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G protein coupled receptor

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https://www.readbyqxmd.com/read/29786747/microrna-137-dysregulation-predisposes-to-osteoporotic-fracture-by-impeding-alp-activity-and-expression-via-suppression-of-leucine-rich-repeat-containing-g-protein-coupled-receptor-4-expression
#1
Xiangjun Liu, Xiaohui Xu
Osteoporosis is defined as a loss of bone mass and deterioration of its architecture resulting in bone weakness, which becomes prone to fracture. The objective of this study was to investigate the molecular mechanism by which miR-137 can reduce the risk of fracture in patients with osteoporosis. An online miRNA database and a luciferase reporter assay system were used to confirm that leucine-rich repeat-containing G-protein-coupled receptor 4 (LGR4) was the target of miR-137. Real-time PCR and western blot analysis were used to study miR-137 mRNA, the expression of LGR4 mRNA and protein among different groups or cells transfected with a scrambled miRNA control, miR-137 mimic, LGR4 siRNA and miR-137 inhibitor...
May 17, 2018: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/29786430/galaxygpcrloop-template-based-and-ab-initio-structure-sampling-of-the-extracellular-loops-of-g-protein-coupled-receptors
#2
Jonghun Won, Gyu Rie Lee, Hahnbeom Park, Chaok Seok
The second extracellular loops (ECL2s) of G-protein-coupled receptors (GPCRs) are often involved in GPCR functions, and their structures have important implications in drug discovery. However, structure prediction of ECL2 is difficult because of its long length and the structural diversity among different GPCRs. In this study, a new ECL2 conformational sampling method involving both template-based and ab initio sampling was developed. Inspired by observation of similar ECL2 structures of closely related GPCRs, a template-based sampling method employing loop structure templates selected from the structure database was developed...
May 22, 2018: Journal of Chemical Information and Modeling
https://www.readbyqxmd.com/read/29785433/the-immunomodulatory-activity-and-mechanism-of-docosahexenoic-acid-dha-on-immunosuppressive-mice-models
#3
Lirong Han, Huanna Lei, Ziwei Tian, Xu Wang, Dai Cheng, Chunling Wang
In this study, the immunomodulatory activity of docosahexaenoic acid (DHA) on the immunosuppressive BALB/c mice model and its molecular mechanism are elucidated. It was found that the weight indexes of the spleen and thymus were significantly increased by DHA (44.0 mg kg-1 and 88.0 mg kg-1) treatment in the prevention or cure groups. The result of macrophages showed that DHA (44.0 mg kg-1 and 88.0 mg kg-1) could promote the proliferation and phagocytosis activity of macrophages in the prevention or cure groups...
May 22, 2018: Food & Function
https://www.readbyqxmd.com/read/29782904/intracellular-s1p-levels-dictates-fate-of-different-regions-of-the-hippocampus-following-transient-global-cerebral-ischemia
#4
Sherif Rashad, Kuniyasu Niizuma, Daisuke Saigusa, Xiaobo Han, Mika Sato-Maeda, Ritsumi Saito, Akira Uruno, Miki Fujimura, Shuntaro Ikawa, Masayuki Yamamoto, Teiji Tominaga
Sphingosine-1-phosphate (S1P) is a sphingolipid molecule produced by the action of sphingosine kinases (SphK) on sphingosine. It possesses various intracellular functions through its interactions with intracellular proteins or via its action on five G-protein-coupled cell membrane receptors. Following transient global cerebral ischaemia (tGCI), only the CA1 subregion of the hippocampus undergoes apoptosis. In this study, we evaluated S1P levels and S1P processing enzyme expression in different hippocampal areas following tGCI in rats...
