The kinin system:
Gespeichert in:
| Format: | Buch |
|---|---|
| Sprache: | English |
| Veröffentlicht: |
San Diego [u.a.]
Acad. Press
1997
|
| Schriftenreihe: | The handbook of immunopharmacology
|
| Schlagworte: | |
| Online-Zugang: | Inhaltsverzeichnis |
| Beschreibung: | Includes bibliographies and index |
| Beschreibung: | XX, 349 S. Ill., graph. Darst. |
| ISBN: | 0122493400 |
Internformat
MARC
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| 245 | 1 | 0 | |a The kinin system |c ed. by Stephen G. Farmer |
| 264 | 1 | |a San Diego [u.a.] |b Acad. Press |c 1997 | |
| 300 | |a XX, 349 S. |b Ill., graph. Darst. | ||
| 336 | |b txt |2 rdacontent | ||
| 337 | |b n |2 rdamedia | ||
| 338 | |b nc |2 rdacarrier | ||
| 490 | 0 | |a The handbook of immunopharmacology | |
| 500 | |a Includes bibliographies and index | ||
| 650 | 4 | |a Kinins | |
| 650 | 0 | 7 | |a Kinine |0 (DE-588)4163888-8 |2 gnd |9 rswk-swf |
| 689 | 0 | 0 | |a Kinine |0 (DE-588)4163888-8 |D s |
| 689 | 0 | |5 DE-604 | |
| 700 | 1 | |a Farmer, Stephen G. |e Sonstige |4 oth | |
| 856 | 4 | 2 | |m HEBIS Datenaustausch |q application/pdf |u http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=016026073&sequence=000001&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA |3 Inhaltsverzeichnis |
| 999 | |a oai:aleph.bib-bvb.de:BVB01-016026073 | ||
Datensatz im Suchindex
| _version_ | 1804137097956687872 |
|---|---|
| adam_text | The Kinin
System
edited by
Stephen G Farmer
Bioscience, Zeneca Pharmaceuticals
1800 oncord Pike, Wilmington
DE 19850, USA
ACADEMIC PRESS
San Diego London Boston
New York Sydney Tokyo Toronto
Contents
Contributors xiii
Series Preface xvii
Preface xix
1 Discovery of Bra iykimn and the Kallikrein-Kinin System 1
Wilson T Beraldo and Silvia P Andrade
1 Introduction 1
1 1 The Discovery of Bradykinin and its Release
by Snake Venom 1
2 The Discovery of Kallikrein and Kallidin 2
2 1 Kallikrein 2
2 2 Kallidin (Lys-Bradykinin) 2
3 Isolation and Purification of Bradykinin and
Kallidin 2
3 1 Isolation 2
3 2 Purification 3
4 The Bradykinin Precursor - Kininogen 4
5 Kinin Inactivators - Kininases 4
5 1 Kininase Inhibitors and Kinin Potentiators 4
6 Discovery of the Physiological and Pathological
Roles of Kinins 5
7 From Discovery to Clinical Application 7
8 Acknowledgements 7
9 References 7
2 The Pharmacology and Immunopharmacology of Kinin Receptors 9
Judith M Hall and Ian K M Morton
1 Introduction 9
2 Kinin Receptor Classification B; and B2
Receptors 10
2 1 B! Receptors 10
211 Selective Agonists at B i
Receptors 10
212 Selective Antagonists at B l
Receptors 12
213 Radioligand-binding Studies with Bj
Receptors 13
214 Molecular Biology Studies with Bj
Receptors 14
2 2 B2 Receptors 14
221 Selective Agonists at B2
Receptors 14
222 Selective Antagonists at 1 2
Receptors 14
223 Radioligand-binding Studies with B2
Receptors 17
224 Molecular Biology and Isolation of B2
Receptors 19
2 3 Bradykinin Receptor Subtypes 21
231 Tracheal B3 Receptors 21
232 Homologs of B2 Receptors 22
3 Immunopharmacology of Kinin Receptors 26
3 1 Acute Inflammatory Responses 26
311 Mast-cell Histamine Release 27
312 Blood Flow 27
313 Microvascular Permeability 27
314 Neurogenic Inflammation 28
3 2 Bt Receptor Induction and
Inflammation 29
3 3 Pain and Peripheral Inflammatory
Hyperalgesia 29
3 4 Airways Diseases 30
341 Lower Airways and Asthma 30
342 Upper Airways and Rhinitis 30
3 5 Pancreatitis 31
3 6 Endotoxin and Septic Shock 31
3 7 Inflammator v Joint Disease 31
3 8 Central Nervous System 31
4 Summary and Future Directions 32
5 Acknowledgement 32
6 References 32
vi CONTENTS
3 Molecular Pharmacology of Kinin Receptors 45
J Fred Hess
1 Introduction 45
2 Bj Receptors 46
2 1 Pharmacology of Bj Receptors 46
2 2 Molecular Cloning of the Human B!
