Constitutive activity in receptors and other proteins B
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| Format: | Buch |
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| Sprache: | English |
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Elsevier, Acad. Press
2010
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| Ausgabe: | 1. ed. |
| Schriftenreihe: | Methods in enzymology
485 |
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| 020 | |a 9780123812964 |9 978-0-12-381296-4 | ||
| 035 | |a (OCoLC)698612057 | ||
| 035 | |a (DE-599)BVBBV036955976 | ||
| 040 | |a DE-604 |b ger |e rakwb | ||
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| 245 | 1 | 0 | |a Constitutive activity in receptors and other proteins |n B |c ed. by P. Michael Conn |
| 250 | |a 1. ed. | ||
| 264 | 1 | |a Amsterdam [u.a.] |b Elsevier, Acad. Press |c 2010 | |
| 300 | |a LIII, 652 S., [7] Bl. |b Ill., graph. Darst. | ||
| 336 | |b txt |2 rdacontent | ||
| 337 | |b n |2 rdamedia | ||
| 338 | |b nc |2 rdacarrier | ||
| 490 | 1 | |a Methods in enzymology |v 485 | |
| 490 | 0 | |a Methods in enzymology |v ... | |
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| 689 | 1 | 1 | |a Aktivierung |g Chemie |0 (DE-588)4141761-6 |D s |
| 689 | 1 | |C b |5 DE-604 | |
| 700 | 1 | |a Conn, Patrick Michael |d 1949-2016 |e Sonstige |0 (DE-588)136758541 |4 oth | |
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| 830 | 0 | |a Methods in enzymology |v 485 |w (DE-604)BV000000938 |9 485 | |
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| 943 | 1 | |a oai:aleph.bib-bvb.de:BVB01-020870949 | |
Datensatz im Suchindex
| DE-BY-TUM_call_number | 0302 CHE 825f 03.1955 A 741 |
|---|---|
| DE-BY-TUM_katkey | 1752676 |
| DE-BY-TUM_location | 03 |
| DE-BY-TUM_media_number | 040030239519 |
| _version_ | 1820865061260886016 |
| adam_text | Contents
Contributors
xv
Preface
xxiii
Volumes in Series
xxv
Section I. Inverse Agonism and Inverse Agonists
1
1.
Identification and Characterization of Steroidogenic
Factor-
1
Inverse Agonists
3
Mabrouka Doghman,
Franck Madoux,
Peter Hodder, and
Enzo
Lalii
1.
Introduction
4
2.
Characterization of Inverse Agonists of SF-1 by uHTS
6
3.
Effect of SF-1 Inverse Agonists on Adrenocortical Tumor Cell
Proliferation and Steroid Production
17
4.
Conclusion
20
Acknowledgments
22
References
22
2.
Assessment of Inverse Agonism for the Angiotensin II
Type
1
Receptor
25
Hiroshi Akazawa, Noritaka Yasuda, Shin-ichiro Miura, and
Issei
Komuro
1.
Introduction
26
2.
Protocol for Cell Culture and Transfection
26
3.
Radioligand Assay for ATi Receptor
27
4.
Protocol for Cell Stretching
28
5.
Assessment of ATt Receptor Activation
30
6.
Conclusion
33
Acknowledgments
34
References
34
3.
Measurement of Inverse Agonism in
ß-Adrenoceptors 37
Carlos
A. Taira, Federico
Monczor, and Christian
Höcht
1.
Introduction: Basal Spontaneous Receptor Activity. The Rise
of the Concept of Inverse Agonism
38
2. ß-Adrenoceptors: Main
Features
42
v¡
Contents
3.
Methodological
Aspects of the Assessment of Inverse Agonist
Properties at
ßAR 45
4.
Clinical Potential Uses of
ßAR
Inverse Agonists
51
References
53
4.
Techniques for Studying Inverse Agonist Activity of Antidepressants
at
Recombinant Nonedited
б-НТгс-імі
Receptor and Native
Neuronal 5-HT2C
Receptors
61
Mathieu Seimandi, Joël
Bockaert, and Philippe
Marin
1.
Introduction
62
2.
