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G protein-coupled receptors (GPCRs) are the largest family of membrane receptors in animals and humans, which transmit various signals from the extracellular environment into cells. Studies have reported that several GPCRs transmit the same signal; however, the mechanism is unclear. In the present study, we identified all 122 classical GPCRs from the genome of , a lepidopteran pest species. Twenty-four GPCRs were identified as upregulated at the metamorphic stage by comparing the transcriptomes of the midgut at the metamorphic and feeding stages. Nine of them were confirmed to be upregulated at the metamorphic stage. RNA interference in larvae revealed the prolactin-releasing peptide receptor (PRRPR), smoothened (SMO), adipokinetic hormone receptor (AKHR), and 5-hydroxytryptamine receptor (HTR) are involved in steroid hormone 20-hydroxyecdysone (20E)-promoted pupation. Frizzled 7 (FZD7) is involved in growth, while tachykinin-like peptides receptor 86C (TKR86C) had no effect on growth and pupation. Via these GPCRs, 20E regulated the expression of different genes, respectively, including (encoding phosphatidylinositol-3,4,5-trisphosphate 3-phosphatase), (encoding forkhead box O), (encoding broad isoform Z7), (encoding Krüppel homolog 1), (encoding Wingless/Integrated) and , with hormone receptor 3 (HHR3) as their common regulating target. PRRPR was identified as a new 20E cell membrane receptor using a binding assay. These data suggested that 20E, via different GPCRs, regulates different gene expression to integrate growth and development.
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http://dx.doi.org/10.3389/fcell.2021.753787 | DOI Listing |
Front Neurosci
August 2025
Beijing Life Science Academy, Beijing, China.
Hypocretin, also known as orexin, is a hypothalamic neuropeptide that regulates essential physiological processes including arousal, energy metabolism, feeding behavior, and emotional states. Through widespread projections and two G-protein-coupled receptors-HCRT-1R and HCRT-2R-the hypocretin system exerts diverse modulatory effects across the central nervous system. The role of hypocretin in maintaining wakefulness is well established, particularly in narcolepsy type 1 (NT1), where loss of hypocretin neurons leads to excessive daytime sleepiness and cataplexy.
View Article and Find Full Text PDFFASEB Bioadv
September 2025
Kobilka Institute of Innovative Drug Discovery, School of Medicine The Chinese University of Hong Kong Shenzhen Guangdong China.
Formyl peptide receptor 1 (FPR1) is a G protein-coupled receptor (GPCR) that mediates chemotaxis and bactericidal activities in phagocytes. The monoclonal antibody 5F1 is generated against full-length FPR1 and used widely for detection of FPR1 expression. This study aimed to characterize 5F1 for its functions.
View Article and Find Full Text PDFFront Endocrinol (Lausanne)
September 2025
Guangxi Key Laboratory of Tumor Immunology and Microenvironmental Regulation, Guilin Medical University, Guilin, China.
Endometrial cancer (EC) is one of the most common gynecological cancers in developed countries. Like EC, most female reproductive tract malignancies are thought to be hormonally driven, with estrogen signaling acting as an oncogenic signal. The actions of estrogen are mediated through the classical nuclear estrogen receptors α (ER-α) and β (ER-β) as well as transmembrane G protein-coupled estrogen receptors (GPR30 and GPER).
View Article and Find Full Text PDFFront Oral Health
August 2025
Conservative Dentistry and Endodontics, AB Shetty Memorial Institute of Dental Sciences, Nitte (deemed to be) University, Mangalore, India.
Short-chain fatty acids (SCFAs), primarily acetate (C2), propionate (C3), and butyrate (C4), are crucial microbial metabolites formed by the fermentation of dietary fibers by gut microbiota in the colon. These SCFAs, characterized by fewer than six carbon atoms, serve as an essential energy source for colonic epithelial cells and contribute approximately 10% of the body's total energy requirement. They are central to maintaining gut health through multiple mechanisms, including reinforcing intestinal barrier function, exerting anti-inflammatory effects, regulating glucose and lipid metabolism, and influencing host immune responses.
View Article and Find Full Text PDFChem Sci
August 2025
Graduate School of Pharmaceutical Sciences, The University of Tokyo 7-3-1 Hongo Bunkyo Tokyo 113-0033 Japan.
Residence time, which refers to the average duration a drug remains bound to its receptor, is a crucial parameter in determining its pharmacological effects. However, the mechanisms governing the residence time of G protein-coupled receptor (GPCR) ligands remain unclear. In this study, we observed NMR signals from the methyl groups of alanine and methionine located at the intersection of the binding cavity and extracellular loops of AAR under conditions where E165Q and T256A mutations led to reduced residence times.
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