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G protein coupled receptor

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https://www.readbyqxmd.com/read/28646160/loss-of-g%C3%AE-i-proteins-impairs-thymocyte-development-disrupts-t-cell-trafficking-and-leads-to-an-expanded-population-of-splenic-cd4-pd-1-cxcr5-t-cells
#1
Il-Young Hwang, Kathleen Harrison, Chung Park, John H Kehrl
Thymocyte and T cell trafficking relies on signals initiated by G-protein coupled receptors. To address the importance of the G-proteins Gαi2 and Gαi3 in thymocyte and T cell function, we developed several mouse models. Gαi2 deficiency in hematopoietic progenitors led to a small thymus, a double negative (DN)1/DN2 thymocyte transition block, and an accumulation of mature single positive (SP) thymocytes. Loss at the double positive (DP) stage of thymocyte development caused an increase in mature cells within the thymus...
June 23, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28645860/gper-agonist-dilates-mesenteric-arteries-via-pi3k-akt-enos-and-potassium-channels-in-both-sexes
#2
Pollyana Peixoto, Rosária Dias Aires, Virgínia Soares Lemos, Nazaré Souza Bissoli, Roger Lyrio Dos Santos
AIM: The action of oestrogen has traditionally been attributed to the activation of nuclear receptors (ERα and ERβ). A third receptor, the G protein-coupled oestrogen receptor (GPER), has been described as mediator of the rapid action of oestrogen. Based on the possible protective role of oestrogen in the cardiovascular system, the present study was designed to determine whether selective GPER activation induces relaxation of mesenteric resistance arteries in both sexes and which signalling pathways are involved...
June 20, 2017: Life Sciences
https://www.readbyqxmd.com/read/28645833/binding-kinetics-and-pathways-of-ligands-to-gpcrs
#3
REVIEW
Andrea Strasser, Hans-Joachim Wittmann, Roland Seifert
Previously, drugs were developed focusing on target affinity and selectivity. However, it is becoming evident that the drug-target residence time, related to the off-rate, is an important parameter for successful drug development. The residence time influences both the on-rate and overall effectiveness of drugs. Furthermore, ligand binding is now appreciated to be a multistep process because metastable and/or intermediate binding sites in the extracellular region have been identified. In this review, we summarize experimental ligand-binding data for G-protein-coupled receptors (GPCRs), and their binding pathways, analyzed by molecular dynamics (MD)...
June 20, 2017: Trends in Pharmacological Sciences
https://www.readbyqxmd.com/read/28645573/evidence-that-fetal-death-is-associated-with-placental-aging
#4
Kaushik Maiti, Zakia Sultana, Robert John Aitken, Jonathan Morris, Felicity Park, Bronwyn Andrew, Simon C Riley, Roger Smith
BACKGROUND: The risk of unexplained fetal death or stillbirth increases late in pregnancy suggesting that placental aging is an etiological factor. Aging is associated with oxidative damage to DNA, RNA and lipids. We hypothesized that placentas at more than 41 completed weeks of gestation (late-term) would show changes consistent with aging that would also be present in placentas associated with stillbirths. OBJECTIVE: We sought to determine whether placentas from late-term pregnancies and unexplained stillbirth show oxidative damage and other biochemical signs of aging...
June 20, 2017: American Journal of Obstetrics and Gynecology
https://www.readbyqxmd.com/read/28644022/hot-spot-residues-to-be-mutated-common-in-g-protein-coupled-receptors-of-class-a-identification-of-thermostabilizing-mutations-followed-by-determination-of-three-dimensional-structures-for-two-example-receptors
#5
Satoshi Yasuda, Yuta Kajiwara, Yosuke Toyoda, Kazushi Morimoto, Ryoji Suno, So Iwata, Takuya Kobayashi, Takeshi Murata, Masahiro Kinoshita
G protein-coupled receptors (GPCRs), which are indispensable to life and also implicated in a number of diseases, construct important drug targets. For the efficient structure-guided drug design, however, their structural stabilities must be enhanced. An amino-acid mutation is known to possibly lead to the enhancement, but currently available experimental and theoretical methods for identifying stabilizing mutations suffer such drawbacks as the incapability of exploring the whole mutational space with minor effort and the unambiguous physical origin of the enhanced or lowered stability...