Constitutive Activity Toward the Gotq-PLC Effector Pathway
of 5-HT2c.INI Receptors Transiently Expressed in HEK-293 Cells
65
3.
Plasma Membrane Insertion of 5-HT2c.INI Receptors
71
4.
Enhanced Responsiveness of Constitutively Active 5-HT2C
Receptors Upon Prolonged Treatment with Inverse Agonists
73
Acknowledgments
77
References
77
5.
Differential Inverse Agonism at the Human Muscarinic
M3 Receptor
81
Paola Casarosa,
Tobias Kiechle, and Remko A.
Bakker
1.
Introduction to Muscarinic Receptors
82
2.
Role of M3R in Regulating Smooth Muscle Function and Clinical
Use of Anticholinergics
84
3.
In Vitro Assays to Monitor hM3R Activation and Constitutive Activity
85
4.
Constitutive Activity and Receptor Upregulation Studies
95
5.
Physiological Relevance of hM3R Constitutive Activity
98
References
100
6.
Ghrelin Receptor: High Constitutive Activity and Methods for
Developing Inverse Agonists
103
Sylvia Els, Annette G. Beck-Sickinger, and Constance Chollet
1.
Introduction
104
2.
Constitutive Activity and Development of Ghrelin Receptor
Inverse Agonists
105
3.
Synthesis of Ghrelin Receptor Inverse Agonists: Solid-Phase
Peptide
Synthesis (SPPS) 107
4.
Functional Assays for Ghrelin Receptor Inverse Agonists
113
References
цс)
Contents
vii
7.
Constitutive Activity and Inverse Agonism at the ctla and alb
Adrenergic Receptor Subtypes
123
Susanna Cotecchia
1.
Introduction
124
2.
Combination of Computational Modeling and Site-Directed
Mutagenesis of the Receptor to Identify Constitutively
Activating Mutations
127
3.
Measuring Constitutive Activity of Receptor-Mediated Gq Activation
130
4.
Inverse Agonism at the arARs
132
5.
Conclusions
135
Acknowledgments
136
References
136
8.
Measurement of Inverse Agonism of the Cannabinoid Receptors
139
Tung M. Fong
1.
Introduction
139
2.
Gi-cAMP Assay
140
3.
GTPyS Binding Assay
142
4.
Electrophysiological Assays
143
5.
Summary
143
References
144
9.
Constitutively Active Thyrotropin and Thyrotropin-Releasing
Hormone Reteptors and Their Inverse Agonists
147
Susanne
Neumann, Bruce M. Raaka, and Marvin
С
Gershengorn
1.
Introduction
148
2.
TRH-R2 and Its Inverse Agonist Midazolam
149
3.
TSHR and Its Inverse Agonist
NCGCOOlóieSó
153
Acknowledgments
159
References
159
10.
Inverse Agonists and Antagonists of Retinoid Receptors
161
William Bourguet, Angel R.
de Lera,
and Hinrich Gronemeyer
1.
Introduction
162
2.
Functional Classification of Retinoid Receptor Ligands
164
3.
Structural Basis of Retinoid Receptor Action
165
4.
Synthetic Routes and Toolbox for Rational Retinoid Design
169
5.
Protocols for the Study of Ligand Function
177
6.
Chemical Syntheses
190
Acknowledgments
191
References
192
v¡¡¡
Contents
11.
γ
-Aminobutyric
Acid Type A (GABAa) Receptor Subtype Inverse
Agonists as Therapeutic Agents in Cognition
197
Guerrini
Gabriella
and Ciciani
Giovanna
1.
Introduction
198
2.
Inverse Agonism: Definition
203
3.
Negative Allosteric Regulators of GABAa-R in Cognitive Impairment
204
4.
Methods for Evaluating the Affinity and Efficacy at GABAA
Receptor Subtypes
206
5.
Conclusion
208
References
208
12.
Assays for Inverse Agonists in the Visual System
213
Masahiro Kono
1.
Introduction
214
2.
Opsin Preparation
218
3.
Transducin Preparation
219
4.
Transducin Activation Assay
219
Acknowledgments
221
References
221
13.
