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https://www.readbyqxmd.com/read/29451687/gpcrs-in-context-sexual-dimorphism-in-the-cardiovascular-system
#1
REVIEW
Margaret A Mouat, James L J Coleman, Nicola J Smith
Cardiovascular disease remains the largest cause of mortality worldwide and there is a clear gender gap in disease occurrence: men are predisposed to earlier onset of cardiovascular disease, including atherosclerosis and hypertension, than are women. Oestrogen may be a driving factor for female-specific cardioprotection, though androgens and sex chromosomes are also likely to contribute to sexual dimorphism in the cardiovascular system. Many G protein-coupled receptor (GPCR)-mediated processes are involved in cardiovascular homeostasis and some exhibit clear sex-divergence...
February 16, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29448249/the-placental-secretome-identifying-potential-cross-talk-between-placenta-and-islet-%C3%AE-cells
#2
Robert Drynda, Shanta J Persaud, James E Bowe, Peter M Jones
BACKGROUND/AIMS: Insulin-secreting islet β-cells adapt to the insulin resistance associated with pregnancy by increasing functional β-cell mass, but the placental signals involved in this process are not well defined. In the current study, we analysed expression of G-protein coupled receptor (GPCR) mRNAs in mouse islets and islet GPCR ligand mRNAs in placenta during pregnancy to generate an atlas of potential interactions between the placenta and β-cells to inform future functional studies of islet adaptive responses to pregnancy...
February 8, 2018: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/29447945/salmeterol-agonist-of-%C3%AE-2-aderenergic-receptor-prevents-systemic-inflammation-via-inhibiting-nlrp3-inflammasome
#3
Nanshan Song, Yinquan Fang, Xiyang Sun, Qingling Jiang, Chenghuan Song, Miaomiao Chen, Jianhua Ding, Ming Lu, Gang Hu
β2-aderenergic receptor (β2AR) agonist, Salmeterol exhibits anti-inflammatory activities. However, the inhibitory effects of Salmeterol on inflammasome activation are elusive and the underlying mechanisms need to be explored. In this study, we established inflammatory model in primary bone marrow-derived macrophages (BMDM) from C57BL/6J mice and β-arrestin2 knockout (β-arrestin2 -/- ) mice in vitro. In vivo study by LPS intraperitoneally (i.p.) in C57BL/6J mice was carried out to ascertain its roles in systemic inflammation...
February 12, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/29447541/jtc-801-exerts-anti-proliferative-effects-in-human-osteosarcoma-cells-by-inducing-apoptosis
#4
Chang-Jun Zheng, Li-Li Yang, Jun Liu, Lei Zhong
BACKGROUND: The research of G protein-coupled receptors (GPCRs) is a promising strategy for drug discovery. In cancer therapy, there is a need to discover novel agents that can inhibit proliferation and induce apoptosis in cancer cells. JTC-801 is a novel GPCR antagonist with the function of reversing pain and anxiety symptoms. This study aims to investigate the antitumor effects of JTC-801 on human osteosarcoma cells (U2OS) and elucidate the underlying mechanism. MATERIALS AND METHODS: The Cell Counting Kit-8 assay was used to detect the viability of U2OS cells treated with JTC-801 in vitro...
February 15, 2018: Journal of Receptor and Signal Transduction Research
https://www.readbyqxmd.com/read/29447132/role-of-gpcr-mu-opioid-receptor-tyrosine-kinase-epidermal-growth-factor-crosstalk-in-opioid-induced-hyperalgesic-priming-type-ii
#5
Dionéia Araldi, Luiz F Ferrari, Jon D Levine
Repeated stimulation of mu-opioid receptors (MORs), by an MOR-selective agonist DAMGO induces type II priming, a form of nociceptor neuroplasticity, which has 2 components: opioid-induced hyperalgesia (OIH) and prolongation of prostaglandin-E2 (PGE2)-induced hyperalgesia. We report that intrathecal antisense knockdown of the MOR in nociceptors, prevented the induction of both components of type II priming. Type II priming was also eliminated by SSP-saporin, which destroys the peptidergic class of nociceptors...