May 18, 2018: Neuroscience
https://www.readbyqxmd.com/read/29780684/a-new-insight-into-identification-of-in-silico-analysis-of-natural-compounds-targeting-gpr120
#5
Nagaraju Chinthakunta, Srinivasulu Cheemanapalli, Surekha Chinthakunta, C M Anuradha, Suresh Kumar Chitta
G-protein coupled receptor (GPR120) is an omega-3 fatty acid receptor that inhibits macrophage-induced tissue inflammation. Recent studies revealed GPR120 promotes colorectal carcinoma through modulation of VEGF, IL-8, PGE2, and NF-kB expression. However, three-dimensional structure of GPR120 is not yet available in Protein Data Bank (PDB). In the present study, we focused on a 3-D structural model of GPR120 has been constructed using homology modeling techniques. The structural quality of the predicted GPR120 model was verified using Procheck, Whatif, ProSA, and Verify 3D...
2018: Network Modeling and Analysis in Health Informatics and Bioinformatics
https://www.readbyqxmd.com/read/29780538/competition-between-li-and-na-in-sodium-transporters-and-receptors-which-na-binding-sites-are-therapeutic-li-targets
#6
Todor Dudev, Karine Mazmanian, Carmay Lim
Sodium (Na+ ) acts as an indispensable allosteric regulator of the activities of biologically important neurotransmitter transporters and G-protein coupled receptors (GPCRs), which comprise well-known drug targets for psychiatric disorders and addictive behavior. How selective these allosteric Na+ -binding sites are for the cognate cation over abiogenic Li+ , a first-line drug to treat bipolar disorder, is unclear. Here, we reveal how properties of the host protein and its binding cavity affect the outcome of the competition between Li+ and Na+ for allosteric binding sites in sodium transporters and receptors...
May 7, 2018: Chemical Science
https://www.readbyqxmd.com/read/29780163/heteromerization-of-%C3%AE-opioid-receptor-and-cholecystokinin-b-receptor-through-the-third-transmembrane-domain-of-the-%C3%AE-opioid-receptor-contributes-to-the-anti-opioid-effects-of-cholecystokinin-octapeptide
#7
Yin Yang, Qian Li, Qi-Hua He, Ji-Sheng Han, Li Su, You Wan
Activation of the cholecystokinin type B receptor (CCKBR) by cholecystokinin octapeptide (CCK-8) inhibits opioid analgesia. Chronic opiate treatment leads to an increase in the CCK-8 concentration and thus enhances the antagonism of CCK-8 against opioid analgesia; the underlying molecular mechanisms remain of great interest. In the present study, we validated the colocalization of the μ-opioid receptor (MOR) and CCKBR in pain signal transmission-related spinal cord dorsal horn and dorsal root ganglion neurons of rats...
May 21, 2018: Experimental & Molecular Medicine
https://www.readbyqxmd.com/read/29779578/mouse-models-for-the-analysis-of-gonadotropin-secretion-and-action
#8
REVIEW
Sara Babcock Gilbert, Allyson K Roof, T Rajendra Kumar
Gonadotropins are pituitary gonadotrope-derived glycoprotein hormones. They act by binding to G-protein coupled receptors on gonads. Gonadotropins play critical roles in reproduction by regulating both gametogenesis and steroidogenesis. Although biochemical and physiological studies provided a wealth of knowledge, gene manipulation techniques using novel mouse models gave new insights into gonadotropin synthesis, secretion and action. Both gain of function and loss of function mouse models for understanding gonadotropin action in a whole animal context have already been generated...
June 2018: Best Practice & Research. Clinical Endocrinology & Metabolism
https://www.readbyqxmd.com/read/29777575/lgr5-promotes-epithelial-ovarian-cancer-proliferation-metastasis-and-epithelial-mesenchymal-transition-through-the-notch1-signaling-pathway
#9
Wenxue Liu, Jing Zhang, Xupei Gan, Fangqian Shen, Xiaoming Yang, Na Du, Dandan Xia, Lei Liu, Lianqiao Qiao, Jufang Pan, Yunyan Sun, Xiaowei Xi
Leucine-rich repeat-containing G protein-coupled receptor 5 (LGR5) plays a vital role in the development of malignant tumors; however, its biological role and underlying mechanism in epithelial ovarian cancer (EOC) remain unclear. In this study, we aimed to investigate the biological function and clinical significance of LGR5 in human EOC. We evaluated LGR5 expression in EOC cell lines and tissues from ovarian cancer patients by qPCR, Western blotting, and immunohistochemical analysis. Cell proliferation, colony formation, transwell invasion assay, and scratch-wound assays were conducted to evaluate the expansion and invasion abilities of EOC cells...
