G-Protein Coupled Receptors (GPCRs) in Insects—A Potential Target for New Insecticide Development

Abstract

G-protein coupled receptors (GPCRs) play important roles in cell biology and insects’ physiological processes, toxicological response and the development of insecticide resistance. New information on genome sequences, proteomic and transcriptome analysis and expression patterns of GPCRs in organs such as the central nervous system in different organisms has shown the importance of these signaling regulatory GPCRs and their impact on vital cell functions. Our growing understanding of the role played by GPCRs at the cellular, genome, transcriptome and tissue levels is now being utilized to develop new targets that will sidestep many of the problems currently hindering human disease control and insect pest management. This article reviews recent work on the expression and function of GPCRs in insects, focusing on the molecular complexes governing the insect physiology and development of insecticide resistance and examining the genome information for GPCRs in two medically important insects, mosquitoes and house flies, and their orthologs in the model insect species Drosophila melanogaster. The tissue specific distribution and expression of the insect GPCRs is discussed, along with fresh insights into practical aspects of insect physiology and toxicology that could be fundamental for efforts to develop new, more effective, strategies for pest control and resistance management.

Octopamine and tyramine signaling inAedes aegypti:characterization, distribution and potential role in the Dengue vector development and physiology

“…Except for AaOA α 1-R , all other receptors showed an expression pattern characterized by high levels of transcript in eggs, followed by a decline in larval stages and then high levels in pupae and adults. A similar dynamic expression pattern was observed in Plutella xylostella , in which both OA and TA receptors showed the highest expression levels in eggs and pupae, compared with larvae and adult (Liu et al, 2021). Furthermore, in D. melanogaster, Nivaparlata lugens, Mythimna separata and gambiae , the OA β-adrenergic like receptor expression profile over the developmental stages appears similar to that observed in A. aegypti (Kastner et al, 2014; Wu et al, 2019; Guo et al, 2021; Ohhara et al, 2012).…”

Adipokinetic hormone signaling regulates cytochrome P450‐mediated chlorantraniliprole sensitivity in Spodoptera frugiperda (Lepidoptera: Noctuidae)

“…It has been reported that G‐protein‐coupled receptor (GPCR) regulation pathways play key roles in insect physiological processes, toxicological responses and the development of insecticide resistance. The GPCR regulation pathway regulates P450 gene expression and P450‐mediated insecticide resistance by activating downstream effectors, such as heterotrimeric G‐proteins, adenylate cyclase (AC), protein kinase A (PKA), and cyclic adenosine 3′,5′‐monophosphate (cAMP) 32–36 . The ligand adipokinetic hormone (AKH) synthesized and released by the corpora cardiaca (CC) and AKH receptor (AKHR) as rhodopsin‐like GPCR has been proven to be involved in the regulation of energy metabolism, feeding, reproduction, diapause, flight and other activities.…”

“…The GPCR regulation pathway regulates P450 gene expression and P450-mediated insecticide resistance by activating downstream effectors, such as heterotrimeric G-proteins, adenylate cyclase (AC), protein kinase A (PKA), and cyclic adenosine 3 0 ,5 0 -monophosphate (cAMP). [32][33][34][35][36] The ligand adipokinetic hormone (AKH) synthesized and released by the corpora cardiaca (CC) and AKH receptor (AKHR) as rhodopsin-like GPCR has been proven to be involved in the regulation of energy metabolism, feeding, reproduction, diapause, flight and other activities. Particularly under stress conditions, AKH and AKHR can couple and participate in antioxidant stress responses by activating AC, PKA and cAMP.…”

Specificity of Monoterpene Interactions with Insect Octopamine and Tyramine Receptors: Insights fromin SilicoSequence and Structure Comparison

“…GPCRs are known for their critical role in insect physiological functions . Triggered by binding of extracellular ligands, these receptors transfer signals to intracellular signaling proteins, which regulate a diverse array of intracellular signaling cascades. , Among the arthropod GPCRs, the insect octopaminergic receptors have attracted attention for new insecticide discovery due to the specificity of the octopaminergic pathway to arthropods and their crucial roles in insect physiology and cellular response. , Octopamine and tyramine receptors (OARs and TARs, respectively) are under the Class A GPCR classification. OARs are classified into three groups, namely: (1) α-adrenergic-like octopamine receptors (OAR1); (2) β-adrenergic-like octopamine receptors (OAR2); and (3) octopamine/tyramine receptors (TyrR) .…”