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G coupled protein receptors

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https://www.readbyqxmd.com/read/28734639/ffa4-gpr120-pharmacology-and-therapeutic-opportunities
#1
REVIEW
Graeme Milligan, Elisa Alvarez-Curto, Brian D Hudson, Rudi Prihandoko, Andrew B Tobin
Free Fatty Acid receptor 4 (FFA4), also known as GPR120, is a G-protein-coupled receptor (GPCR) responsive to long-chain fatty acids that is attracting considerable attention as a potential novel therapeutic target for the treatment of type 2 diabetes mellitus (T2DM). Although no clinical studies have yet been initiated to assess efficacy in this indication, a significant number of primary publications and patents have highlighted the ability of agonists with potency at FFA4 to improve glucose disposition and enhance insulin sensitivity in animal models...
July 19, 2017: Trends in Pharmacological Sciences
https://www.readbyqxmd.com/read/28734238/decreased-levels-of-g-protein-coupled-estrogen-receptor-in-children-with-autism-spectrum-disorders
#2
Hatice Altun, Ergül Belge Kurutaş, Nilfer Şahin, Hayati Sınır, Ebru Fındıklı
Sex hormones, specially estrogen, and ıt is receptors plays a critical role in the pathogenesis of psychiatric disorders including autism spectrum disorders (ASD). The aim of this study was to investigate the relationship between ASD and G protein-coupled estrogen receptor (GPER), a recently discovered estrogen receptors, and also to study the relation of serum GPER levels with the severity of autistic symptoms. The present study included 45 children with drug naive ASD diagnosed by DSM-V criteria, aged between 3 and 12 years and 40 age- and gender-matched healthy controls...
June 6, 2017: Psychiatry Research
https://www.readbyqxmd.com/read/28733900/the-putative-role-of-environmental-mercury-in-the-pathogenesis-and-pathophysiology-of-autism-spectrum-disorders-and-subtypes
#3
REVIEW
G Morris, B K Puri, R E Frye, M Maes
Exposure to organic forms of mercury has the theoretical capacity to generate a range of immune abnormalities coupled with chronic nitro-oxidative stress seen in children with autism spectrum disorder (ASD). The paper discusses possible mechanisms explaining the neurotoxic effects of mercury and possible associations between mercury exposure and ASD subtypes. Environmental mercury is neurotoxic at doses well below the current reference levels considered to be safe, with evidence of neurotoxicity in children exposed to environmental sources including fish consumption and ethylmercury-containing vaccines...
July 22, 2017: Molecular Neurobiology
https://www.readbyqxmd.com/read/28733525/ackr3-expression-on-diffuse-large-b-cell-lymphoma-is-required-for-tumor-spreading-and-tissue-infiltration
#4
Viola Puddinu, Sabrina Casella, Egle Radice, Sylvia Thelen, Stefan Dirnhofer, Francesco Bertoni, Marcus Thelen
Diffuse large B cell lymphoma (DLBCL) is the most frequent lymphoma accounting for more than the 30% of the cases. Involvement of extranodal sites, such as bone marrow and central nervous system, is associated with poor prognosis. A contribution of the chemokine system in these processes is assumed as it is known as a critical regulator of the metastatic process in cancer. The atypical chemokine receptor 3 (ACKR3), which does not couple to G-proteins and does not mediate cell migration, acts as a scavenger for CXCL11 and CXCL12, interfering with the tumor homing CXCL12/CXCR4 axis...
June 29, 2017: Oncotarget
https://www.readbyqxmd.com/read/28733475/gper-modulates-tone-and-coronary-vascular-reactivity-in-male-and-female-rats
#5
Angelina Rafaela Debortoli, Wender do Nascimento Rouver, Nathalie Tristão Banhos Delgado, Vinicius Mengal, Erick Roberto Gonçalves Claudio, Laena Pernomian, Lusiane Maria Bendhack, Margareth Ribeiro Moysés, Roger Lyrio Dos Santos
Compared with age-matched men, premenopausal women are largely protected from coronary artery disease, a difference that is lost after menopause. The effects of oestrogens are mediated by the activation of nuclear receptors (ERα and ERβ) and by the G protein-coupled oestrogen receptor (GPER). This study aims to evaluate the potential role of GPER in coronary circulation in female and male rats. The baseline coronary perfusion pressure (CPP) and the concentration-response curve with a GPER agonist (G-1) were evaluated in isolated hearts before and after the blockade of GPER...
