

490

(5)

References

495

(4)

27 A Method for Parallel Solid-Phase Synthesis of Iodinated Analogs of the Cannabinoid Receptor Type I (CB1) Inverse Agonist Rimonabant

499

(28)

Alan C. Spivey

Chih-Chung Tseng

1 Introduction

500

(4)

2 Concepts for Molecular Imaging

504

(1)

3 Conventional Methods for Preparation of Radiolabeled Pharmaceuticals for Imaging the CB1 Receptor

504

(5)

4 Parallel Solid-Phase Synthesis of lodinated Analogs of the CB1 Receptor Inverse Agonist Rimonabant

509

(5)

5 Materials and Methods

514

(9)

References

523

(4)

28 Coexpression Systems as Models for the Analysis of Constitutive GPCR Activity

527

(32)

Erich H. Schnelder

Roland Seifert

1 Introduction

528

(1)

2 Coexpression of GPCRs and Signaling Proteins: hH4R as Paradigm

529

(6)

3 Investigation of GPCR Constitutive Activity with Coexpression Systems

535

(19)

4 Application to Other Receptors

554

(2)

Acknowledgments

556

(1)

References

556

(3)

29 Modeling and Simulation of Inverse Agonism Dynamics

559

(24)

L.J. Bridge

1 Introduction

560

(3)

2 Single-Ligand Analysis

563

(6)

3 Two Competing Ligands

569

(9)

4 Discussion

578

(3)

Acknowledgments

581

(1)

References

582

(1)

30 Design and Use of Constitutively Active STAT5 Constructs

583

(14)

Michael A. Farrar

1 Introduction

583

(2)

2 Design of Constitutively Active STAT5 Constructs

585

(4)

3 Use of Constitutively Active STAT5 Constructs

589

(4)

4 Concerns with the Use of Constitutively Active STAT5 Constructs

593

(2)

Acknowledgments

595

(1)

References

595

(2)

31 In Vitro and In Vivo Assays of Protein Kinase CK2 Activity

597

(14)

Renaud Prudent

Celine F. Sautel

Virginie Moucadel

Beatrice Laudet

Odile Filhol

Claude Cochet

1 Introduction

598

(1)

2 Monitoring of CK2 Catalytic Activity in Living Cells

598

(3)

3 Assays of CK2 Subunit Interaction

601

(2)

4 Visualization of CK2α-CK2β Interaction in Living Cells

603

(6)

Acknowledgments

609

(1)

References

609

(2)

Author Index

611

(28)

Subject Index

639

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E-grāmata: Constitutive Activity in Receptors and Other Proteins, Part B

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