May 18, 2018: Cancer Medicine
https://www.readbyqxmd.com/read/29777201/novel-smoothened-inhibitors-for-therapeutic-targeting-of-na%C3%A3-ve-and-drug-resistant-hedgehog-pathway-driven-cancers
#10
Qing-Rou Li, Hui Zhao, Xue-Sai Zhang, Henk Lang, Ker Yu
The G protein-coupled receptor (GPCR) smoothened (SMO) is a key signaling component of the sonic hedgehog (Hh) pathway and a clinically validated target for cancer treatment. The FDA-approved SMO inhibitors GDC-0449/Vismodegib and LDE225/Sonidegib demonstrated clinical antitumor efficacy. Nevertheless, relatively high percentage of treated patients would eventually develop acquired cross resistance to both drugs. Here, based on published structure and activity of GDC-0449 inhibitor class, we replaced its amide core with benzimidazole which retained bulk of the SMO-targeting activity as measured in our Hh/SMO/Gli1-reporter system...
May 18, 2018: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29777099/targeting-g-protein-coupled-receptor-signaling-at-the-g-protein-level-with-a-selective-nanobody-inhibitor
#11
Sahil Gulati, Hui Jin, Ikuo Masuho, Tivadar Orban, Yuan Cai, Els Pardon, Kirill A Martemyanov, Philip D Kiser, Phoebe L Stewart, Christopher P Ford, Jan Steyaert, Krzysztof Palczewski
G protein-coupled receptors (GPCRs) activate heterotrimeric G proteins by mediating a GDP to GTP exchange in the Gα subunit. This leads to dissociation of the heterotrimer into Gα-GTP and Gβγ dimer. The Gα-GTP and Gβγ dimer each regulate a variety of downstream pathways to control various aspects of human physiology. Dysregulated Gβγ-signaling is a central element of various neurological and cancer-related anomalies. However, Gβγ also serves as a negative regulator of Gα that is essential for G protein inactivation, and thus has the potential for numerous side effects when targeted therapeutically...
May 18, 2018: Nature Communications
https://www.readbyqxmd.com/read/29777058/gpr40-is-a-low-affinity-epoxyeicosatrienoic-acid-receptor-in-vascular-cells
#12
Sang Kyu Park, Anja Herrnreiter, Sandra L Pfister, Kathryn M Gauthier, Benjamin A Falck, John R Falck, William B Campbell
Endothelium-derived epoxyeicosatrienoic acids (EETs) have numerous vascular activities mediated by G protein--coupled receptors. Long-chain free fatty acids and EETs activate GPR40, prompting us to investigate the role of GPR40 in some vascular EET activities. 14,15-EET, 11,12-EET, arachidonic acid, and the GPR40 agonist GW9508 increase intracellular calcium concentrations in human GPR40-overexpressing HEK293 cells (EC50 = 0.58 ± 0.08 μM, 0.91 ± 0.08 μM, 3.9 ± 0.06 μM and 19 ± 0.37 nM, respectively)...
May 18, 2018: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/29776606/advances-in-membrane-trafficking-and-endosomal-signaling-of-g-protein-coupled-receptors
#13
Aylin C Hanyaloglu
The integration of GPCR signaling with membrane trafficking, as a single orchestrated system, is a theme increasingly evident with the growing reports of GPCR endosomal signaling. Once viewed as a mechanism to regulate cell surface heterotrimeric G protein signaling, the endocytic trafficking system is complex, highly compartmentalized, yet deeply interconnected with cell signaling. The organization of receptors into distinct plasma membrane signalosomes, biochemically distinct endosomal populations, endosomal microdomains, and its communication with distinct subcellular organelles such as the Golgi provides multiple unique signaling platforms that are critical for specifying receptor function physiologically and pathophysiologically...