August 2017: Journal of Molecular Endocrinology
https://www.readbyqxmd.com/read/28733085/functional-consequences-of-chemically-induced-%C3%AE-arrestin-binding-to-chemokine-receptors-cxcr4-and-ccr5-in-the-absence-of-ligand-stimulation
#6
Marcel Liebick, Sarah Henze, Viola Vogt, Martin Oppermann
Chemokine receptor signaling is a tightly regulated process which was for a long time exclusively attributed to heterotrimeric G proteins. β-Arrestins constitute a separable signaling arm from classical heterotrimeric G proteins, in addition to their well-established roles in receptor desensitization and endocytosis. In order to clearly dissect β-arrestin- from G protein-dependent effects we forced the recruitment of β-arrestin to CXCR4 and CCR5 independently of agonist-promoted receptor activation through chemically-induced dimerization...
July 18, 2017: Cellular Signalling
https://www.readbyqxmd.com/read/28733084/reciprocal-regulation-of-%C3%AE-2-adrenoceptor-activated-camp-response-element-binding-protein-signalling-by-arrestin2-and-arrestin3
#7
Alexander Pearce, Lucy Sanders, Paul J Brighton, Shashi Rana, Justin C Konje, Jonathon M Willets
Activation of Gs coupled receptors (e.g. β2-adrenoreceptor (β2AR)) expressed within the uterine muscle layer (myometrium), promotes intracellular cAMP generation, inducing muscle relaxation through short-term inhibition of contractile proteins, and longer-term modulation of cellular phenotype to promote quiescence. In the myometrium cAMP-driven modulation of cell phenotype is facilitated by CREB activity, however despite the importance of CREB signalling in the promotion of myometrial quiescence during pregnancy, little is currently known regarding the molecular mechanisms involved...
July 18, 2017: Cellular Signalling
https://www.readbyqxmd.com/read/28731695/how-rhodopsin-tunes-the-equilibrium-between-protonated-and-deprotonated-forms-of-the-retinal-chromophore
#8
Siri Camee van Keulen, Alicia Solano, Ursula Rothlisberger
Rhodopsin is a photoactive G-protein-coupled receptor (GPCR) that converts dim light into a signal for the brain, leading to eyesight. Full activation of this GPCR is achieved after passing through several steps of the protein's photoactivation pathway. Key events of rhodopsin activation are the initial cis-trans photoisomerisation of the covalently bound retinal moiety followed by conformational rearrangements and deprotonation of the chromophore's protonated Schiff base (PSB), which ultimately lead to full activation in the meta II state...
July 21, 2017: Journal of Chemical Theory and Computation
https://www.readbyqxmd.com/read/28731171/protective-role-of-pollen-typhae-total-flavone-against-the-palmitic-acid-induced-impairment-of-glucose-stimulated-insulin-secretion-involving-gpr40-signaling-in-ins-1-cells
#9
Xiao-Tao Feng, Hui-Ming Duan, Shuang-Lei Li
Prolonged elevated levels of free fatty acids (FFAs) contribute to the impairment of insulin secretion function of pancreatic β cells, a hallmark of type 2 diabetes, which is partly attributed to the dysfunction of G-protein-coupled receptor 40 (GPR40) signaling. Pollen Typhae total flavone (PTF), an extract from a Chinese herbal medicine named Pollen Typhae, has been reported to effectively treat type 2 diabetes, but the underlying mechanisms remain to be fully elucidated. In the present study, palmitic acid (PA), a saturated fatty acid, severely impaired glucose-stimulated insulin secretion (GSIS) in a time-dependent manner in INS-1 cells, and PTF treatment prevented the impairment in a dose-dependent manner...
July 18, 2017: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/28731148/molecular-genetics-and-targeted-therapy-of-wnt-related-human-diseases-review
#10
Masuko Katoh, Masaru Katoh
Canonical WNT signaling through Frizzled and LRP5/6 receptors is transduced to the WNT/β-catenin and WNT/stabilization of proteins (STOP) signaling cascades to regulate cell fate and proliferation, whereas non-canonical WNT signaling through Frizzled or ROR receptors is transduced to the WNT/planar cell polarity (PCP), WNT/G protein-coupled receptor (GPCR) and WNT/receptor tyrosine kinase (RTK) signaling cascades to regulate cytoskeletal dynamics and directional cell movement. WNT/β-catenin signaling cascade crosstalks with RTK/SRK and GPCR-cAMP-PKA signaling cascades to regulate β-catenin phosphorylation and β-catenin-dependent transcription...
