G protein-coupled receptors function as cell membrane receptors for the steroid hormone 20-hydroxyecdysone
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REVIEW
Open Access
G protein-coupled receptors function as cell membrane receptors for the steroid hormone 20-hydroxyecdysone Xiao-Fan Zhao
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/PKAsignaling 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. Keywords: GPCR, Steroid hormone, 20-hydroxyecdysone, Cell membrane receptor, Signal pathway
Background 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. GPCRs mediate various cellular responses from the extracellular environment. A GPCR is activated upon binding of its ligand, which causes a conformational change in the GPCR’s structure. The activated GPCR then interacts with G Correspondence: [email protected] Shandong Provincial Key Laboratory of Animal Cells and Developmental Biology, School of Life Sciences, Shandong University, Qingdao 266237, China
protein to induce further signaling cascades [1]. Over 800 GPCRs have been identified in the human genome [2], 1000 in the Caenorhabditis elegans genome [3], and 200 in the Drosophila melanogaster genome [4]. GPCRs have been identified as the cell membrane receptors of various ligands, including biological amines, amino acids, ions, lipids, peptides/proteins, light, odorant, pheromones, nucleotides, and opiates [5]. However, the functions and pathways of GPCRs as receptors of animal, including insect steroid hormo
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