January 11, 2018: Pain
https://www.readbyqxmd.com/read/29445190/the-chemokine-receptor-ccr10-promotes-inflammation-driven-hepatocarcinogenesis-via-pi3k-akt-pathway-activation
#6
Qiong Wu, Jin-Xian Chen, Yu Chen, Li-Li Cai, Xiao-Zhong Wang, Wu-Hua Guo, Jian-Feng Zheng
G-protein-coupled receptor (GPCR)-related proteins are dysregulated and the GPCR CC-chemokine receptor 10 (CCR10) is significantly upregulated in inflammation-driven HCC. However, CCR10's role in inflammation-driven hepatocarcinogenesis remains unknown. The aim of this study was to evaluate the role of CCR10 in inflammation-driven hepatocarcinogenesis. Via a targeted gene expression microarray screening alterations in GPCR family gene expression, we found CCR10 to be significantly upregulated in hepatocytes isolated from inflammation-driven human HCC tumors and matching paracancerous tissues...
February 14, 2018: Cell Death & Disease
https://www.readbyqxmd.com/read/29444827/site-specific-polyubiquitination-differentially-regulates-parathyroid-hormone-receptor-initiated-mapk-signaling-and-cell-proliferation
#7
Qiangmin Zhang, Kunhong Xiao, Hongda Liu, Lei Song, Jennifer C McGarvey, W Bruce Sneddon, Alessandro Bisello, Peter A Friedman
G protein-coupled receptor (GPCR) signaling and trafficking are essential for cellular function and regulated by phosphorylation, β-arrestin, and ubiquitination. The GPCR parathyroid hormone receptor (PTHR) exhibits time-dependent reversible ubiquitination. The exact ubiquitination sites in PTHR are unknown, but extend upstream of its intracellular tail. Here, using tandem MS, we identified Lys-388 in the third loop and Lys-484 in the C-terminal tail as primary ubiquitination sites in PTHR. We found that PTHR ubiquitination requires β-arrestin and does not display a preference for β-arrestin1 or 2...
February 14, 2018: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/29443979/gpcr-lock-and-key-become-flexible
#8
Marc Baldus
No abstract text is available yet for this article.
February 14, 2018: Nature Chemical Biology
https://www.readbyqxmd.com/read/29443899/protease-activated-receptor-4-par4-a-promising-target-for-antiplatelet-therapy
#9
REVIEW
Gamariel Rwibasira Rudinga, Ghulam Jilany Khan, Yi Kong
Cardiovascular diseases (CVDs) are currently among the leading causes of death worldwide. Platelet aggregation is a key cellular component of arterial thrombi and major cause of CVDs. Protease-activated receptors (PARs), including PAR1, PAR2, PAR3 and PAR4, fall within a subfamily of seven-transmembrane G-protein-coupled receptors (GPCR). Human platelets express PAR1 and PAR4, which contribute to the signaling transduction processes. In association with CVDs, PAR4 not only contributes to platelet activation but also is a modulator of cellular responses that serve as hallmarks of inflammation...
February 14, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29442133/follicle-stimulating-hormone-enhances-hepatic-gluconeogenesis-by-grk2-mediated-ampk-hyperphosphorylation-at-ser485-in-mice
#10
Xiaoyi Qi, Yanjing Guo, Yongfeng Song, Chunxiao Yu, Lifang Zhao, Li Fang, Dehuan Kong, Jiajun Zhao, Ling Gao
AIMS/HYPOTHESIS: Increased serum follicle-stimulating hormone (FSH) is correlated with fasting hyperglycaemia. However, the underlying mechanism remains unclear. Because excessive hepatic gluconeogenesis is a major cause of fasting hyperglycaemia the present study investigated whether FSH increases hepatic gluconeogenesis in mice. METHODS: Ovariectomised mice supplemented with oestradiol (E2) to maintain normal levels of serum E2 (OVX+E2 mice) were injected with low or high doses of FSH...
February 13, 2018: Diabetologia
https://www.readbyqxmd.com/read/29433403/the-essential-role-of-g-protein-coupled-receptor-gpcr-signaling-in-regulating-t-cell-immunity
#11
Dashan Wang
AIM: The aim of this paper is to clarify the critical role of GPCR signaling in T cell immunity. METHODS: The G protein-coupled receptors (GPCRs) are the most common targets in current pharmaceutical industry, and represent the largest and most versatile family of cell surface communicating molecules. GPCRs can be activated by a diverse array of ligands including neurotransmitters, chemokines as well as sensory stimuli. Therefore, GPCRs are involved in many key cellular and physiological processes, such as sense of light, taste and smell, neurotransmission, metabolism, endocrine and exocrine secretion...
