Abstract
G protein-coupled receptors (GPCRs) are cell membrane receptors for various ligands. Recent studies have suggested that GPCRs transmit animal steroid hormone signals. Certain GPCRs have been shown to bind steroid hormones, for example, G protein-coupled estrogen receptor 1 (GPER1) binds estrogen in humans, and Drosophila dopamine/ecdysteroid receptor (DopEcR) binds the molting hormone 20-hydroxyecdysone (20E) in insects. This review summarizes the research progress on GPCRs as animal steroid hormone cell membrane receptors, including the nuclear and cell membrane receptors of steroid hormones in mammals and insects, the 20E signaling cascade via GPCRs, termination of 20E signaling, and the relationship between genomic action and the nongenomic action of 20E. Studies indicate that 20E induces a signal via GPCRs to regulate rapid cellular responses, including rapid Ca2+ release from the endoplasmic reticulum and influx from the extracellular medium, as well as rapid protein phosphorylation and subcellular translocation. 20E via the GPCR/Ca2+/PKC/signaling axis and the GPCR/cAMP/PKA-signaling axis regulates gene transcription by adjusting transcription complex formation and DNA binding activity. GPCRs can bind 20E in the cell membrane and after being isolated, suggesting GPCRs as cell membrane receptors of 20E. This review deepens our understanding of GPCRs as steroid hormone cell membrane receptors and the GPCR-mediated signaling pathway of 20E (20E-GPCR pathway), which will promote further study of steroid hormone signaling via GPCRs, and presents GPCRs as targets to explore new pharmaceutical materials to treat steroid hormone-related diseases or control pest insects.Ex2qbyg2iQ_s9X6U5oRhrvVideo abstractGraphical abstract
Highlights
G protein-coupled receptors (GPCRs) are seventransmembrane proteins that are located in the cell membrane, with their N- and C-termini located on the outer and inner surfaces, respectively
Activated-phospholipase C gamma 1 (PLCG1) migrates toward the cell membrane to initiate intracellular Ca2+ signaling and calcium channel-controlled Ca2+ influx, which triggers protein kinase C (PKC)-mediated ultraspiracle protein (USP) phosphorylation to modulate USP binding to ecdysone response elements (EcRE) for subsequent gene transcription
These findings provide evidence that 20E regulates the genomic pathway for gene transcription through an 20E-responsive GPCR (ErGPCR)-1/ G protein alpha q subunit (Gαq)/PLCG1/Ca2+/PKCdependent nongenomic pathway [52]
Summary
G protein-coupled receptors (GPCRs) are seventransmembrane proteins that are located in the cell membrane, with their N- and C-termini located on the outer and inner surfaces, respectively. Activated-PLCG1 migrates toward the cell membrane to initiate intracellular Ca2+ signaling and calcium channel-controlled Ca2+ influx, which triggers PKC-mediated USP phosphorylation to modulate USP binding to EcRE for subsequent gene transcription. These findings provide evidence that 20E regulates the genomic pathway for gene transcription through an ErGPCR-1/ Gαq/PLCG1/Ca2+/PKCdependent nongenomic pathway [52]. From the studies in H. armigera, the genomic action/pathway of 20E is regulated by the nongenomic action/pathway, because the 20E-induced rapid calcium increase in cells activates protein kinases [52, 56], promotes EcR-USP transcription complex formation, which initiates gene transcription in 20E pathway [64]. The insecticidal activity of the 20E can be developed to control insect pests [74]
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