Receptor-Driven Identification of Novel Human
A3
Adenosine
Receptor Antagonists as Potential Therapeutic Agents
225
Silvia Paoletta, Stephanie
Federico, Giampiero Spalluto,
and
Stefano Moro
1.
Introduction
226
2.
Newer Potential Therapeutic Role of A3 Adenosine Receptors
226
3.
A3 Adenosine Receptor Antagonists
228
4.
Receptor-Based Antagonist Design
231
Acknowledgments
243
References
243
14.
Inverse Agonist Activity of Steroidogenic Factor SF-1
245
Fabrice
Piu
and And
ria
L
Del
Tredici
1.
Introduction
246
2.
SF-1 Inverse Agonism in the R-SAT® Assay of Cellular Proliferation
247
3.
SF-1 Inverse Agonism in Luciferase Transcriptional Assay
251
4.
SF-1 Inverse Agonism in Adrenocortical Cultures
254
Acknowledgments
257
References
257
Contents________________________________________________________jx
15.
Methods to Measure G-Protein-Coupled Receptor Activity
for the Identification of Inverse Agonists
261
Gabriel
Barreda-Gómez,
M.
Teresa
Giralt,
and Rafael
Rodríguez-Puertas
1.
Introduction
262
2.
[35S]GTPyS Binding Assay in Membrane
Homogenates
266
3.
[35S]GTPyS Autoradiography in Brain Sections
270
Acknowledgments
272
References
273
Section II. Novel Strategies and Techniques for
Constitutive Activity and Inverse Agonism
275
16.
Use of Pharmacoperones to Reveal GPCR Structural Changes
Associated with Constitutive Activation and Trafficking
277
Jo Ann Janovick and P. Michael Conn
1.
Introduction
278
2.
Methods for Measuring Receptors and Receptor Activity
279
3.
Assessment of Results
283
4.
Conclusions
290
Acknowledgments
290
References
290
17.
Application of Large-Scale Transient Transfection to Cell-Based
Functional Assays for Ion Channels and GPCRs
293
Jun
Chen, Sujatha Gopalakrishnan, Marc R. Lake, Bruce R.
Bianchi,
John Locklear, and
Regina
M. Reilly
1.
Introduction
294
2.
Large-Scale Transient Transfection
295
3.
Cryopreservation of Cells
296
4.
Application to Ion Channel Assays
297
5.
Application to GPCR Assays
305
6.
Conclusion
308
Acknowledgment
309
References
309
Contents
18.
Quantification
of RNA
Editing of the Serotonin 2C Receptor
(S-HTzcR) Ex Vivo
311
Maria Fe Lanfranco,
Noëlle
С.
Anastasio,
Patricia
К.
Seitz, and
Kathryn A. Cunningham
1.
RNA
Editing of the
5-HT2CR
312
2.
Functional Properties of
б-НТгсИ
Edited Isoforms
314
3.
Current Methods for Quantification of
ö-HTzcR
Editing Events Ex Vivo
315
4.
Quantification of 5-HT2CR Editing Events Ex Vivo with qRT-PCR
318
Acknowledgments
325
References
325
19.
Strategies for Isolating Constitutively Active and
Dominant-Negative Pheromone Receptor Mutants in Yeast
329
Mercedes Dosil and James
B. Konôpka
1.
Introduction
330
2.
Selecting a Yeast Strain and Expression Vector
332
3.
Transforming Plasmids into Yeast
335
4.
Gap-Repair Approach for Targeting Mutagenesis to
Genes on Plasmids
337
5.
Isolation of Constitutively Active Mutants
338
6.
Isolation of Dominant-Negative Mutants
342
7.
Further Methods for Analysis of Mutant Receptors
344
Acknowledgments
347
References
347
20.
Development of a GPR23 Cell-Based
ß-Lactamase
Reporter Assay
349
Paul H. Lee and Bonnie J. Hanson
1.
Introduction
350
2.
GPCR Cell-Based Assays
352
3.
Development of a Cell-Based
ß-Lactamase
Reporter Assay
for Constitutively Active GPR23
357
4.
Identification of GPR23 Inverse Agonists Using
a
ß-Lactamase
Reporter Screen
362
5.
Concluding Remarks
365
Acknowledgments
З66
References
366
Contents xi
21.