February 12, 2018: Immunopharmacology and Immunotoxicology
https://www.readbyqxmd.com/read/29432522/wdl-rf-predicting-bioactivities-of-ligand-molecules-acting-with-g-protein-coupled-receptors-by-combining-weighted-deep-learning-and-random-forest
#12
Jiansheng Wu, Qiuming Zhang, Weijian Wu, Tao Pang, Haifeng Hu, Wallace K B Chan, Xiaoyan Ke, Yang Zhang, Jonathan Wren
Motivation: Precise assessment of ligand bioactivities (including IC50, EC50, Ki, Kd, etc.) is essential for virtual screening and lead compound identification. However, not all ligands have experimentally-determined activities. In particular, many G protein-coupled receptors (GPCRs), which are the largest integral membrane protein family and represent targets of nearly 40% drugs on the market, lack published experimental data about ligand interactions. Computational methods with the ability to accurately predict the bioactivity of ligands can help efficiently address this problem...
February 8, 2018: Bioinformatics
https://www.readbyqxmd.com/read/29430989/nk1r-5-ht1ar-interaction-is-related-to-the-regulation-of-melanogenesis
#13
Huali Wu, Yucheng Zhao, Qiaoling Huang, Minxuan Cai, Qi Pan, Mengsi Fu, Xiaohong An, Zhenjiang Xia, Meng Liu, Yu Jin, Ling He, Jing Shang
Substance P (SP) is a candidate mediator along the brain-skin axis and can mimic the effects of stress to regulate melanogenesis. Previously, we and others have found that the regulation of SP for pigmentary function was mediated by neurokinin 1 receptor (NK1R). Emerging evidence has accumulated that psychologic stress can induce dysfunction in the cutaneous serotonin 5-hydroxytryptamine (5-HT)-5-HT1A/1B receptor system, thereby resulting in skin hypopigmentation. Moreover, NK1R and 5-HTR (except 5-HT3) belong to GPCR...
February 7, 2018: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/29425893/the-mechanisms-behind-decreased-internalization-of-angiotensin-ii-type-1-receptor
#14
REVIEW
Jingwei Bian, Suli Zhang, Ming Yi, MingmingYue, Huirong Liu
The internalization of angiotensin II type 1 receptor (AT 1 R) plays an important role in maintaining cardiovascular homeostasis. Decreased receptor internalization is closely related to cardiovascular diseases induced by the abnormal activation of AT 1 R, such as hypertension. However, the mechanism behind reduced AT 1 R internalization is not fully understood. This review focuses on four parts of the receptor internalization process (the combination of agonists and receptors, receptor phosphorylation, endocytosis, and recycling) and summarizes the possible mechanisms by which AT 1 R internalization is reduced based on these four parts of the process...
February 6, 2018: Vascular Pharmacology
https://www.readbyqxmd.com/read/29425482/to-bind-or-not-to-bind-unravelling-gpcr-polypharmacology
#15
Patrick M Sexton, Arthur Christopoulos
Interaction of a single drug with multiple targets through "polypharmacology" is increasingly recognized as necessary for treatment of complex diseases, such as schizophrenia. G protein-coupled receptors (GPCRs) are major medicinal targets, and understanding the structural basis of both GPCR drug selectivity and promiscuity could provide novel avenues for drug development.
February 8, 2018: Cell
https://www.readbyqxmd.com/read/29420171/ap2-mutations-impair-calcium-sensing-receptor-trafficking-and-signaling-and-show-an-endosomal-pathway-to-spatially-direct-g-protein-selectivity
#16
Caroline M Gorvin, Angela Rogers, Benoit Hastoy, Andrei I Tarasov, Morten Frost, Silvia Sposini, Asuka Inoue, Michael P Whyte, Patrik Rorsman, Aylin C Hanyaloglu, Gerda E Breitwieser, Rajesh V Thakker
Spatial control of G-protein-coupled receptor (GPCR) signaling, which is used by cells to translate complex information into distinct downstream responses, is achieved by using plasma membrane (PM) and endocytic-derived signaling pathways. The roles of the endomembrane in regulating such pleiotropic signaling via multiple G-protein pathways remain unknown. Here, we investigated the effects of disease-causing mutations of the adaptor protein-2 ? subunit (AP2?) on signaling by the class C GPCR calcium-sensing receptor (CaSR)...
