ArticleScientific reports2013
Novel selective and irreversible mosquito acetylcholinesterase inhibitors for controlling malaria and other mosquito-borne diseases.
Article in Scientific reports, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed, 39 citations in OpenAlex.
- Mild and efficient synthesis of carbamates using dioxazolones as bench-stable isocyanate surrogates: application in AChE-inhibiting agent development.RSC advances · 2026Article
- Potent and selective indole-based inhibitors targeting disease-transmitting mosquitoes.RSC medicinal chemistry · 2026Article
- Enzyme Dynamics Determine the Potency and Selectivity of Inhibitors Targeting Disease-Transmitting Mosquitoes.ACS infectious diseases · 2024Article
- Combination of computational techniques and RNAi reveal targets in Anopheles gambiae for malaria vector control.PloS one · 2024Article
- Structure-Activity Relationships Reveal Beneficial Selectivity Profiles of Inhibitors Targeting Acetylcholinesterase of Disease-Transmitting Mosquitoes.Journal of medicinal chemistry · 2023Article
- Article
- Acetylcholinesterase target sites for developing environmentally friendly insecticides against Tetranychus urticae (Acari: Tetranychidae).Experimental & applied acarology · 2021Article
- Transgenic Expression of dsRNA Targeting thePlants (Basel, Switzerland) · 2021Article
- RNAi technology for management of banana bunchy top disease.Food and energy security · 2020Review
- Anopheles metabolic proteins in malaria transmission, prevention and control: a review.Parasites & vectors · 2020Review
- Reply to Comment on "Cysteine-Targeted Insecticides againstACS medicinal chemistry letters · 2020Article
- Comment on "Cysteine-Targeted Insecticides againstACS medicinal chemistry letters · 2020Article
- Cysteine-Targeted Insecticides againstACS medicinal chemistry letters · 2020Article
- Select β- and γ-branched 1-alkylpyrazol-4-yl methylcarbamates exhibit high selectivity for inhibition ofPesticide biochemistry and physiology · 2018Article
- Structure of the G119S Mutant Acetylcholinesterase of the Malaria Vector Anopheles gambiae Reveals Basis of Insecticide Resistance.Structure (London, England : 1993) · 2018Article
- Rapid Mechanistic Evaluation and Parameter Estimation of Putative Inhibitors in a Single-Step Progress-Curve Analysis: The Case of Horse Butyrylcholinesterase.Molecules (Basel, Switzerland) · 2017Article
- Discovery of Species-selective and Resistance-breaking Anticholinesterase Insecticides for the Malaria Mosquito.Current medicinal chemistry · 2017Review
- Isatin Derived Spirocyclic Analogues with α-Methylene-γ-butyrolactone as Anticancer Agents: A Structure-Activity Relationship Study.Journal of medicinal chemistry · 2016Article
- Analysis of esterase enzyme activity in adults of the major malaria vector Anopheles funestus.Parasites & vectors · 2016Article
- Article
Corrections and comments
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Authors and funding
6 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
We reported previously that insect acetylcholinesterases (AChEs) could be selectively and irreversibly inhibited by methanethiosulfonates presumably through conjugation to an insect-specific cysteine in these enzymes. However, no direct proof for the conjugation has been published to date, and doubts remain about whether such cysteine-targeting inhibitors have desirable kinetic properties for insecticide use. Here we report mass spectrometric proof of the conjugation and new chemicals that irreversibly inhibited African malaria mosquito AChE with bimolecular inhibition rate constants (k(inact)/K(I)) of 3,604-458,597 M(-1)sec(-1) but spared human AChE. In comparison, the insecticide paraoxon irreversibly inhibited mosquito and human AChEs with k(inact)/K(I) values of 1,915 and 1,507 M(-1)sec(-1), respectively, under the same assay conditions. These results further support our hypothesis that the insect-specific AChE cysteine is a unique and unexplored target to develop new insecticides with reduced insecticide resistance and low toxicity to mammals, fish, and birds for the control of mosquito-borne diseases.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.