ISBN: 3540676252
TITLE: Biochemical Sites of Insecticide Action and Resistance
AUTHOR: Ishaaya, Isaac (Ed.)
TOC:

Biochemical Processes Related to Insecticide Action: an Overview
I. ISHAAYA
1 Introduction 1
2 Chitin Synthesis Inhibition 2
3 Ecdysone and Juvenile Hormone Receptors 4
4 Acetylcholine Receptors 5
5 GABA and Glutamate Receptors and Ion Channels 6
6 Other Biochemical Sites 8
7 Conclusions 9
References 10
GABA and Glutamate Receptors as Biochemical Sites for Insecticide Action
J.R. BLOOMQUIST
1 Introduction 17
2 GABA Receptors in Mammals and Insects 18
2.1 Classification of GABA Receptors 18
2.2 Structure and Physiological Role of Insect GABA Receptors 18
2.3 Pharmacology of GABA Receptors 19
3 Summary of Effects of Convulsants and Avermectins on the GABA Receptor 19
3.1 Polychlorocycloalkanes and Related Norbornanes 21
3.2 Picrodendrin and Silphinene Natural Products 22
3.3 Fipronil and Fipronil Analogs 25
3.4 Trioxabicyclooctanes and Related Compounds 27
3.5 New Avermectins and the Mammalian GABA Receptor 28
3.6 Altered GABA Receptors in Resistance 30
3.7 Resistance to New and Experimental Insecticides 31
4 Glutamate-Gated Chloride Channels 33
4.1 Physiology, Pharmacology, and Molecular Structure 33
4.2 Effects of the Avermectins 34
4.3 New Avermectins and Their Uses 35
4.4 Target Site Resistance to the Avermectins 36
5 Conclusions 36
References 37
Insecticides Affecting Voltage-Gated Ion Channels
E. ZLOTKIN
1 Insecticides and Ion Channels 43
1.1 Scope and Aim 43
1.2 Voltage-Gated Ion Channels 44
2 Industrial Insecticides Targeting Ion Channels 48
2.1 Insecticides of the Voltage-Gated Sodium Channels 48
2.2 Insecticides of the Potassium and Calcium Channels 52
3 The Functional Diversity of Insecticides 54
3.1 Multiplicity of Effects 54
3.2 Distinction Between Mammals and Insects 56
4 Neurotoxic Polypeptides 57
4.1 Animal Group Specificity 57
4.2 Insect-Selective Neurotoxins Affecting the Voltage-Gated Sodium Channels 58
4.2.1 Scorpion Venom Toxins 58
4.2.2 Spider Venom Toxins 61
4.3 Insect-Selective Neurotoxins Affecting the Voltage-Gated Calcium Channel 61
5 Recombinant Baculovirus Bioinsecticides 62
6 Allosteric Coupling and Allosteric Antagonism 64
References 69
Acetylcholine Receptors as Sites for Developing Neonicotinoid Insecticides
R NAUEN, U. EBBINGHAUS-KINTSCHER, A. ELBERT, P. JESCHKE, and K. TIETJEN
1 Introduction 77
2 Insect Nicotinic Acetylcholine Receptors 80
2.1 Structure 80
2.2 Diversity 80
3 Compounds Acting on the Nicotinic Acetylcholine Receptor 83
3.1 R adioligand Binding Studies 83
3.2 Neonicotinoids 86
3.2.1 Imidacloprid and Related Structures 86
3.2.2 Mannich Adducts as Experimental Pro-Neonicotinoids 91
4 Electrophysiological Considerations 92
4.1 Whole Cell Voltage Clamp of Native Neuron Preparations 94
4.1.1 Correlation Between Electrophysiology and Radioligand Binding Studies 96
4.2 Agonists vs. Antagonists 98
4.3 Receptor Subtypes in Locusta migratoria 99
References 101
Ecdysteroid and Juvenile Hormone Receptors: Properties and Importance in Developing Novel Insecticides
S.R. PALLI and A. RETNAKARAN
1 Introduction 107
2 Ecdysteroids 107
2.1 Biology, Endocrinology and Molecular Biology 108
2.2 Receptors and Other Target Sites 112