July 19, 2017: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/28730837/molecular-basis-of-trpa1-regulation-in-nociceptive-neurons-a-review
#11
A Kádková, V Synytsya, J Krusek, L Zímová, V Vlachová
Transient receptor potential A1 (TRPA1) is an excitatory ion channel that functions as a cellular sensor, detecting a wide range of proalgesic agents such as environmental irritants and endogenous products of inflammation and oxidative stress. Topical application of TRPA1 agonists produces an acute nociceptive response through peripheral release of neuropeptides, purines and other transmitters from activated sensory nerve endings. This, in turn, further regulates TRPA1 activity downstream of G-protein and phospholipase C-coupled signaling cascades...
July 18, 2017: Physiological Research
https://www.readbyqxmd.com/read/28730831/the-galanin-and-galanin-receptor-subtypes-its-regulatory-role-in-the-biological-and-pathological-functions
#12
J Šípková, I Kramáriková, S Hynie, V Klenerová
The multitalented neuropeptide galanin was first discovered 30 years ago but initially no biologic activity was found. Further research studies discovered the presence of galanin in the brain and some peripheral tissues, and galanin was identified as a modulator of neurotransmission in the central and peripheral nervous system. Over the last decade there were performed very intensive studies of the neuronal actions and also of nonneuronal actions of galanin. Other galanin family peptides have been described, namely galanin, galanin-like peptide, galanin-message associated peptide and alarin...
July 18, 2017: Physiological Research
https://www.readbyqxmd.com/read/28729619/effects-of-4-1h-quinolinone-derivative-a-novel-non-nucleotide-allosteric-purinergic-p2y-2-agonist-on-cardiomyocytes-in-neonatal-rats
#13
Kensuke Sakuma, Hideyuki Nakagawa, Tatsuo Oikawa, Masakuni Noda, Shota Ikeda
Purinergic P2Y 2 receptors, G-protein coupled receptors that primarily couple with Gαq/11-proteins, are activated equipotently by adenosine-5'-triphosphate (ATP) and uridine-5'-triphosphate. Evidence suggests that P2Y 2 agonists make potential drug candidates for the treatment of cardiovascular diseases. However, selective non-nucleotide, small-molecule P2Y 2 agonists have yet to be developed. In this report, we discuss Compound 89, a novel non-nucleotide allosteric P2Y 2 agonist that was active in signal transduction and gene induction, and in our in vitro cardiac hypertrophy model...
July 20, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28729439/striatal-gpr88-modulates-foraging-efficiency
#14
Aundrea Rainwater, Elisenda Sanz, Richard D Palmiter, Albert Quintana
The striatum is anatomically and behaviorally implicated in behaviors that promote efficient foraging. To investigate this function, we studied instrumental choice behavior in mice lacking GPR88, a striatum-enriched orphan G-protein-coupled receptor that modulates striatal medium spiny neuron (MSN) excitability. Our results reveal that hungry mice lacking GPR88 (KO mice) were slow to acquire food-reinforced lever-press, but could lever press similar to controls on a progressive-ratio schedule. Both WT and KO mice discriminated between reward and no-reward levers; however, KO mice failed to discriminate based on relative quantity- reward (1 versus 3 food pellets) or effort (3 versus 9 lever presses)...
July 20, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28728843/expression-and-prognostic-role-of-orphan-receptor-gpr110-in-glioma
#15
Haiping Shi, Shiyuan Zhang
Glioma is the most common type of malignancy in the central nervous system, which has a poor prognosis due to its rapid progression and diffuse invasion. Identification of novel biomarkers for glioma would be invaluable for studying disease mechanism and improving prognosis. Orphan G protein-coupled receptor 110 (GPR110) belongs to the subfamily VI of adhesion GPCR. The knowledge of the ligand, signaling pathway or physiology function of GPR110 is poorly elucidated. The potential role of GPR110 as an oncogene in mouse has been recently reported by mutagenesis screen...
