G protein-coupled receptors (GPCRs) play a central role in signal transmission, thereby controlling many facets of cellular function. Overwhelming evidence now implicates GPCRs, G proteins and their downstream signaling targets in cancer initiation and progression, where they can influence aberrant cell growth and survival, largely through activation of AKT/mTOR, MAPKs, and Hippo signaling pathways. GPCRs also play critical roles in the invasion and metastasis of cancer cells via activation of Rho GTPases and cytoskeletal changes, and angiogenesis to supply the tumor with nutrients and provide routes for metastasis. Lastly, GPCRs contribute to the establishment and maintenance of a permissive tumor microenvironment. Understanding GPCR involvement in cancer malignancy may help identify novel therapeutic opportunities for cancer prevention and treatment.
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http://dx.doi.org/10.1016/j.ceb.2014.01.005 | DOI Listing |
Int J Mol Sci
December 2024
Department of Biochemistry and Molecular Biology, School of Basic Medical Sciences, Cheeloo College of Medicine, Shandong University, Jinan 250012, China.
G protein-coupled receptors (GPCRs) play essential roles in numerous physiological processes and are key targets for drug development. Among them, adhesion GPCRs (aGPCRs) stand out for their unique domain structures and diverse functions. ADGRG2 is a member of the aGPCR family and is involved in the regulation of various systems in the human body, including reproductive, nervous, cardiovascular, and endocrine systems.
View Article and Find Full Text PDFInsects
November 2024
Shandong Engineering Research Center for Environment-Friendly Agricultural Pest Management, College of Plant Health and Medicine, Qingdao Agricultural University, Qingdao 266109, China.
Neuropeptide (abbreviated as ) is a recently discovered peptide that is present in many arthropods and is the ligand of the , a member of the G protein-coupled receptors (GPCRs) superfamily, which plays a regulatory role in diverse physiological processes such as feeding, circadian rhythm, insulin production, lipid metabolism, growth, and reproduction. However, the function of this gene in aphids is still unknown. Here, we characterized and determined the potential role of / signaling in the pea aphid, , which is a notorious pest in agriculture.
View Article and Find Full Text PDFInt J Mol Sci
December 2024
Department of Pharmacology and Therapeutic Innovation, School of Pharmaceutical Sciences, Nagasaki University, Nagasaki 852-8521, Japan.
The receptor transporter protein 4 (RTP4) is a receptor chaperone protein that targets class A G-protein coupled receptor (GPCR)s. Recently, it has been found to play a role in peripheral inflammatory regulation, as one of the interferon-stimulated genes (ISGs). However, the detailed role of RTP4 in response to inflammatory stress in the central nervous system has not yet been fully understood.
View Article and Find Full Text PDFCells
December 2024
Laboratory of Molecular Science, Institute of Cytology, Russian Academy of Sciences, Saint Petersburg 194064, Russia.
Osteoporosis is characterized by increased resorption and decreased bone formation; it is predominantly influenced by genetic factors. G-protein coupled receptors (GPCRs) play a vital role in bone homeostasis, and mutations in these genes are associated with osteoporosis. This study aimed to investigate the impact of single nucleotide polymorphism (SNP) rs1042713 in the gene, encoding the beta-2-adrenergic receptor, on osteoblastogenesis.
View Article and Find Full Text PDFJ Am Chem Soc
January 2025
Materials and Process Simulation Center, California Institute of Technology, Pasadena, California 91125, United States.
G protein-coupled receptors (GPCRs) play central roles in regulating cellular responses through heterotrimeric G proteins (GP). Extensive studies have elucidated the complex cellular signaling mediated by GPCRs that accompany dynamic conformational changes upon activation. However, there has been less focus on the role of the GP on the activation process, particularly for class C GPCRs that function as obligate dimers.
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