2.3 Non-Steroidal Ecdysone Analogs and Their Mode of Action 115
2.4 Receptor-Based Screening Assays 119
2.5 Future Directions 120
3 Juvenile Hormone 121
3.1 Biology, Endocrinology and Molecular Biology 121
3.2 Receptors and Other Target Sites 122
3.3 JH Analogs and Their Modes of Action 125
3.4 Receptor-Based Screening Assays 126
3.5 Future Directions 126
References 127
Imaginal Discs and Tissue Cultures as Targets for Insecticide Action
H. OBERLANDER and G. SMAGGHE
1 Introduction 133
2 Imaginal Discs as Targets of Insect Hormones in Vivo and in Vitro 133
3 Insecticide Action in Vitro: Juvenile Hormone Mimics 136
4 Insecticide Action in Vitro: Chitin Synthesis Inhibitors 137
4.1 Organ Cultures 137
4.2 Cell Lines 139
5 Insecticide Action in Vitro: Ecdysteroid Agonists 139
5.1 Organ Cultures 139
5.2 Cell Lines 140
References 145
Insect Neuropeptide Antagonists: a Novel Approach for Insect Control
M. ALTSTEIN and C. GILON
1 Introduction 151
2 Backbone Cyclic Neuropeptide-Based Antagonist (BBC-NBA)
Approach 153
2.1 Determination of the Active Sequence in the Neuropeptide 153
2.2 Development of a Competitive Lead Antagonist 154
2.3 Improvement of the Antagonistic Activity by Conformational Constraint 155
2.4 Backbone Cyclization: a Tool for Imposing Conformational
Constraint on Peptides 156
2.5 Cycloscan: Conformationally Constrained BBC Peptide Libraries 156
3 Pheromone Biosynthesis Activating Neuropeptide 158
4 Implementation of the BBC-NBA Strategy to the Pyrokinin/PBAN Family 159
5 Conversion of Neuropeptide Antagonists into Insecticide Prototypes 160
6 Concluding Remarks 161
References 163
Ion Balance in the Lepidopteran Midgut and Insecticidal Action of Bacillus thuringiensis
J.L. GRINGORTEN
1 Introduction 167
2 Pathogenesis 168
3 Dependence of Host and Pathogen on Midgut pH 169
4 Midgut K^+ and H^+ Regulation 170
4.1 The K^+ Pump 170
4.2 The 2K^+/1ATP Model for Midgut Alkalization 171
4.3 The 1K^+/1ATP Model for Midgut Alkalization 173
4.4 Transmembrane and Transepithelial Ion Gradients 175
5 Disruption of Midgut Ion Homeostasis by Bacillus thuringiensis 176
5.1 In Vivo Changes 176
5.2 In Vitro Changes 179
5.3 What is the Source of the Elevated Hemolymph K^+? 181
5.4 Larval Paralysis and Mortality Factors 182
5.5 delta-Endotoxin Effects on K^+-Dependent Uptake of Amino Acids 182
5.6 Correlating delta-Endotoxin Effects on the Isolated Midgut with Insecticidal Activity 185
6 Receptor Binding and Ion-Channel Formation 186
6.1 Receptor Binding 186
6.2 Ion-Channel Formation in Artificial Membranes and BBMVs 188
6.3 Insect Cell Lines as Proxies for Midgut Cells In Vivo 190
7 Membrane Insertion and Pore Formation 192
8 Conclusions and Thoughts 196
References 197
Evolution of Amplified Esterase Genes as a Mode of Insecticide Resistance In Aphids
L.M. FIELD, R.L. BLACKMAN, and A.L. DEVONSHIRE
1 Introduction 209
2 Biochemistry of Esterase-Based Resistance in M. persicae 210
3 Molecular Genetics of Esterase Overproduction 210
3.1 Esterase Genes in Susceptible Aphids 211
3.2 Organization of Amplified Esterase Genes 212
3.3 Cytogenetic Studies of Amplified Esterases 213
4 Expression of Esterase Genes 215
5 Wider Implications 216
References 217