Computational Modeling of Constitutively Active Mutants
of GPCRs: C5a Receptor
369
Gregory V. Nikiforovich and Thomas J. Baranski
1.
Introduction
370
2.
Modeling CAMs Based on Experimental Data for the Ground
and Activated States of GPCRs
371
3.
Rotational Sampling of the TM Regions of GPCRs
377
4.
Modeling Structural Mechanisms of Constitutive Activity in C5aRs
382
5.
Conclusions and Perspectives
387
Acknowledgments
387
References
387
22.
TSH Receptor Monoclonal Antibodies with Agonist, Antagonist,
and Inverse Agonist Activities
393
Jane Sanders,
Ricardo
Núñez
Miguel,
Jadwiga Furmaniak,
and Bernard
Rees
Smith
1.
Introduction
394
2.
Production of Monoclonal Antibodies to the TSH
R
with the
Characteristics of Patient Serum Autoantibodies
397
3.
Characterization of 5C9 a Human Autoantibody with TSH
Antagonist and TSH
R
Inverse Agonist Activity
399
4.
Effects of TSHR Mutations on the Activity of MAb 5C9
405
5.
Structure of MAb 5C9 Fab
412
6.
Conclusions
415
Acknowledgment
416
References
417
23.
Current Standards, Variations, and Pitfalls for the
Determination of Constitutive TSHR Activity In Vitro
421
Sandra Mueller,
Holger Jaeschke,
and
Ralf Paschke
1.
Introduction
422
2.
Detection of Constitutive TSHR Activity
425
3.
Methods and Required Materials for LRA
429
4.
Conclusion
432
Acknowledgment
433
References
433
x¡¡
Contents
24.
Toward the Rational Design of Constitutively Active
КСаЗ.1
Mutant Channels
437
Line Garneau,
Hélène
Klein,
Lucie
Parent, and
Rémy Sauvé
1.
Introduction
438
2.
Production of Constitutively Active
КСаЗ.1
Mutant Channels
441
3.
Concluding Remarks c
454
References
455
25.
Fusion Proteins as Model Systems for the Analysis of
Constitutive GPCR Activity
459
Erich H. Schneider and Roland
Seifert
1.
Introduction
460
2.
Expression of Fusion Proteins:
hl^R-Go^
and
hhUR-GAlP
as Paradigms
462
3.
Investigation of GPCR Constitutive Activity with Fusion
Proteins: H4R as Paradigm
466
4.
Application of the Fusion Protein Approach to other GPCRs
476
Acknowledgments
478
References
479
26.
Screening for Novel Constitutively Active CXCR2 Mutants
and Their Cellular Effects
481
Giljun Park, Tom
Masi,
Chang K. Choi, Heejung Kim, Jeffrey M. Becker,
and Tim E. Sparer
1.
Introduction
482
2.
Establishment of a Yeast System to Identify CXCR2 CAMs
483
3.
Establishment of a Mammalian System to Characterize CXCR2 CAMs
490
References
495
27.
A Method for Parallel Solid-Phase Synthesis of lodinated
Analogs of the Cannabinoid Receptor Type
1
(CBj) Inverse
Agonist Rimonabant
499
Alan
С
Spivey and Chih-Chung Tseng
1.
Introduction
500
2.
Concepts for Molecular Imaging
504
3.
Conventional Methods for Preparation of
Radiolabeled
Pharmaceuticals for Imaging the
СЕц
Receptor
504
4.
Parallel Solid-Phase Synthesis of lodinated Analogs of the
CBi Receptor Inverse Agonist Rimonabant
509
5.
Materials and Methods
514
References
523
Contents xiii
28. Coexpression Systems
as
Models
for the Analysis of
Constitutive GPCR Activity
527
Erich H. Schneider and Roland
Seifert
1.
Introduction
528
2.
Coexpression of GPCRs and Signaling Proteins: hH4R as Paradigm
529
3.
Investigation of GPCR Constitutive Activity with Coexpression Systems
535
4.
Application to Other Receptors
554
Acknowledgments
556
References
556
29.
Modeling and Simulation of Inverse Agonism Dynamics
559
L J.
Bridge
1.
Introduction
560
2.