Receptor 47
2 3 Molecular Pharmacology of B, Receptor
Species Homologs 47
231 Cloned Human B[ Receptors 48
232 Cloned Rabbit B, Receptors 49
233 Cloned Mouse B, Receptors 49
3 B2 Receptors 49
3 1 Molecular Cloning of the Rat li2
Receptor 50
3 2 Molecular Cloning of Human and Mouse B2
Receptors 50
3 3 B2 Receptor Gene Structure 50
3 4 B2 Receptor Subtypes 51
341 B, Receptors 51
342 Smooth Muscle and Neuronal B2
Receptor Subtypes 51
343 Species Differences in the Effects of B2
Receptor Antagonists 52
3 5 Targeted Disruption of the B2 Receptor 52
4 Summary 52
5 Acknowledgements 53
6 References 53
4 Gene Expression, Regulation and Cell Surface Presentation of the Kininogens 57
Alvin H Schmaier
1 Introduction 57 6 Physiological Activities of the Kininogens 63
2 Kininogen Gene Expression and Regulation 57 6 1 Thrombin Inhibition 64
3 Protein Chemistry and Structure of the 6 2 Participation of Kininogens in
Kininogens 58 Fibrinolysis 65
4 The Domain Structure of the Kininogens 59 7 Summary 66
5 Cell Surface Expression of Kininogen s 61 8 Acknowledgement 66
5 1 Mechanisms of Kininogen Cell-surface 9 References 66
Presentation 61
5 2 The Kininogen Binding Site on che
Endothelial Cell Surface 63
5 The Molecular Biology of the Kallikreins and their Roles in Inflammation
Judith A Clements
1 Introduction 72
2 The Plasma Kallikrein Gene 72
3 The Tissue Kallikrein Gene Family 73
3 1 General Overview 73
3 2 Locus, Genomic Organization, Size of
Families and Sequence Conservation 74
321 The Human Tissue Kallikrein (KLK)
Gene Family 74
322 The Monkey Tissue Kallikrein (cmKLK;
rmKLK) Gene Families 74
323 The Dog Tissue Kallikrein (dKLK)
Gene Family 75
324 The Mouse Tissue Kallikrein (mKlk)
Gene Family 75
325 The Rat Tissue Kallikrein (rKLK)
Gene Family 76
326 Other Tissue Kallikrein Gene
Families 77
3 3 Tissue- and Cell-specific Expression 77
331 KLKl/Tissut Kallikrein in the
Salivary Gland, Kidney and
Pancreas 77
332 KLKl/Tissue Kallikrein in Other
Tissues 78
333 Expression of Other KLK Genes 79
334 Transcriptional Regulation of Tissue-
specific KLK Expression 80
335 Rat KLK Transgenics 80
336 Human KLK Transgenics 81
3 4 Transcriptional and Post-transcriptional
Hormonal Regulation 82
341 Post-transcriptional Regulation of
KLK1 Expression and Tissue
Kallikrein Activity 82
342 Hormonal Regulation of KLK1 at
the Transcriptional Level 83
343 Post-transcriptional Regulation of
Expression and Enzyme Activity of
Other KLK Genes 84
344 Hormonal Regulation of Other
KLK Genes at the Transcriptional
Level 84
3 5 Predicted Substrate Specificity and
Function 85
CONTENTS vii
351 KLK1/Tissue Kallikrein: Function 4
via Kinin Generation 85
352 KLK1/Tissue Kallikrein: Function 5
via Other Substrates 86
353 Potential Function of Other KLK
Gene Products 86
The Complex Interactions of KLK Enzymes, Their
Inhibitors and Substrates in Inflammation 87
References 87
6, Immunological Probes for the Bradykinin B2 Receptor A Toolbox 99
Werner Muller-Esterl
1 Introduction 99
2 Immunological Tools for the B2 Receptor -
Methodology 100
2 1 Anti-idiotypic Antibodies 100
211 Preparation of Peptide Carrier
, Conjugates 101
2 1 2 Generation of Idiotypic
Antibodies 101
213 Production of Anti-idiotypic
Antibodies 102
214 Applications of Ami- idiotypic
Antibodies 102
2 2 Antiligand Antibodies 103
221 Ligand-carrier Conjugates 104
222 Production of Antiligand
Antibodies 104
223 Application of Antiligand
Antibodies 104
2 3 Antipeptide Antibodies 105
231 Production, Characterization and
Derivatization of Antipeptide
Antibodies 105
232 Application of Antipeptide
Antibodies 106
233 Immunocytochemistry 107
3 Perspectives 108
4 Acknowledgements 108
5 References 108
7 Metabolism of Bradykinin by Peptidases in Health and Disease 111
Ervin G Erdos and Randal A Skidgel
1 Introduction 112
2 Kininase II (Angiotensin I-converting
Enzyme) 112
2 1 Localization 113
2 2 Physical and Structural Properties 113
2 3 Enzymatic Properties 114
2 4 Soluble ACE 114
241 Release of Bound ACE 114
2 5 Cloning and Sequencing 115
2 6 Variations in ACE Activity in Disease 115
261 Acute Lung Injury 115
2 7 Hydrolysis of Kinins by ACE 115
271 Bradykinin 115
272 DesArg -Bradykinin 116
2 8 Inhibition of ACE and Potentiation of the
Effects of Endogenous Bradykinin 116
281 Effects Attributed to Inhibition of
Bradykinin Degradation 116
282 Effects Not Attributed to Inhibition
of Bradykinin Degradation 117
3 Neutral Endopeptidase 24 11 118
3 1 Localization 118
3 2 Enzymatic Properties 118
321 Soluble NEP 118
3 3 Inhibition of NEP and its Role as a
Kininase 119
4 Hydrolysis of Bradykinin by Carboxypeptidases 119
4 1 Metallocarboxypeptidases 119
411 General Characteristics 119
412 Carboxypeptidase N 120
413 Carboxypeptidase M 122
414 Carboxypeptidase U 124
4 2 Serine Carboxypeptidases 125
421 Physical and Structural
Properties 125
422 Enzymatic Properties 126
423 Localization 126
424 Role of Serine Carboxypeptidases as
Kininases 126