Insensitive Acetylcholinesterase as Sites for Resistance to Organophosphates and Carbamates in Insects: Insensitive Acetylcholinesterase Confers Resistance in Lepidoptera
R.V. GUNNING and G.D. MOORES
1 Introduction 221
2 Acetylcholinesterase as a Resistance Mechanism 222
3 Insensitive AChE in Lepidopteran Species 224
4 Insensitive AChE in H. punctigera 225
5 Forms of AChE in Lepidoptera 226
6 Effects of Altered AChE on Acetylcholine Hydrolysis 229
7 Inhibition Ratios and Toxicity in Lepidoptera 230
8 Cross Resistance Between Organophosphates and Carbamates in Lepidoptera 231
9 Genetics of Resistance in Lepidoptera 231
10 Fitness of Resistance in Lepidoptera 232
11 Evolution 233
12 Control of Altered AChE in Lepidoptera 233
13 Population Genetics and Monitoring 234
14 Conclusions 235
References 236
Glutathione S-Transferases and Insect Resistance to Insecticides
C.-N. SUN, H.-Y. HUANG, N.-T. HU, and W.-Y. CHUNG
1 Introduction 239
2 General Features of Glutathione S-Transferases (GSTs) 239
2.1 Roles 239
2.2 Biochemical and Physiological Characteristics 240
2.3 Structure, Regulation, and Evolution of GST Genes 241
3 Insect GSTs 242
3.1 Roles 242
3.2 Biochemical and Physiological Characteristics 243
3.3 GSTs and Insecticide Resistance 244
3.4 Molecular Biology Studies 245
4 GST Studies of Several Insects 246
4.1 Drosophila melanogaster 246
4.2 Musca domestica 246
4.3 Anopheles gambiae 247
4.4 Plutella xylostella 248
5 Concluding Remarks 251
References 252
Cytochrome P450 Monooxygenases and Insecticide Resistance: Lessons from CYP6D1
J.G. SCOTT
1 Cytochrome P450 Monooxygenases 255
2 Insecticide Resistance 256
3 Monooxygenase-Mediated Insecticide Resistance 256
4 CYP6D1 and Insecticide Resistance 257
5 Summary of the Lessons Learned from CYP6D1 261
References 263
Mechanisms of Organophosphate Resistance in Insects
B.D. SIEGFRIED and M.E. SCHARF
1 Introduction 269
2 Physiological Mechanisms of Resistance 270
2.1 Resistance Mechanisms Involving Enhanced Biotransformation 272
2.1.1 Cytochrome-P450-Dependent Monooxygenases 272
2.1.2 Glutathione S-Transferases 274
2.1.3 Hydrolytic Enzymes 276
2.1.3.1 Quantitative Changes (Gene Amplification) 277
2.1.3.2 Qualitative Changes 281
2.2 Target Site Insensitivity 283
2.3 Interactions Between Resistance Mechanisms 284
3 Summary 286
References 287
Insect Midgut as a Site for Insecticide Detoxification and Resistance
G. SMAGGHE and L. TIRRY
1 Introduction 293
2 The Insect Gut: a Natural Digestive-Absorption Architecture 294
3 Enzymatic Metabolism of Pesticide Involved in Resistance 298
4 Impact of Ingestion, and Penetration and Disposition in the Insect Body on Resistance to Pesticides 304
5 Attempts for Chemical Modeling of Digestion and Absorption in Insect Midgut 310
6 In Vitro Gut Cultures for Insecticidal Activity Studies 314
References 316
Impact of Insecticide Resistance Mechanisms on Management Strategies
A.R. HOROWITZ and I. DENHOLM
1 Introduction 323
2 Overview of Resistance Mechanisms 324
3 Overview of Resistance Management Tactics 325
4 Diagnosing Resistance 327
4.1 In Vitro Assays for Diagnosing Resistance 328
5 Overpowering Resistance Mechanisms 331
6 Resolving and Exploiting Cross-Resistance 332
7 Conclusions 334
References 335
Subject Index 339
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