June 23, 2017: Journal of Physical Chemistry. B
https://www.readbyqxmd.com/read/28643288/inhibitory-effect-of-fsllry-nh2-on-inflammatory-responses-induced-by-hydrogen-peroxide-in-hepg2-cells
#6
Yeon Joo Lee, Su Jin Kim, Kyoung Wan Kwon, Won Mo Lee, Wi Joon Im, Uy Dong Sohn
Proteinase activated receptor 2 (PAR2), which is localized in the GI tract, the respiratory system, and the kidney tubules is a G protein-coupled receptor associated with inflammation, metabolism, and disease. The aim of this study was to explore the role of PAR2 in hydrogen peroxide (H2O2)-induced HepG2 cells by using FSLLRY-NH2 a PAR2 antagonist. H2O2 treatment resulted in induction of PAR2 in esophageal, gastric, and liver cells, with the most robust response being in HepG2 cells. Furthermore, this effect was dose-dependent in HepG2 cells...
June 22, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28642345/evolution-of-nonspectral-rhodopsin-function-at-high-altitudes
#7
Gianni M Castiglione, Frances E Hauser, Brian S Liao, Nathan K Lujan, Alexander Van Nynatten, James M Morrow, Ryan K Schott, Nihar Bhattacharyya, Sarah Z Dungan, Belinda S W Chang
High-altitude environments present a range of biochemical and physiological challenges for organisms through decreases in oxygen, pressure, and temperature relative to lowland habitats. Protein-level adaptations to hypoxic high-altitude conditions have been identified in multiple terrestrial endotherms; however, comparable adaptations in aquatic ectotherms, such as fishes, have not been as extensively characterized. In enzyme proteins, cold adaptation is attained through functional trade-offs between stability and activity, often mediated by substitutions outside the active site...
June 22, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28642167/mice-lacking-gpr37-exhibit-decreased-expression-of-the-myelin-associated-glycoprotein-mag-and-increased-susceptibility-to-demyelination
#8
Brilee M Smith, Michelle M Giddens, Jessica Neil, Sharon Owino, TrangKimberly T Nguyen, Duc Duong, Fengqiao Li, Randy A Hall
GPR37 is an orphan G protein-coupled receptor that is predominantly expressed in the brain and found at particularly high levels in oligodendrocytes. GPR37 has been shown to exert effects on oligodendrocyte differentiation and myelination during development, but the molecular basis of these actions is incompletely understood and moreover nothing is known about the potential role(s) of this receptor under demyelinating conditions. To shed light on the fundamental biology of GPR37, we performed proteomic studies comparing protein expression levels in the brains of mice lacking GPR37 and its close relative GPR37-like 1 (GPR37L1)...
June 19, 2017: Neuroscience
https://www.readbyqxmd.com/read/28642113/paralog-divergent-features-may-help-reduce-off-target-effects-of-drugs-hints-from-glucagon-subfamily-analysis
#9
Zhining Sa, Jingqi Zhou, Yangyun Zou, Zhixi Su, Xun Gu
Side effects from targeted drugs remain a serious concern. One reason is the nonselective binding of a drug to unintended proteins such as its paralogs, which are highly homologous in sequences and have similar structures and drug-binding pockets. To identify targetable differences between paralogs, we analyzed two types (type-I and type-II) of functional divergence between two paralogs in the known target protein receptor family G-protein coupled receptors (GPCRs) at the amino acid level. Paralogous protein receptors in glucagon-like subfamily, glucagon receptor (GCGR) and glucagon-like peptide-1 receptor (GLP-1R), exhibit divergence in ligands and are clinically validated drug targets for type 2 diabetes...
June 19, 2017: Genomics, Proteomics & Bioinformatics
https://www.readbyqxmd.com/read/28641070/elmo-proteins-transduce-g-protein-coupled-receptor-signal-to-control-reorganization-of-actin-cytoskeleton-in-chemotaxis-of-eukaryotic-cells
#10
Xuehua Xu, Tian Jin
Chemotaxis, which is chemoattractant-guided directional cell migration, plays major roles in recruitment of neutrophils, the metastasis of cancer cells, and the development of the model organism Dictyostelium discoideum. These cells share remarkable similarities in the signaling pathways by which they control chemotaxis. They all use a G protein-coupled receptor (GPCR)-mediated signal transduction pathway to sense the chemotactic gradient to guide cell migration. Diverse chemokines activate Rac through conserved GPCR signaling pathways...