July 17, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28728565/identification-of-differential-co-expressed-gene-networks-in-early-rheumatoid-arthritis-achieving-sustained-drug-free-remission-after-treatment-with-a-tocilizumab-based-or-methotrexate-based-strategy
#16
Xavier M Teitsma, Johannes W G Jacobs, Michal Mokry, Michelle E A Borm, Attila Pethö-Schramm, Jacob M van Laar, Johannes W J Bijlsma, Floris P J Lafeber
BACKGROUND: Methotrexate is endorsed to be used as first-line treatment in rheumatoid arthritis (RA). However, a large proportion of patients need additional treatment with a biological disease-modifying anti-rheumatic drug (DMARD) to adequately suppress their disease activity. A better understanding of genotypes could help to distinguish between patients with different pathogenic mechanisms. The aim of this study was therefore to identify networks of genes within DMARD-naive early RA patients associated with achieving sustained drug-free remission (sDFR) after initiating tocilizumab plus methotrexate, tocilizumab, or methotrexate therapy...
July 20, 2017: Arthritis Research & Therapy
https://www.readbyqxmd.com/read/28728042/pharmacological-relationships-and-ligand-discovery-of-g-protein-coupled-receptors-revealed-by-simultaneous-ligand-and-receptor-clustering
#17
Cheng Zhang, Yi-Ming Shao, Xiaohua Ma, Siew Lee Cheong, Chu Qin, Lin Tao, Peng Zhang, Shangying Chen, Xian Zeng, Hongxia Liu, Giorgia Pastorin, Yuyang Jiang, Yu Zong Chen
Conventional ligand and receptor similarity methods have been extensively used for exposing pharmacological relationships and drug lead discovery. They may in some cases neglect minor relationships useful for target hopping particularly against the remote family members. To complement the conventional methods for capturing these minor relationships, we developed a new method that uses a SLARC (Simultaneous Ligand And Receptor Clustering) 2D map to simultaneously characterize the ligand structural and receptor binding-site sequence relationships of a receptor family...
July 11, 2017: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/28727763/loss-of-receptor-activity-modifying-protein-2-in-mice-causes-placental-dysfunction-and-alters-pth1r-regulation
#18
Mahita Kadmiel, Brooke C Matson, Scott T Espenschied, Patricia M Lenhart, Kathleen M Caron
Receptor activity-modifying protein 2 (Ramp2) is a single-pass transmembrane protein that heterodimerizes with several family B G-protein coupled receptors to alter their function. Ramp2 has been primarily characterized in association with calcitonin receptor-like receptor (Calcrl, CLR), forming the canonical receptor complex for the endocrine peptide adrenomedullin (Adm, AM). However, we previously demonstrated that Ramp2+/- female mice display a constellation of endocrine-related phenotypes that are distinct from those of Adm+/- and Calcrl+/- mice, implying that RAMP2 has physiological functions beyond its canonical complex...
2017: PloS One
https://www.readbyqxmd.com/read/28727179/overexpression-of-g%C3%AE-s-in-murine-osteoblasts-in-vivo-leads-to-increased-bone-mass-and-decreased-bone-quality
#19
Lucia Zhang, Kim S Sugamori, Colin Claridge, Ariana Dela Cruz, Marc D Grynpas, Jane Mitchell
GαS is a heterotrimeric G protein that transduces signals from activated G protein-coupled receptors on the cell surface to stimulate adenylyl cyclase/cyclic AMP signaling. GαS plays a central role in mediating numerous growth and maintenance processes including osteogenesis and bone turnover. Decreased GαS expression or activating mutations in GαS both affect bone suggesting that modulating GαS protein levels may be important for bone health and development. To examine the effects of increased osteoblastic GαS expression on bone development in vivo, we generated transgenic mice with GαS over-expression in osteoblasts (HOM-Gs mice) driven by the 3...
July 20, 2017: Journal of Bone and Mineral Research: the Official Journal of the American Society for Bone and Mineral Research
https://www.readbyqxmd.com/read/28727112/effect-of-in-ovo-feeding-of-l-arginine-on-the-hatchability-growth-performance-gastrointestinal-hormones-and-jejunal-digestive-and-absorptive-capacity-of-posthatch-broilers
#20
T Gao, M Zhao, L Zhang, J Li, L Yu, P Lv, F Gao, G Zhou
This study was conducted to investigate the effects of in ovo feeding (IOF) of Arg solution on the hatchability, growth performance, gastrointestinal hormones, serum AA, activities of digestive enzymes, and mRNA expressions of sensing receptors and nutrient transporters in the jejunum of posthatch broilers. One thousand two hundred embryonated eggs with similar weight were randomly allocated to 5 groups consisting of 8 replicates of 40 eggs each. The 5 treatments were arranged as a noninjected control, a diluent-injected (0...
July 2017: Journal of Animal Science
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