Circumventing Resistance to Channel-Targeting Insecticides: A Challenge for Global Health and Food Security

Dear Colleagues,

Only a very small fraction of insects in the world are pests or harmful to humans and livestock. However, those that serve as damaging pests or vectors can inflict tremendous damage. For example, they can contaminate food, destroy cultivated crops, and transmit parasites and viruses. Each year, more than 700,000 human deaths result from vector-borne diseases worldwide. Among several approaches to insect control, chemical control predominates in the control of pests or vector-borne diseases and modification of their essential behaviors. The compounds deployed include natural products, synthesized mimics of natural products, and completely synthetic compounds. Many are neurotoxic and specifically affect the voltage-gated ion channels involved in axonal action potential propagation, either through blocking, hyperactivating, and/or deregulating their intrinsic functional properties. Ion channels (voltage-gated and ligand-gated) remain the primary target of most insecticide molecules widely used commercially for insect control.

Resistance to insecticides is of growing importance and threatens progress being made in disease and pest control. Among different mechanisms of resistance, target-site resistance, in which an ion channel target site is mutated, thereby reducing the insecticide’s actions, is frequently reported. Metabolic resistance, penetration resistance, and behavioral resistance are also described. The development of resistance has led the scientific community to rethink the use of chemicals by elucidating these insecticide-resistance-associated mutations, which can reveal details of insecticide-binding sites and/or different sites that allosterically affect the insecticide. Preferred conformation of the ion channels is required in order to propose strategies to circumvent the development of resistance.

This Special Issue aims to highlight recent scientific advances in this field proposed to limit and even circumvent the appearance of these resistance mechanisms. Therefore, we seek submissions of original research and review articles dealing with different strategies proposed in this area, including, for example, the following:

-Alternating the use of chemicals with distinct modes of action;
-Co-application of chemicals with distinct modes of action;
-Co-application of a synergistic agent with an insecticide to optimize efficacy while reducing the insecticide dose;
-Targeting epigenetic regulators to overcome insecticide resistance;
-Identifying the compensatory mechanisms of resistance, which may reduce insecticide efficacy to discover novel strategies for insect control;
-Recent progress in structural studies of ion channels such as molecular docking, crystallography, cryo-EM, etc., aimed at providing accurate templates for identifying unexpected structure-based target sites and facilitating rational design.

Prof. Dr. Bruno Lapied
Prof. Dr. David Barry Sattelle
Guest Editors

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