5 Hydrolysis of Bradykinin by Aminopeptidases 127
5 1 Aminopeptidase P 127
511 Physical and Structural
Properties 127
512 Enzymatic Properties 127
513 Localization 128
514 Role of Aminopeptidase P as a
Kininase 128
6 Hydrolysis of Bradykinin by Other
Endopeptidases 128
6 1 Meprin 129
6 2 Prolylendopeptidase 129
6 3 Endopeptidase 24 15 129
6 4 Endopeptidase 24 16 130
7 Conclusions 130
8 Acknowledgement 131
9 References 131
viii CONTENTS
8 Kinin BI Receptor Induction and Inflammation 143
Franfois Marceau
1 The Kinin Bt Receptor: An Inducible, G Protein-
coupled Receptor 143
2 Place of the Bj Receptor in Kinin Receptor
Classification 144
2 1 Criteria for Defining the Kinin Receptor
Subtypes 144
2 2 Problems and Controversies in the Definition
of the Bt Receptor 146
2 3 Relationship of the Bj Receptor with
Specific Forms of Kininogen and Kallikreins:
A Separate Tissue Kallikrein-Kinin
System? 147
3 Evidence for B, Receptor Upregulation in
Immunopathology 148
3 1 Evidence In Vivo 148
3 2 Evidence In Vitro 148
4 Mechanisms of Bj Receptor Induction 150
5 Summary and Conclusion 153
6 References 153
9 Kinins and Pain 157
A ndy Dray and Martin Perkins
1 Introduction 157
1 1 The Kinins 158
2 Kinins in the Periphery 158
2 1 Formation and Degradation of Kinins 158
2 2 Kinin Receptors 158
2 3 Kinin-induced Activation of
Nociceptors 159
231 Direct Activation of Afferent Fibers
via Stimulation of B2 Receptors 159
2 4 Desensitization to Bradykinin 161
2 5 Bradykinin-induced Sensitization of Sensory
Neurons 161
2 6 Bradykinin and Cytokine Production 162
2 7 Other Indirect Mechanisms of Bradykinin-
induced Sensitization _ 162
2 8 Bj Receptors and Hyperalgesia 163
3 Kinins in the Central Nervous System 163
3 1 Do Kinins Cause Hyperalgesia via Actions in
the CNS? 163
3 2 The Occurrence of Kinins and Kinin Binding
Sites in the CNS 164
3 3 The Functions of Kinins in the CNS 164
3 4 Kinins and CNS Inflammation 164
3 5 Kinins and Central Pain Mechanisms 165
4 Conclusions 166
5 References 167
10 The Kalltkrein-Kinin System in Sepsis Syndrome 173
Robin A Pixley and Robert W Colman
1 Sepsis Syndrome 173
1 1 The Kallikrein-Kinin System J 74
1 2 The Complement System 174
1 3 CI-Inhibitor 174
1 4 Experimental Detection of Contact
Activation 176
2 Clinical Studies of the Kallikrein-Kinin
System 177
2 1 Clinical Sepsis 177
2 2 Systemic Inflammatory Response
Syndrome 178
221 Admission values 178
222 Serial values 178
223 48 h values 179
224 Post-48 h values 179
3 Controlled Studies 180
3 1 Sepsis and the Kallikrein-Kinin System in
Baboons 180
311 Use of an Anti-Factor XII Antibody to
Establish the Role of the Kallikrein-
Kinin System in Sepsis 180
312 Effects on Complement Activation by
the Kallikrein-Kinin System 181
3 2 The Kallikrein-Kinin System in Human
Endotoxinemia 182
4 General Findings of the Kallikrein-Kinin System in
Sepsis 182
4 1 Activation Sequence in Baboon Sepsis 183
4 2 Concluding Remarks 183
5 References 184
CONTENTS ix
11 The Kinin System and Neutrophils 187
Yugen Naidoo and Kanti Bhoola
1 Historical Overview 187 3 Neutrophils and the Kallikrein-Kinin System
2 Production and Metabolism of Kinins 187 4 Mechanisms Involved in Inflammatory
2 1 Kallikreins 187 Disorders 192
211 Tissue Kallikrein 188 5 Clinical Indications 193
212 Plasma Kallikrein 189 6 References 194
2 2 Kininogens 189
2 3 Metabolism and Cellular Actions of
Kinins 190
12 Putative Roles of Bradykinin and the Kinin System in Pancreatitis 197
Thomas Griesbachi r and Fred Lembeck
1 Discovery of the Kallikrein-Kinin System in the
Pancreas 198
1 1 Kallikrein 198
1 2 Kinins 198
1 3 Kininogens 198
1 4 Kinin System of the Rat 198
1 5 Implications for Pancreas
Pathophysiology 199
2 Clinical Pancreatitis 199
2 1 Classification 199
2 2 Edematous and Necrotizing
Pancreatitis 199
3 Experimental Models of Acute Pancreatitis
in Vivo 199
3 1 Interstitial-Edematous Pancreatitis 200
3 2 Necrotizing-Hemorrhagic Pancreatitis 200
3 3 Models of Pancreatitis in Vitro 201
3 4 Clinical Relevance of Experimental
Models 201
4 Research in the Kallikrein-Kinin System in
Pancreatitis 201
4 1 Kinin and Kallikrein Levels 201
4 2 Bradykinin Receptor Antagonists 201
5 Clinical and Experimental Studies 202
5 1 Kinin, Kallikrein and Kininogen Levels in
Clinical Pancreatitis 202
511 Other Clinical Observations 202
5 2 Kinin, Kallikrein and Kininogen Levels in
Experimental Studies 203
521 Necrotizing-Hemorrhagic
Pancreatitis 203
522 Interstitial-Edematous
Pancreatitis 204
5 3 Studies with Bradykinin Antagonists 204
531 Interstitial-Edematous
Pancreatitis 204
532 Necrotizing-Hemorrhagic
Pancreatitis 205
5 4 Significance of Kinins During Acute
Pancreatitis 206
541 Vascular Functions 207
542 Pain 207
543 Drug-induced Pancreatitis 207
6 Possible Physiological Roles of Kinins in the
Pancreas 208
6 1 From Early Discoveries to Recent
Findings 208
6 2 Pancreatic Blood Flow and
Microcirculation 208
6 3 Pancreatic Secretion 209