June 22, 2017: Small GTPases
https://www.readbyqxmd.com/read/28639411/mapping-the-allosteric-sites-of-the-a2a-adenosine-receptor
#11
Alisha D Caliman, Yinglong Miao, J Andrew McCammon
The A2A adenosine receptor (A2A AR) is a G protein-coupled receptor that is pharmacologically targeted for the treatment of inflammation, sepsis, cancer, neuro-degeneration, and Parkinson's disease. Recently, we applied long-timescale molecular dynamics simulations on two ligand-free receptor conformations, starting from the agonist-bound (PDB ID:3QAK) and antagonist-bound (PDB ID:3EML) X-ray structures. This analysis revealed four distinct conformers of the A2A AR: the active, intermediate 1, intermediate 2, and inactive...
June 22, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28637808/dmt-efficiently-inhibits-hepatic-gluconeogenesis-involving-g%C3%AE-q-signaling-pathway
#12
Ting-Ting Zhou, Fei Ma, Xiao-Fan Shi, Xin Xu, Te Du, Xiao-Dan Guo, Gai-Hong Wang, Liang Yu, Vatcharin Rukachaisirikul, Li-Hong Hu, Jing Chen, Xu Shen
Type 2 diabetes mellitus (T2DM) is a chronic metabolic disease with complicated pathogenesis, and targeting gluconeogenesis inhibition is a promising strategy for anti-diabetic drug discovery. G protein-coupled receptors (GPCRs) are classified as distinct families by heterotrimeric G proteins, primarily including Gαs, Gαi and Gαq. Gαs-coupled GPCRs function potently in the regulation of hepatic gluconeogenesis through activating cyclic adenosine monophosphate (cAMP)/protein kinase A (PKA) pathway, and Gαi-coupled GPCRs exhibit inhibitory effect on adenylyl cyclase and reduce intracellular cAMP level...
June 21, 2017: Journal of Molecular Endocrinology
https://www.readbyqxmd.com/read/28637676/editorial-focus-on-balance-between-s-nitrosylation-and-denitrosylation-modulates-myoblast-proliferation-independently-of-soluble-guanylyl-cyclase-activation
#13
Hugo P Monteiro, Fernando T Ogata
Myogenesis involves a complex series of signaling events that will result in the formation of muscle fibers. The participation of nitric oxide (NO) in myogenesis is well established. NO generation in skeletal muscle comes from the neuronal isoform of the NO synthase (nNOS). NO signals through cGMP production and s-nitrosylation of proteins in skeletal muscle. In skeletal muscle, nNOS interacts with two domains of caveolin-3 which is part of caveolae, and forms a signaling complex through additional interactions with Src kinase and p21Ras...
June 21, 2017: American Journal of Physiology. Cell Physiology
https://www.readbyqxmd.com/read/28636986/the-positivity-of-g-protein-coupled-receptor-30-gpr-30-an-alternative-estrogen-receptor-is-not-different-between-type-1-and-type-2-endometrial-cancer
#14
Jiayi Wan, Yongxiang Yin, Min Zhao, Fang Shen, Miaoxin Chen, Qi Chen
It is well-known that the clinical outcomes are different between type 1 (estrogen dependent) and type 2 (estrogen independent) endometrial cancer. Studies have suggested that the estrogen receptor (ER) is positively correlated with endometrial cancer survival, however we previously reported that there is no difference in the positivity of ER as well as sex hormone levels between subtypes of cancer. G-protein-coupled receptor-30 (GPR 30), an alternative estrogen receptor has been suggested to be negatively correlated with clinical outcomes of endometrial cancer...
June 17, 2017: Oncotarget
https://www.readbyqxmd.com/read/28635314/fluorescent-labeled-bioconjugates-of-the-opioid-peptides-biphalin-and-dpdpe-incorporating-fluorescein-maleimide-linkers
#15
Azzurra Stefanucci, Wei Lei, Victor J Hruby, Giorgia Macedonio, Grazia Luisi, Simone Carradori, John M Streicher, Adriano Mollica
AIM: The conjugation of fluorescent labels to opioid peptides is an extremely challenging task, which needs to be overcome to create new classes of probes for biological assays. MATERIALS & METHODS: Three opioid peptide analogs of biphalin and [D-Pen2,5]-Enkephalin (DPDPE) containing a fluorescein-maleimide motif were synthesized. RESULTS & DISCUSSION: The biphalin analog 17 binds to opioid receptors with Ki(μ) = 530 ± 90 nM and Ki(δ) = 69...
