Neuropeptide Systems as Targets for Parasite and Pest Control

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Oktober 2010



The need to continually discover new agents for the control or treatment of invertebrate pests and pathogens is undeniable. Agriculture, both animal and plant, succeeds only to the extent that arthropod and helminth consumers, vectors and pathogens can be kept at bay. Humans and their companion animals are also plagued by invertebrate parasites. The deployment of chemical agents for these purposes inevitably elicits the selection of resistant populations of the targets of control, necessitating a regular introduction of new kinds of molecules. Experience in other areas of chemotherapy has shown that a thorough understanding of the biology of disease is an essential platform upon which to build a discovery program. Unfortunately, investment of research resources into understanding the basic physiology of invertebrates as a strategy to illuminate new molecular targets for pesticide and parasiticide discovery has been scarce, and the pace of introduction of new molecules for these indications has been slowed as a result. An exciting and so far unexploited area to explore in this regard is invertebrate neuropeptide physiology. This book was assembled to focus attention on this promising field by compiling a comprehensive review of recent research on neuropeptides in arthropods and helminths, with contributions from many of the leading laboratories working on these systems.


1. Receptor?Based Discovery Strategies for Insecticides and Parasiticides: A Review
Debra Woods, Cheryl Butler, Tracey Williams and Karen Greenwood
Mechanistic Receptor?Based Screens
Selection of Compounds for Screening'Hit?to?Lead': Converting a Mechanistic Screen Active into a Lead Molecule
Lead?to?Candidate: Identification of Molecules for Progressionto Market
Conclusion and Discussion
2. Nonpeptide Ligands for Peptidergic G Protein?Coupled Receptors
Timothy G. Geary
Druggable Targets in Neuropeptidergic Signaling
Neuropeptide?Targeted Drugs: Basic Features
Historical Perspectives
Screening for Novel Nonpeptide Ligands
Discovery of Novel Nonpeptide Ligands through Screening
Current Status
Applications in Invertebrate Systems: General Considerations
3. Interaction of Mimetic Analogs of Insect Kinin Neuropeptides with Arthropod Receptors
Ronald J. Nachman and Patricia V. Pietrantonio
Functional Analysis of Arthropod Receptors Selective for Insect Kinins
Chemical, Conformational and Stereochemical Aspects of Receptor Interaction
Interaction of Biostable Insect Kinin Analogs with Receptors and Activity in In Vitro and In Vivo Bioassays
C?Terminal Aldehyde Analogs of Insect Kinins
Nonpeptide Mimetic Agonists/Antagonists of Expressed Insect Kinin Receptors
Prospects for Enhanced Topical and/or Oral Bioavailability
4. Neuropeptides in Helminths: Ocurrence and Distribution
Nikki J. Marks and Aaron G. Maule
Nematode Neuropeptides
Platyhelminth Neuropeptides
Targets for Parasite Control
Note Added in Proof
5. Neuropeptide Physiology in Helminths
Angela Mousley, Ekaterina Novozhilova, Michael J. Kimber and Tim A. Day
Neuropeptide Function in Nematodes
Neuropeptide Function in Platyhelminths
6. Neuropeptide Gene Fa milies in Caenorhabditis elegans
Chris Li and KyuhyungKim
Identification of Neuropeptide Genes in C. elegans
Expression of Neuropeptide Genes
Cleavage and Processing of Neuropeptides
Biochemical Isolation of Neuropeptides
Neuropeptide Function
Behaviors Affected by Multiple Classes of Neuropeptides
Neuropeptide Receptors
Pharmacology of FLP Neuropeptides
7. Control of Nematode Parasites with Agents Acting on Neuro?Musculature Systems: Lessons for Neuropeptide Ligand Discovery
Richard J. Martin and Alan P. Robertson
The Existing Anti?Nematodal Drugs with Effects on Neuromuscular Systems
Resistance Is Predicted
Broad Spectrum or Narrow Spectrum
Potential Problems Associated with Neuropeptide Receptors as Target Sites for Anthelmintics
High?Throughput Screens for Neuropeptide Ligands
Toxicity and Safety
8. Neuropeptide signaling in insects
Miriam Altstein and Dick R. Nässel
Neuropeptides: Their biosynthesis, processing and expression
Neuropeptides families, GPCRs and peptide functions
Insect neuropeptides as potential targets for pest management
9. Neuropeptide Physiology in Insects
William G. Bendena
Neuropeptide Biosynthesis and Action
Potential Physiological Targets for Pest Control
Future Developments
10. Neuropeptide Biology in Drosophila
Elke Clynen, Ank Reumer, Geert Baggerman, Inge Mertens and Liliane Schoofs
Introduction: Drosophila as a Model to Study Neuropeptide Signaling
Deorphanization of Drosophila Neuropeptide GPCRs
Functional Role of Neuropeptides: Localization, Reverse Genetics and Bioassays
Other Neuronal Molecules as Potential Targets for Insecticides
11. Neuropeptide Receptors as Possible Targets for Development of Insect Pest Control Agents
Matthias B. Van Hiel, Tom Van Loy, Jeroen Poels, Hans Peter Vandersmissen,Heleen Verlinden, Liesbeth Badisco and Jozef Vanden Broeck
Receptors Controlling Insect


TIMOTHY G. GEARY is a Tier I Canada Research Chair and is Professor and Director of the Institute of Parasitology at McGill University in Montréal, Québec, Canada. Geary received a BSc degree from the University of Notre Dame in South Bend, IN (USA) and a PhD in Pharmacology from the University of Michigan in Ann Arbor, MI (USA, 1980). He worked on malaria chemotherapy at Michigan State University in East Lansing, MI (USA) until 1985, when he joined The Upjohn Company in Kalamazoo, MI (USA) as a staff scientist working on discovery of antiparasitic drugs. Geary joined the Faculty at McGill in 2005; research interests include proteomics and genomics analyses of the host-parasite interface, discovery of anthelmintics and the pharmacology of antiparasitic drugs. AARON G. MAULE is a Director of Research for Molecular Biosciences and Professor of Molecular Parasitology at Queen's University Belfast, Northern Ireland. Maule was awarded a BSc(Hons) in Biology (1986) and a PhD in Experimental Parasitology (1989) at Queen's where he began working on parasite neuromuscular systems. He focused on molecular aspects of parasite neurobiology during postdoctoral positions at Queen's and at The Upjohn Company in Kalamazoo, MI (USA). Maule returned to Queen's as a member of academic staff in 1995 to pursue the basic biology of helminth signaling systems. Research interests include parasite neurobiology and the development and exploitation of gene silencing platforms for target validation and parasite control.
EAN: 9781441969019
ISBN: 1441969012
Untertitel: 'Advances in Experimental Medicine and Biology'. 28 schwarz-weiße Abbildungen, 21 schwarz-weiße Tabellen. Sprache: Englisch.
Verlag: Springer-Verlag GmbH
Erscheinungsdatum: Oktober 2010
Seitenanzahl: XVIII
Format: gebunden
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