6 4 From Physiological Function to Pathological
Events 209
7 Perspectives in the Treatment of Pancreatitis 209
8 References 211
13 The Role of the Kallikrein-Kinin System in Inflammation-induced Bone Metabolism 219
Ulf H Lerner
1 Introduction 219
2 Bone-cell Biology 220
2 1 Osteoblasts 220
2 2 Osteocytes 221
-2 3 Osteoclasts 221
2 4 Osteoblast-Osteoclast Interactions 222
3 Inflammation-induced Bone Loss 223
4 Kinins in Inflammation-induced Bone Lesions 224
5 Effects of Kinins on Bone Metabolism 224
6 Prostaglandins in Kinin-induced Bone
Resorption 226
7 Kinin Receptors in Bone 227
8 Kinin Signal Transduction in Bone 228
9 Interactions Between Kinins and Cytokines 230
10 Systemic Effects on Bone by Local
Inflammation 231
11 Acknowledgements 231
12 References 231
x CONTENTS
14 Bradykinin as an Inflammatory Mediator in the Urinary Tract 235
Carlo Alberto Maggi
1 Introduction 235
2 Bradykinin in the Urinary Tract and the Barrier
Function of the Urothelium 235
3 Kinin Receptors and Actions in the I rinarv
Tract 236
3 1 Kinins and Smooth Muscle Tone 236
311 Kinins and Local Regulation of
Pyeloureteral Motility 236
312 Kinins and Local Regulation of
Urinary Bladder Motility 237
3 2 Kinins and Microvascular Permeability 238
3 3 Kinins and Afferent Nerves 238
Evidence that Kinins are Inflammatory Mediators in
the Urinary Tract 241
Clinical Implications 243
References 245
15 The Kallikrein-Kinin System in Asthma
Stephen
1 Introduction 249
2 Airway Kinin Receptors 249
3 Bradykinin and Asthma 250
3 1 Airway Effects of Bradykinin ii i
Humans 250
3 2 Kinin Generation in Asthma 251
3 3 Bradykinin Receptor Antagonists in Animal
Models of Asthma 251
331 Sheep 251
332 Guinea Pigs 252
333 Rats 254
4 Bradykinin Antagonists in Humans 254
5 Bradykinin in Acute Respiratory Distress
Syndrome 254
and Acute Respiratory Distress Syndrome
G Farmer
Effects of Kinins Consistent with a Role in
ARDS 255
511 Effects of Bradykinin on Pulmonary
Blood Pressure 256
5 2 Kinin Generation in ARDS 256
5 3 Bradykinin Receptor Antagonists in Sepsis
and ARDS in Animals 257
5 4 Bradykinin Receptor Antagonists in Sepsis
and ARDS in Humans 257
6 Conclusions 257
7 References 258
16 Bradykinin Formation in Allergic Diseases and Hereditary Angioedema 265
Sesha R Reddigari, Michael Silverberg and Allen P Kaplan
1 Introduction 265
2 Protein Constituents of the Kallikrein-Kinin System
2 1 Factor XII 265
2 2 Prekallikrein 267 5
2 3 Prokallikrein and Tissue Kallikieins 267
2 4 Factor XI 268
2 5 High Molecular Weight Kinin gen 268
2 6 Low Molecular Weight Kininogen and
Kininogen Genes 270
3 Mechanisms of Bradykinin Formation 270
3 1 Contact Activation 270 6
311 Regulation of Contact
Activation 271
3 2 Tissue Pathway of Bradykinin
Formation 273
Bradykinin: Functions and Control
Mechanisms 273
Hereditary Angioedema and Acquired CI Inhibitor
Deficiency 275
5 1 Kinin Formation in Hereditary
Angioedema 277
5 2 Contact Activation in Allergic Diseases 277
521 Allergic Rhinitis 277
522 Asthma 278
References 279
17 The Nasal Airway Pharmacology of Bradykinin 287
James W Dear and John C Foreman
1 Introduction 287
1 1 Allergic Rhinitis 288
2 Methods For Studying Kinin Pharmacology in the
Nasal Airways 288
2 1 Active Posterior Rhinomanometry 288
2 2 Anterior Rhinomanometry 288
2 3 Acoustic Rhinometry 289
2 4 Nasal Lavage and Tissue Sampling 289
CONTENTS xi
3 Bradykinin as a Mediator of Allergic Rhinitis 289
3 1 Kinins are Synthesized During Nasal
Allergy 289
3 2 Kinins Mimic the Symptoms of Allergic
Rhinitis 290
3 3 Bradykinin Receptor Antagonists in Human
Nasal Airways 291
331 Normal Subjects 291
332 Perennial Allergic Rhinitis 292
333 Seasonal Allergic Rhinitis 293
4 Mechanisms of Action of Kinins in Human Nasal
Airways 293
4 1 The Role of Nitric Oxide 293
4 2 The Role of Histamine 295
4 3 The Role of Nerves 295
4 4 The Role of Prostaglandins 296
5 Radioligand-binding Studies of Human Nasal
Bradykinin Receptors 297
6 Conclusion 297
7 References 297
18 Bradykinin as a Growth Factor 301
David A Walsh and Tai-Ping D Fan
1 Introduction 301
2 Cell Proliferation in vitro 301
2 1 Stimulation of Cell Proliferation by
Bradykinin 302
2 2 Antimitogenic Effects of Kinins 302
2 3 Kinin Receptor Subtypes Mediating
Regulation of Cell Proliferation 304
2 4 Signal Transduction in Bradykinin-induced
Mitogenesis 305
2 5 Signal Transduction in Antimitogenic Actions
of Bradykinin 305
2 6 Synergy Between Bradykinin and Other
Growth Factors 305
2 7 Regulation of Growth Factor Release by
Bradykinin 306
3 Angiogenesis 306
4 Proliferative Synovitis 308
4 1 Kinin Systems in Chronically Inflamed
Synovium 308
4 2 Kinins and Synovial Proliferation 309
5 Neoplasia 309
6 Other Proliferative Conditions 310
7 Conclusions 310
8 References 311
19 The Role of Kinins in the Cardiac Effects of ACE Inhibitors and Myocardial Ischemia
Wolfgang Linz, Gabriele Wiemer, Klaus Wirth and Bernward A Scholkens
1 Introduction 315
2 Kinins Administered Locally Exert Beneficial