June 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28634819/establishment-of-a-tagged-variant-of-lgr4-receptor-suitable-for-functional-and-expression-studies-in-the-mouse
#16
Vitezslav Kriz, Michaela Krausova, Petra Buresova, Jan Dobes, Dusan Hrckulak, Olga Babosova, Jiri Svec, Vladimir Korinek
Leucine-rich repeat-containing G-protein-coupled receptor 4 (LGR4) is produced in a broad spectrum of mouse embryonic and adult tissues and its deficiency results in embryonal or perinatal lethality. The LGR4 function was mainly related to its potentiation of canonical Wnt signaling; however, several recent studies associate LGR4 with additional signaling pathways. To obtain a suitable tool for studying the signaling properties of Lgr4, we generated a tagged variant of the Lgr4 receptor using gene targeting in the mouse oocyte...
June 20, 2017: Transgenic Research
https://www.readbyqxmd.com/read/28634209/genetic-evidence-that-%C3%AE-arrestins-are-dispensable-for-the-initiation-of-%C3%AE-2-adrenergic-receptor-signaling-to-erk
#17
Morgan O'Hayre, Kelsie Eichel, Silvia Avino, Xuefeng Zhao, Dana J Steffen, Xiaodong Feng, Kouki Kawakami, Junken Aoki, Karen Messer, Roger Sunahara, Asuka Inoue, Mark von Zastrow, J Silvio Gutkind
The β2-adrenergic receptor (β2AR) has provided a paradigm to elucidate how G protein-coupled receptors (GPCRs) control intracellular signaling, including the discovery that β-arrestins, which bind to ligand-activated GPCRs, are central for GPCR function. We used genome editing, conditional gene deletion, and small interfering RNAs (siRNAs) to determine the roles of β-arrestin 1 (β-arr1) and β-arr2 in β2AR internalization, trafficking, and signaling to ERK. We found that only β-arr2 was essential for β2AR internalization...
June 20, 2017: Science Signaling
https://www.readbyqxmd.com/read/28632878/identification-of-novel-g-protein-coupled-receptor-143-ligands-as-pharmacologic-tools-for-investigating-x-linked-ocular-albinism
#18
Elisabetta De Filippo, Prashiela Manga, Anke C Schiedel
Purpose: GPR143 regulates melanosome biogenesis and organelle size in pigment cells. The mechanisms underlying receptor function remain unclear. G protein-coupled receptors (GPCRs) are excellent pharmacologic targets; thus, we developed and applied a screening approach to identify potential GPR143 ligands and chemical modulators. Methods: GPR143 interacts with β-arrestin; we therefore established a β-arrestin recruitment assay to screen for compounds that modulate activity...
June 1, 2017: Investigative Ophthalmology & Visual Science
https://www.readbyqxmd.com/read/28631980/orexin-research-patent-news-from-2016
#19
Christoph Boss, Catherine Roch
The orexin (hypocretin) system consists of two G-protein-coupled receptors, orexin 1 (Ox1) and orexin 2 (Ox2) and two endogenous peptidic ligands, orexin A (OxA) and orexin B (OxB). It is evolutionarily highly conserved. In the brain, it is involved in the promotion of wakefulness under motivational circumstances as well as in anxiety and addictive disorders. In addition, its activation via the Ox1 receptor triggers apoptosis in several cancer cell lines. Dual orexin receptor antagonists (DORAs) such as suvorexant are successfully used to treat primary insomnia...
June 20, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28631012/rapid-preparation-of-bioluminescent-tracers-for-relaxin-family-peptides-using-sortase-catalysed-ligation
#20
Jia-Hui Wang, Xiao-Xia Shao, Meng-Jun Hu, Dian Wei, Wei-Han Nie, Ya-Li Liu, Zeng-Guang Xu, Zhan-Yun Guo
Relaxin family is a group of peptide hormones with a variety of biological functions by activating G protein-coupled receptors RXFP1-4. We recently developed bioluminescent tracers for their receptor-binding assays by chemical conjugation with the ultrasensitive NanoLuc reporter. To simplify preparation of the bioluminescent tracers, in the present study, we established a sortase-catalysed ligation approach using the chimeric R3/I5 as a model. Following catalysis by recombinant sortase A, a NanoLuc reporter carrying the LPETG sortase recognition motif at the C-terminus was efficiently ligated to an R3/I5 peptide carrying four successive Gly residues at the A-chain N-terminus, via the formation of a peptide bond between the C-terminal LPET sequence of NanoLuc and the A-chain N-terminal Gly residue of R3/I5...
June 19, 2017: Amino Acids
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