January 23, 2018: Cell Reports
https://www.readbyqxmd.com/read/29420021/a-selective-photoaffinity-probe-enables-assessment-of-cannabinoid-cb2-receptor-expression-and-ligand-engagement-in-human-cells
#17
Marjolein Soethoudt, Sara C Stolze, Matthias V Westphal, Luuk van Stralen, Andrea Martella, Eva J van Rooden, Wolfgang Guba, Zoltan V Varga, Hui Deng, Sander I van Kasteren, Uwe Grether, Adriaan P IJzerman, Pal Pacher, Erick M Carreira, Herman S Overkleeft, Andreea Ioan-Facsinay, Laura H Heitman, Mario van der Stelt
Chemical tools and methods that report on G protein-coupled receptor (GPCR) expression levels and receptor occupancy by small molecules are highly desirable. We report the development of LEI121 as a photoreactive probe to study the type 2 cannabinoid receptor (CB2R), a promising GPCR to treat tissue injury and inflammatory diseases. LEI121 is the first CB2R-selective bifunctional probe that covalently captures CB2R upon photoactivation. An incorporated alkyne serves as ligation handle for the introduction of reporter groups...
February 8, 2018: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/29412765/nomad-biosensors-a-new-multiplexed-technology-for-the-screening-of-gpcr-ligands
#18
Rosa M Mella, Danel Kortazar, Meritxell Roura-Ferrer, Clarisa Salado, María Valcárcel, Amaia Castilla, Patricia Villacé
Nomad Technology (Innoprot [Innovative Technologies in Biological Systems], Derio, Spain), a novel tool for multiplexing high-throughput cell-based G protein-coupled receptor (GPCR) assays, is described in this work. This new technology comprises a family of fluorescent biosensors called Nomad Biosensors that allow for the measurement of responses mediated by G proteins through their interactions with second-messenger transduction proteins. GPCRs are one of the largest protein families of receptors in eukaryotes, and their signaling mediates important physiological processes within cells...
February 1, 2018: SLAS Technology
https://www.readbyqxmd.com/read/29412102/cloning-expression-purification-and-characterization-of-oligomeric-states-of-the-native-5ht2a-g-protein-coupled-receptor
#19
Gopa Mahesh, Priyank Jaiswal, Sandip Dey, Jayati Sengupta, Sujoy Mukherjee
The serotonin 5HT2A G-protein coupled receptor (GPCR) is involved in a plethora of neuromodulatory functions and its dysregulation is linked to psychiatric disorders. However, there is insufficient, direct structural evidence of the structure, dynamics and the mechanism of function of this receptor. Cholesterol plays an important role in the function of many GPCRs and reduced cholesterol levels may be linked to serotonergic pathway disruptions. But cholesterol's effect on the structure, especially the oligomeric states of the 5HT2A receptor is not well understood...
February 6, 2018: Protein and Peptide Letters
https://www.readbyqxmd.com/read/29411438/a-rapid-fluorogenic-gpcr-%C3%AE-arrestin-interaction-assay
#20
Qiang Zhang, Yao-Wu Zheng, Shaun R Coughlin, Xiaokun Shu
Detection of protein-protein interactions involved in signal transduction in live cells and organisms has a variety of important applications. We report a fluorogenic assay for G protein-coupled receptor (GPCR) - β-arrestin interaction that is genetically encoded, generalizes to multiple GPCRs and features high signal-to-noise because fluorescence is absent until its components interact upon GPCR activation. Fluorescence after protease-activated receptor-1 activation developed in minutes and required specific serine-threonine residues in the receptor carboxyl tail, consistent with a classical G protein-coupled receptor kinase dependent β-arrestin recruitment mechanism...
February 7, 2018: Protein Science: a Publication of the Protein Society
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