Cardiac Effects 316
3 Inhibition of Kinin Breakdown Induces Beneficial
Effects in Myocardial Ischemia 317
4 Antagonism of B2 Receptors Reverses
Cardioprotective Effects of Bradykinin or ACE
Inhibitors During Ischemia 318
5 Kinins are Released Under Conditions of
Ischemia 319
6 Kinin-generating Pathways are Present in the
Heart 320
7 Conclusion 321
8 References 321
Glossary 325
Key to Illustrations 335
Index 341
|
| adam_txt |
The Kinin
System
edited by
Stephen G Farmer
Bioscience, Zeneca Pharmaceuticals
1800 'oncord Pike, Wilmington
DE 19850, USA
ACADEMIC PRESS
San Diego London Boston
New York Sydney Tokyo Toronto
Contents
Contributors xiii
Series Preface xvii
Preface xix
1 Discovery of Bra iykimn and the Kallikrein-Kinin System 1
Wilson T Beraldo and Silvia P Andrade
1 Introduction 1
1 1 The Discovery of Bradykinin and its Release
by Snake Venom 1
2 The Discovery of Kallikrein and Kallidin 2
2 1 Kallikrein 2
2 2 Kallidin (Lys-Bradykinin) 2
3 Isolation and Purification of Bradykinin and
Kallidin 2
3 1 Isolation 2
3 2 Purification 3
4 The Bradykinin Precursor - Kininogen 4
5 Kinin Inactivators - Kininases 4
5 1 Kininase Inhibitors and Kinin Potentiators 4
6 Discovery of the Physiological and Pathological
Roles of Kinins 5
7 From Discovery to Clinical Application 7
8 Acknowledgements 7
9 References 7
2 The Pharmacology and Immunopharmacology of Kinin Receptors 9
Judith M Hall and Ian K M Morton
1 Introduction 9
2 Kinin Receptor Classification B; and B2
Receptors 10
2 1 B! Receptors 10
211 Selective Agonists at B i
Receptors 10
212 Selective Antagonists at B l
Receptors 12
213 Radioligand-binding Studies with Bj
Receptors 13
214 Molecular Biology Studies with Bj
Receptors 14
2 2 B2 Receptors 14
221 Selective Agonists at B2
Receptors 14
222 Selective Antagonists at 1'2
Receptors 14
223 Radioligand-binding Studies with B2
Receptors 17
224 Molecular Biology and Isolation of B2
Receptors 19
2 3 Bradykinin Receptor Subtypes 21
231 Tracheal B3 Receptors 21
232 Homologs of B2 Receptors 22
3 Immunopharmacology of Kinin Receptors 26
3 1 Acute Inflammatory Responses 26
311 Mast-cell Histamine Release 27
312 Blood Flow 27
313 Microvascular Permeability 27
314 Neurogenic Inflammation 28
3 2 Bt Receptor Induction and
Inflammation 29
3 3 Pain and Peripheral Inflammatory
Hyperalgesia 29
3 4 Airways Diseases 30
341 Lower Airways and Asthma 30
342 Upper Airways and Rhinitis 30
3 5 Pancreatitis 31
3 6 Endotoxin and Septic Shock 31
3 7 Inflammator v Joint Disease 31
3 8 Central Nervous System 31
4 Summary and Future Directions 32
5 Acknowledgement 32
6 References 32
vi CONTENTS
3 Molecular Pharmacology of Kinin Receptors 45
J Fred Hess
1 Introduction 45
2 Bj Receptors 46
2 1 Pharmacology of Bj Receptors 46
2 2 Molecular Cloning of the Human B!
Receptor 47
2 3 Molecular Pharmacology of B, Receptor
Species Homologs 47
231 Cloned Human B[ Receptors 48
232 Cloned Rabbit B, Receptors 49
233 Cloned Mouse B, Receptors 49
3 B2 Receptors 49
3 1 Molecular Cloning of the Rat li2
Receptor 50
3 2 Molecular Cloning of Human and Mouse B2
Receptors 50
3 3 B2 Receptor Gene Structure 50
3 4 B2 Receptor Subtypes 51
341 B, Receptors 51
342 Smooth Muscle and Neuronal B2
Receptor Subtypes 51
343 Species Differences in the Effects of B2
Receptor Antagonists 52
3 5 Targeted Disruption of the B2 Receptor 52
4 Summary 52
5 Acknowledgements 53
6 References 53
4 Gene Expression, Regulation and Cell Surface Presentation of the Kininogens 57
Alvin H Schmaier
1 Introduction 57 6 Physiological Activities of the Kininogens 63
2 Kininogen Gene Expression and Regulation 57 6 1 Thrombin Inhibition 64
3 Protein Chemistry and Structure of the 6 2 Participation of Kininogens in
Kininogens 58 Fibrinolysis 65
4 The Domain Structure of the Kininogens 59 7 Summary 66
5 Cell Surface Expression of Kininogen s 61 8 Acknowledgement 66
5 1 Mechanisms of Kininogen Cell-surface 9 References 66
Presentation 61
5 2 The Kininogen Binding Site on che
Endothelial Cell Surface 63
5 The Molecular Biology of the Kallikreins and their Roles in Inflammation
Judith A Clements
1 Introduction 72
2 The Plasma Kallikrein Gene 72
3 The Tissue Kallikrein Gene Family 73
3 1 General Overview 73
3 2 Locus, Genomic Organization, Size of
Families and Sequence Conservation 74
321 The Human Tissue Kallikrein (KLK)
Gene Family 74
322 The Monkey Tissue Kallikrein (cmKLK;
rmKLK) Gene Families 74
323 The Dog Tissue Kallikrein (dKLK)
Gene Family 75
324 The Mouse Tissue Kallikrein (mKlk)
Gene Family 75
325 The Rat Tissue Kallikrein (rKLK)
Gene Family 76
326 Other Tissue Kallikrein Gene
Families 77
3 3 Tissue- and Cell-specific Expression 77
331 KLKl/Tissut Kallikrein in the
Salivary Gland, Kidney and
Pancreas 77
332 KLKl/Tissue Kallikrein in Other
Tissues 78
333 Expression of Other KLK Genes 79
334 Transcriptional Regulation of Tissue-
specific KLK Expression 80
335 Rat KLK Transgenics 80
336 Human KLK Transgenics 81