Single-Ligand Analysis
563
3.
Two Competing Ligands
569
4.
Discussion
578
Acknowledgments
581
References
582
30.
Design and Use of Constitutively Active STAT5 Constructs
583
Michael A. Farrar
1.
Introduction
583
2.
Design of Constitutively Active STAT5 Constructs
585
3.
Use of Constitutively Active STAT5 Constructs
589
4.
Concerns with the Use of Constitutively Active STAT5 Constructs
593
Acknowledgments
595
References
595
31.
In Vitro and In Vivo Assays of Protein Kinase CK2 Activity
597
Renaud
Prudent,
Céline F. Sautel, Virginie Moucadel, Béatrice Laudet,
Odile Filhol,
and Claude
Cochet
1.
Introduction
598
2.
Monitoring of CK2 Catalytic Activity in Living Cells
598
3.
Assays of CK2
Subunit
Interaction
601
4.
Visualization of
CK2a-CK2ß
Interaction in Living Cells
603
Acknowledgments
609
References
609
Author Index
611
Subject Index
639
|
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| author_GND | (DE-588)136758541 |
| building | Verbundindex |
| bvnumber | BV036955976 |
| classification_rvk | WC 4355 WE 5240 |
| classification_tum | CHE 825f CHE 893f |
| ctrlnum | (OCoLC)698612057 (DE-599)BVBBV036955976 |
| discipline | Chemie / Pharmazie Biologie |
| edition | 1. ed. |
| format | Book |
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| genre | (DE-588)4143413-4 Aufsatzsammlung gnd-content |
| genre_facet | Aufsatzsammlung |
| id | DE-604.BV036955976 |
| illustrated | Illustrated |
| indexdate | 2024-12-24T00:17:42Z |
| institution | BVB |
| isbn | 9780123812964 |
| language | English |
| oai_aleph_id | oai:aleph.bib-bvb.de:BVB01-020870949 |
| oclc_num | 698612057 |
| open_access_boolean | |
| owner | DE-91G DE-BY-TUM DE-19 DE-BY-UBM DE-355 DE-BY-UBR DE-12 |
| owner_facet | DE-91G DE-BY-TUM DE-19 DE-BY-UBM DE-355 DE-BY-UBR DE-12 |
| physical | LIII, 652 S., [7] Bl. Ill., graph. Darst. |
| publishDate | 2010 |
| publishDateSearch | 2010 |
| publishDateSort | 2010 |
| publisher | Elsevier, Acad. Press |
| record_format | marc |
| series | Methods in enzymology |
| series2 | Methods in enzymology |
| spellingShingle | Constitutive activity in receptors and other proteins Methods in enzymology Rezeptor (DE-588)4049722-7 gnd Aktivierung Chemie (DE-588)4141761-6 gnd G-Protein gekoppelter Rezeptor (DE-588)7723480-7 gnd |
| subject_GND | (DE-588)4049722-7 (DE-588)4141761-6 (DE-588)7723480-7 (DE-588)4143413-4 |
| title | Constitutive activity in receptors and other proteins |
| title_auth | Constitutive activity in receptors and other proteins |
| title_exact_search | Constitutive activity in receptors and other proteins |
| title_full | Constitutive activity in receptors and other proteins B ed. by P. Michael Conn |
| title_fullStr | Constitutive activity in receptors and other proteins B ed. by P. Michael Conn |
| title_full_unstemmed | Constitutive activity in receptors and other proteins B ed. by P. Michael Conn |
| title_short | Constitutive activity in receptors and other proteins |
| title_sort | constitutive activity in receptors and other proteins |
| topic | Rezeptor (DE-588)4049722-7 gnd Aktivierung Chemie (DE-588)4141761-6 gnd G-Protein gekoppelter Rezeptor (DE-588)7723480-7 gnd |
| topic_facet | Rezeptor Aktivierung Chemie G-Protein gekoppelter Rezeptor Aufsatzsammlung |
| url | http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=020870949&sequence=000002&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA |
| volume_link | (DE-604)BV036886201 (DE-604)BV000000938 |
| work_keys_str_mv | AT connpatrickmichael constitutiveactivityinreceptorsandotherproteinsb |