Insect acetylcholinesterase as a target for effective and environmentally safe insecticides

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8 Citations (Scopus)

Abstract

Insecticides are a cost-effective approach to managing disease-carrying, crop-destroying, and residential pest insects. However, current anticholinesterase insecticides are toxic to beneficial insects and vertebrates because they target the catalytic serine residue of acetylcholinesterase, a hydrolase vital to the regulation of acetylcholine in both invertebrates and vertebrates. Targeting this serine residue for more than 70 years has also contributed to current problems with insecticide resistance. This chapter presents data undergirding a mechanistically new insecticide concept that targets a cysteine residue unique in pest insect acetylcholinesterase to impart species-selective toxicity and a low propensity for resistance. These data are used to discuss how gainful deployment of the mechanism of irreversible inhibition of the acetylcholinesterase responsible for cholinergic functions in pest insects-but not in social bees and other higher social hymenopterans-may lead to cysteine-targeting anticholinesterases that are effective and environmentally safe in controlling pest insects while sparing economically important beneficial insects.

Original languageEnglish (US)
Pages (from-to)435-494
Number of pages60
JournalAdvances in Insect Physiology
Volume46
DOIs
StatePublished - 2014

Fingerprint

acetylcholinesterase
insect pests
insecticides
beneficial insects
insects
serine
cysteine
vertebrates
insecticide resistance
cholinergic agents
acetylcholine
hydrolases
Apoidea
Hymenoptera
invertebrates
toxicity
crops

Keywords

  • Acetylcholinesterase
  • Anticholinesterases
  • Cysteine-targeting insecticides
  • Insecticide resistance
  • Irreversible inhibitors
  • Neuroactive insecticides
  • Selective toxicity

ASJC Scopus subject areas

  • Insect Science

Cite this

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title = "Insect acetylcholinesterase as a target for effective and environmentally safe insecticides",
abstract = "Insecticides are a cost-effective approach to managing disease-carrying, crop-destroying, and residential pest insects. However, current anticholinesterase insecticides are toxic to beneficial insects and vertebrates because they target the catalytic serine residue of acetylcholinesterase, a hydrolase vital to the regulation of acetylcholine in both invertebrates and vertebrates. Targeting this serine residue for more than 70 years has also contributed to current problems with insecticide resistance. This chapter presents data undergirding a mechanistically new insecticide concept that targets a cysteine residue unique in pest insect acetylcholinesterase to impart species-selective toxicity and a low propensity for resistance. These data are used to discuss how gainful deployment of the mechanism of irreversible inhibition of the acetylcholinesterase responsible for cholinergic functions in pest insects-but not in social bees and other higher social hymenopterans-may lead to cysteine-targeting anticholinesterases that are effective and environmentally safe in controlling pest insects while sparing economically important beneficial insects.",
keywords = "Acetylcholinesterase, Anticholinesterases, Cysteine-targeting insecticides, Insecticide resistance, Irreversible inhibitors, Neuroactive insecticides, Selective toxicity",
author = "Yuan-Ping Pang",
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AU - Pang, Yuan-Ping

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N2 - Insecticides are a cost-effective approach to managing disease-carrying, crop-destroying, and residential pest insects. However, current anticholinesterase insecticides are toxic to beneficial insects and vertebrates because they target the catalytic serine residue of acetylcholinesterase, a hydrolase vital to the regulation of acetylcholine in both invertebrates and vertebrates. Targeting this serine residue for more than 70 years has also contributed to current problems with insecticide resistance. This chapter presents data undergirding a mechanistically new insecticide concept that targets a cysteine residue unique in pest insect acetylcholinesterase to impart species-selective toxicity and a low propensity for resistance. These data are used to discuss how gainful deployment of the mechanism of irreversible inhibition of the acetylcholinesterase responsible for cholinergic functions in pest insects-but not in social bees and other higher social hymenopterans-may lead to cysteine-targeting anticholinesterases that are effective and environmentally safe in controlling pest insects while sparing economically important beneficial insects.

AB - Insecticides are a cost-effective approach to managing disease-carrying, crop-destroying, and residential pest insects. However, current anticholinesterase insecticides are toxic to beneficial insects and vertebrates because they target the catalytic serine residue of acetylcholinesterase, a hydrolase vital to the regulation of acetylcholine in both invertebrates and vertebrates. Targeting this serine residue for more than 70 years has also contributed to current problems with insecticide resistance. This chapter presents data undergirding a mechanistically new insecticide concept that targets a cysteine residue unique in pest insect acetylcholinesterase to impart species-selective toxicity and a low propensity for resistance. These data are used to discuss how gainful deployment of the mechanism of irreversible inhibition of the acetylcholinesterase responsible for cholinergic functions in pest insects-but not in social bees and other higher social hymenopterans-may lead to cysteine-targeting anticholinesterases that are effective and environmentally safe in controlling pest insects while sparing economically important beneficial insects.

KW - Acetylcholinesterase

KW - Anticholinesterases

KW - Cysteine-targeting insecticides

KW - Insecticide resistance

KW - Irreversible inhibitors

KW - Neuroactive insecticides

KW - Selective toxicity

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