3 4 Transcriptional and Post-transcriptional
Hormonal Regulation 82
341 Post-transcriptional Regulation of
KLK1 Expression and Tissue
Kallikrein Activity 82
342 Hormonal Regulation of KLK1 at
the Transcriptional Level 83
343 Post-transcriptional Regulation of
Expression and Enzyme Activity of
Other KLK Genes 84
344 Hormonal Regulation of Other
KLK Genes at the Transcriptional
Level 84
3 5 Predicted Substrate Specificity and
Function 85
CONTENTS vii
351 KLK1/Tissue Kallikrein: Function 4
via Kinin Generation 85
352 KLK1/Tissue Kallikrein: Function 5
via Other Substrates 86
353 Potential Function of Other KLK
Gene Products 86
The Complex Interactions of KLK Enzymes, Their
Inhibitors and Substrates in Inflammation 87
References 87
6, Immunological Probes for the Bradykinin B2 Receptor A Toolbox 99
Werner Muller-Esterl
1 Introduction 99
2 Immunological Tools for the B2 Receptor -
Methodology 100
2 1 Anti-idiotypic Antibodies 100
211 Preparation of Peptide Carrier
, Conjugates 101
2 1' 2 Generation of Idiotypic
Antibodies 101
213 Production of Anti-idiotypic
Antibodies 102
214 Applications of Ami- idiotypic
Antibodies 102
2 2 Antiligand Antibodies 103
221 Ligand-carrier Conjugates 104
222 Production of Antiligand
Antibodies 104
223 Application of Antiligand
Antibodies 104
2 3 Antipeptide Antibodies 105
231 Production, Characterization and
Derivatization of Antipeptide
Antibodies 105
232 Application of Antipeptide
Antibodies 106
233 Immunocytochemistry 107
3 Perspectives 108
4 Acknowledgements 108
5 References 108
7 Metabolism of Bradykinin by Peptidases in Health and Disease 111
Ervin G Erdos and Randal A Skidgel
1 Introduction 112
2 Kininase II (Angiotensin I-converting
Enzyme) 112
2 1 Localization 113
2 2 Physical and Structural Properties 113
2 3 Enzymatic Properties 114
2 4 Soluble ACE 114
241 Release of Bound ACE 114
2 5 Cloning and Sequencing 115
2 6 Variations in ACE Activity in Disease 115
261 Acute Lung Injury 115
2 7 Hydrolysis of Kinins by ACE 115
271 Bradykinin 115
272 DesArg'-Bradykinin 116
2 8 Inhibition of ACE and Potentiation of the
Effects of Endogenous Bradykinin 116
281 Effects Attributed to Inhibition of
Bradykinin Degradation 116
282 Effects Not Attributed to Inhibition
of Bradykinin Degradation 117
3 Neutral Endopeptidase 24 11 118
3 1 Localization 118
3 2 Enzymatic Properties 118
321 Soluble NEP 118
3 3 Inhibition of NEP and its Role as a
Kininase 119
4 Hydrolysis of Bradykinin by Carboxypeptidases 119
4 1 Metallocarboxypeptidases 119
411 General Characteristics 119
412 Carboxypeptidase N 120
413 Carboxypeptidase M 122
414 Carboxypeptidase U 124
4 2 Serine Carboxypeptidases 125
421 Physical and Structural
Properties 125
422 Enzymatic Properties 126
423 Localization 126
424 Role of Serine Carboxypeptidases as
Kininases 126
5 Hydrolysis of Bradykinin by Aminopeptidases 127
5 1 Aminopeptidase P 127
511 Physical and Structural
Properties 127
512 Enzymatic Properties 127
513 Localization 128
514 Role of Aminopeptidase P as a
Kininase 128
6 Hydrolysis of Bradykinin by Other
Endopeptidases 128
6 1 Meprin 129
6 2 Prolylendopeptidase 129
6 3 Endopeptidase 24 15 129
6 4 Endopeptidase 24 16 130
7 Conclusions 130
8 Acknowledgement 131
9 References 131
viii CONTENTS
8 Kinin BI Receptor Induction and Inflammation 143
Franfois Marceau
1 The Kinin Bt Receptor: An Inducible, G Protein-
coupled Receptor 143
2 Place of the Bj Receptor in Kinin Receptor
Classification 144
2 1 Criteria for Defining the Kinin Receptor
Subtypes 144
2 2 Problems and Controversies in the Definition
of the Bt Receptor 146
2 3 Relationship of the Bj Receptor with
Specific Forms of Kininogen and Kallikreins:
A Separate Tissue Kallikrein-Kinin
System? 147
3 Evidence for B, Receptor Upregulation in
Immunopathology 148
3 1 Evidence In Vivo 148
3 2 Evidence In Vitro 148
4 Mechanisms of Bj Receptor Induction 150
5 Summary and Conclusion 153
6 References 153
9 Kinins and Pain 157
A ndy Dray and Martin Perkins
1 Introduction 157
1 1 The Kinins 158
2 Kinins in the Periphery 158
2 1 Formation and Degradation of Kinins 158
2 2 Kinin Receptors 158
2 3 Kinin-induced Activation of
Nociceptors 159
231 Direct Activation of Afferent Fibers
via Stimulation of B2 Receptors 159
2 4 Desensitization to Bradykinin 161
2 5 Bradykinin-induced Sensitization of Sensory
Neurons 161
2 6 Bradykinin and Cytokine Production 162
2 7 Other Indirect Mechanisms of Bradykinin-
induced Sensitization _ 162
2 8 Bj Receptors and Hyperalgesia 163
3 Kinins in the Central Nervous System 163
3 1 Do Kinins Cause Hyperalgesia via Actions in
the CNS? 163
3 2 The Occurrence of Kinins and Kinin Binding
Sites in the CNS 164
3 3 The Functions of Kinins in the CNS 164
3 4 Kinins and CNS Inflammation 164
3 5 Kinins and Central Pain Mechanisms 165
4 Conclusions 166
5 References 167
10 The Kalltkrein-Kinin System in Sepsis Syndrome 173
Robin A Pixley and Robert W Colman
1 Sepsis Syndrome 173
