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.

Highlights

  • G-protein-coupled receptors (GPCRs), which are proteins that share a seven α-helical transmembrane structure, govern a number of biological and physiological processes in both the vertebrate and invertebrate kingdoms

  • GPCR binding to a wide variety of molecules, including hormones, neurotransmitters, ions, photons, odorants, neuropeptides and other stimuli through coupling with G proteins and arrestins [1], results in interactions with G proteins that, in turn, activate the downstream effectors of GPCR pathways, including the adenylate cyclase/cyclic AMP (AC/cAMP), phosphatidylinositol/diacylglycerol/protein kinase C (PI/DAG/PKC) and voltage gated calcium channel (Ca2+ channels) pathways, playing an indispensable role in the organism’s growth, development, reproduction and other physiological activities [6,7,8,9,10]

  • The functions of GPCR regulatory pathways and GPCR downstream intracellular cascades have been explored in the development of insecticide resistance in Culex quinquefasciatus [42,43,44], providing a good understanding of the complex molecular processes that govern the development of insecticide resistance through the GPCR signally transduction pathways

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Summary

Introduction

G-protein-coupled receptors (GPCRs), which are proteins that share a seven α-helical transmembrane structure, govern a number of biological and physiological processes in both the vertebrate and invertebrate kingdoms. GPCR binding to a wide variety of molecules (ligands), including hormones, neurotransmitters, ions, photons, odorants, neuropeptides and other stimuli through coupling with G proteins and arrestins [1], results in interactions with G proteins that, in turn, activate the downstream effectors of GPCR pathways, including the adenylate cyclase/cyclic AMP (AC/cAMP), phosphatidylinositol/diacylglycerol/protein kinase C (PI/DAG/PKC) and voltage gated calcium channel (Ca2+ channels) pathways, playing an indispensable role in the organism’s growth, development, reproduction and other physiological activities [6,7,8,9,10] These critical functions mean that a better understanding of the role played by GPCRs in cell physiology and biochemistry is crucial for efforts to develop new molecular-level human disease therapies [10,11,12,13,14,15,16]. This section reviews GPCRs and their possible functions for several insect species at the whole genome level

Classification Systems Used in Characterizing GPCRs
Tissue Specific Expression Analysis of GPCRs in Insects
Brain Tissue and Central Nervous System
Digestion and Reproduction Systems
Other Insect Organs
Conclusions
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