1 1 The Kallikrein-Kinin System J 74
1 2 The Complement System 174
1 3 CI-Inhibitor 174
1 4 Experimental Detection of Contact
Activation 176
2 Clinical Studies of the Kallikrein-Kinin
System 177
2 1 Clinical Sepsis 177
2 2 Systemic Inflammatory Response
Syndrome 178
221 Admission values 178
222 Serial values 178
223 48 h values 179
224 Post-48 h values 179
3 Controlled Studies 180
3 1 Sepsis and the Kallikrein-Kinin System in
Baboons 180
311 Use of an Anti-Factor XII Antibody to
Establish the Role of the Kallikrein-
Kinin System in Sepsis 180
312 Effects on Complement Activation by
the Kallikrein-Kinin System 181
3 2 The Kallikrein-Kinin System in Human
Endotoxinemia 182
4 General Findings of the Kallikrein-Kinin System in
Sepsis 182
4 1 Activation Sequence in Baboon Sepsis 183
4 2 Concluding Remarks 183
5 References 184
CONTENTS ix
11 The Kinin System and Neutrophils 187
Yugen Naidoo and Kanti Bhoola
1 Historical Overview 187 3 Neutrophils and the Kallikrein-Kinin System
2 Production and Metabolism of Kinins 187 4 Mechanisms Involved in Inflammatory
2 1 Kallikreins 187 Disorders 192
211 Tissue Kallikrein 188 5 Clinical Indications 193
212 Plasma Kallikrein 189 6 References 194
2 2 Kininogens 189
2 3 Metabolism and Cellular Actions of
Kinins 190
12 Putative Roles of Bradykinin and the Kinin System in Pancreatitis 197
Thomas Griesbachi r and Fred Lembeck
1 Discovery of the Kallikrein-Kinin System in the
Pancreas 198
1 1 Kallikrein 198
1 2 Kinins 198
1 3 Kininogens 198
1 4 Kinin System of the Rat 198
1 5 Implications for Pancreas
Pathophysiology 199
2 Clinical Pancreatitis 199
2 1 Classification 199
2 2 Edematous and Necrotizing
Pancreatitis 199
3 Experimental Models of Acute Pancreatitis
in Vivo 199
3 1 Interstitial-Edematous Pancreatitis 200
3 2 Necrotizing-Hemorrhagic Pancreatitis 200
3 3 Models of Pancreatitis in Vitro 201
3 4 Clinical Relevance of Experimental
Models 201
4 Research in the Kallikrein-Kinin System in
Pancreatitis 201
4 1 Kinin and Kallikrein Levels 201
4 2 Bradykinin Receptor Antagonists 201
5 Clinical and Experimental Studies 202
5 1 Kinin, Kallikrein and Kininogen Levels in
Clinical Pancreatitis 202
511 Other Clinical Observations 202
5 2 Kinin, Kallikrein and Kininogen Levels in
Experimental Studies 203
521 Necrotizing-Hemorrhagic
Pancreatitis 203
522 Interstitial-Edematous
Pancreatitis 204
5 3 Studies with Bradykinin Antagonists 204
531 Interstitial-Edematous
Pancreatitis 204
532 Necrotizing-Hemorrhagic
Pancreatitis 205
5 4 Significance of Kinins During Acute
Pancreatitis 206
541 Vascular Functions 207
542 Pain 207
543 Drug-induced Pancreatitis 207
6 Possible Physiological Roles of Kinins in the
Pancreas 208
6 1 From Early Discoveries to Recent
Findings 208
6 2 Pancreatic Blood Flow and
Microcirculation 208
6 3 Pancreatic Secretion 209
6 4 From Physiological Function to Pathological
Events 209
7 Perspectives in the Treatment of Pancreatitis 209
8 References 211
13 The Role of the Kallikrein-Kinin System in Inflammation-induced Bone Metabolism 219
Ulf H Lerner
1 Introduction 219
2 Bone-cell Biology 220
2 1 Osteoblasts 220
2 2 Osteocytes 221
-2 3 Osteoclasts 221
2 4 Osteoblast-Osteoclast Interactions 222
3 Inflammation-induced Bone Loss 223
4 Kinins in Inflammation-induced Bone Lesions 224
5 Effects of Kinins on Bone Metabolism 224
6 Prostaglandins in Kinin-induced Bone
Resorption 226
7 Kinin Receptors in Bone 227
8 Kinin Signal Transduction in Bone 228
9 Interactions Between Kinins and Cytokines 230
10 Systemic Effects on Bone by Local
Inflammation 231
11 Acknowledgements 231
12 References 231
x CONTENTS
14 Bradykinin as an Inflammatory Mediator in the Urinary Tract 235
Carlo Alberto Maggi
1 Introduction 235
2 Bradykinin in the Urinary Tract and the Barrier
Function of the Urothelium 235
3 Kinin Receptors and Actions in the I 'rinarv
Tract 236
3 1 Kinins and Smooth Muscle Tone 236
311 Kinins and Local Regulation of
Pyeloureteral Motility 236
312 Kinins and Local Regulation of
Urinary Bladder Motility 237
3 2 Kinins and Microvascular Permeability 238
3 3 Kinins and Afferent Nerves 238
Evidence that Kinins are Inflammatory Mediators in
the Urinary Tract 241
Clinical Implications 243
References 245
15 The Kallikrein-Kinin System in Asthma
Stephen
1 Introduction 249
2 Airway Kinin Receptors 249
3 Bradykinin and Asthma 250
3 1 Airway Effects of Bradykinin ii i
Humans 250
3 2 Kinin Generation in Asthma 251
3 3 Bradykinin Receptor Antagonists in Animal
Models of Asthma 251
331 Sheep 251
332 Guinea Pigs 252
333 Rats 254
4 Bradykinin Antagonists in Humans 254
5 Bradykinin in Acute Respiratory Distress
Syndrome 254
and Acute Respiratory Distress Syndrome
G Farmer
Effects of Kinins Consistent with a Role in
ARDS 255
511 Effects of Bradykinin on Pulmonary
Blood Pressure 256
5 2 Kinin Generation in ARDS 256
5 3 Bradykinin Receptor Antagonists in Sepsis
and ARDS in Animals 257
5 4 Bradykinin Receptor Antagonists in Sepsis
and ARDS in Humans 257
6 Conclusions 257
7 References 258
16 Bradykinin Formation in Allergic Diseases and Hereditary Angioedema 265
Sesha R Reddigari, Michael Silverberg and Allen P Kaplan
1 Introduction 265
2 Protein Constituents of the Kallikrein-Kinin System
2 1 Factor XII 265
2 2 Prekallikrein 267 5
2 3 Prokallikrein and Tissue Kallikieins 267
2 4 Factor XI 268
2 5 High Molecular Weight Kinin gen 268
2 6 Low Molecular Weight Kininogen and
Kininogen Genes 270
3 Mechanisms of Bradykinin Formation 270
3 1 Contact Activation 270 6
311 Regulation of Contact
Activation 271
3 2 Tissue Pathway of Bradykinin
Formation 273
Bradykinin: Functions and Control
Mechanisms 273
Hereditary Angioedema and Acquired CI Inhibitor
Deficiency 275
5 1 Kinin Formation in Hereditary
Angioedema 277
5 2 Contact Activation in Allergic Diseases 277
521 Allergic Rhinitis 277
522 Asthma 278
References 279
17 The Nasal Airway Pharmacology of Bradykinin 287
James W Dear and John C Foreman
1 Introduction 287
1 1 Allergic Rhinitis 288
2 Methods For Studying Kinin Pharmacology in the
Nasal Airways 288
2 1 Active Posterior Rhinomanometry 288
2 2 Anterior Rhinomanometry 288
2 3 Acoustic Rhinometry 289
2 4 Nasal Lavage and Tissue Sampling 289
CONTENTS xi
3 Bradykinin as a Mediator of Allergic Rhinitis 289
3 1 Kinins are Synthesized During Nasal
Allergy 289
3 2 Kinins Mimic the Symptoms of Allergic
Rhinitis 290
3 3 Bradykinin Receptor Antagonists in Human
Nasal Airways 291
331 Normal Subjects 291
332 Perennial Allergic Rhinitis 292
333 Seasonal Allergic Rhinitis 293
4 Mechanisms of Action of Kinins in Human Nasal
Airways 293
4 1 The Role of Nitric Oxide 293
4 2 The Role of Histamine 295
4 3 The Role of Nerves 295
4 4 The Role of Prostaglandins 296
5 Radioligand-binding Studies of Human Nasal
Bradykinin Receptors 297
6 Conclusion 297
7 References 297
18 Bradykinin as a Growth Factor 301
David A Walsh and Tai-Ping D Fan
1 Introduction 301
2 Cell Proliferation in vitro 301
2 1 Stimulation of Cell Proliferation by
Bradykinin 302
2 2 Antimitogenic Effects of Kinins 302
2 3 Kinin Receptor Subtypes Mediating
Regulation of Cell Proliferation 304
2 4 Signal Transduction in Bradykinin-induced
Mitogenesis 305
2 5 Signal Transduction in Antimitogenic Actions
of Bradykinin 305
2 6 Synergy Between Bradykinin and Other
Growth Factors 305
2 7 Regulation of Growth Factor Release by
Bradykinin 306
3 Angiogenesis 306
4 Proliferative Synovitis 308
4 1 Kinin Systems in Chronically Inflamed
Synovium 308
4 2 Kinins and Synovial Proliferation 309
5 Neoplasia 309
6 Other Proliferative Conditions 310
7 Conclusions 310
8 References 311
19 The Role of Kinins in the Cardiac Effects of ACE Inhibitors and Myocardial Ischemia
Wolfgang Linz, Gabriele Wiemer, Klaus Wirth and Bernward A Scholkens
1 Introduction 315
2 Kinins Administered Locally Exert Beneficial
Cardiac Effects 316
3 Inhibition of Kinin Breakdown Induces Beneficial
Effects in Myocardial Ischemia 317
4 Antagonism of B2 Receptors Reverses
Cardioprotective Effects of Bradykinin or ACE
Inhibitors During Ischemia 318
5 Kinins are Released Under Conditions of
Ischemia 319
6 Kinin-generating Pathways are Present in the
Heart 320
7 Conclusion 321
8 References 321
Glossary 325
Key to Illustrations 335
Index 341 |
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| illustrated | Illustrated |
| index_date | 2024-07-02T18:39:51Z |
| indexdate | 2024-07-09T21:06:53Z |
| institution | BVB |
| isbn | 0122493400 |
| language | English |
| lccn | 97008628 |
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| series2 | The handbook of immunopharmacology |
| spelling | The kinin system ed. by Stephen G. Farmer San Diego [u.a.] Acad. Press 1997 XX, 349 S. Ill., graph. Darst. txt rdacontent n rdamedia nc rdacarrier The handbook of immunopharmacology Includes bibliographies and index Kinins Kinine (DE-588)4163888-8 gnd rswk-swf Kinine (DE-588)4163888-8 s DE-604 Farmer, Stephen G. Sonstige oth HEBIS Datenaustausch application/pdf http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=016026073&sequence=000001&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA Inhaltsverzeichnis |
| spellingShingle | The kinin system Kinins Kinine (DE-588)4163888-8 gnd |
| subject_GND | (DE-588)4163888-8 |
| title | The kinin system |
| title_auth | The kinin system |
| title_exact_search | The kinin system |
| title_exact_search_txtP | The kinin system |
| title_full | The kinin system ed. by Stephen G. Farmer |
| title_fullStr | The kinin system ed. by Stephen G. Farmer |
| title_full_unstemmed | The kinin system ed. by Stephen G. Farmer |
| title_short | The kinin system |
| title_sort | the kinin system |
| topic | Kinins Kinine (DE-588)4163888-8 gnd |
| topic_facet | Kinins Kinine |
| url | http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=016026073&sequence=000001&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA |
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