2018: International Review of Cell and Molecular Biology
https://www.readbyqxmd.com/read/29776605/g-protein-coupled-receptor-resensitization-paradigms
#14
Manveen K Gupta, Maradumane L Mohan, Sathyamangla V Naga Prasad
Cellular responses to extracellular milieu/environment are driven by cell surface receptors that transmit the signal into the cells resulting in a synchronized and measured response. The ability to provide such exquisite responses to changes in external environment is mediated by the tight and yet, deliberate regulation of cell surface receptor function. In this regard, the seven transmembrane G protein-coupled receptors (GPCRs) are the largest family of cell surface receptors that regulate responses like cardiac contractility, vision, and olfaction including platelet activation...
2018: International Review of Cell and Molecular Biology
https://www.readbyqxmd.com/read/29776604/biased-agonism-antagonism-of-cardiovascular-gpcrs-for-heart-failure-therapy
#15
Victoria L Desimine, Katie A McCrink, Barbara M Parker, Shelby L Wertz, Jennifer Maning, Anastasios Lymperopoulos
G protein-coupled receptors (GPCRs) are among the most important drug targets currently used in clinic, including drugs for cardiovascular indications. We now know that, in addition to activating heterotrimeric G protein-dependent signaling pathways, GPCRs can also activate G protein-independent signaling, mainly via the βarrestins. The major role of βarrestin1 and -2, also known as arrestin2 or -3, respectively, is to desensitize GPCRs, i.e., uncoupled them from G proteins, and to subsequently internalize the receptor...
2018: International Review of Cell and Molecular Biology
https://www.readbyqxmd.com/read/29776603/regulation-of-g-protein-%C3%AE-%C3%AE-signaling
#16
Kanishka Senarath, Dinesh Kankanamge, Saroopa Samaradivakara, Kasun Ratnayake, Mithila Tennakoon, Ajith Karunarathne
Heterotrimeric guanine nucleotide-binding proteins (G proteins) deliver external signals to the cell interior, upon activation by the external signal stimulated G protein-coupled receptors (GPCRs).While the activated GPCRs control several pathways independently, activated G proteins control the vast majority of cellular and physiological functions, ranging from vision to cardiovascular homeostasis. Activated GPCRs dissociate GαGDPβγ heterotrimer into GαGTP and free Gβγ. Earlier, GαGTP was recognized as the primary signal transducer of the pathway and Gβγ as a passive signaling modality that facilitates the activity of Gα...
2018: International Review of Cell and Molecular Biology
https://www.readbyqxmd.com/read/29776602/blurring-boundaries-receptor-tyrosine-kinases-as-functional-g-protein-coupled-receptors
#17
Caitrin Crudden, Takashi Shibano, Dawei Song, Naida Suleymanova, Ada Girnita, Leonard Girnita
Receptor tyrosine kinases (RTKs) such as the insulin-like growth factor type 1 receptor (IGF-1R) control important biological activities as well as being involved in pathological processes. Due to their supportive nature in many human cancers they have long been considered attractive therapeutic targets. However, lessons learnt from early targeting trials highlight that a simple "active versus inactive" state model with classical kinase-only signaling is overly simplistic and does not describe reality...
2018: International Review of Cell and Molecular Biology
https://www.readbyqxmd.com/read/29775410/apelin-and-apj-orchestrate-complex-tissue-specific-control-of-cardiomyocyte-hypertrophy-and-contractility-in-the-hypertrophy-heart-failure-transition
#18
Victoria Nicole Parikh, Jing Liu, Ching Shang, Christopher Woods, Alex Chia Yu Chang, Mingming Zhao, David N Charo, Zachary Grunwald, Yong Huang, Kinya Seo, Philip S Tsao, Daniel Bernstein, Pilar Ruiz-Lozano, Thomas Quertermous, Euan A Ashley
The G protein coupled receptor APJ is a promising therapeutic target for heart failure. Constitutive deletion of APJ in the mouse is protective against the hypertrophy-heart failure transition via elimination of ligand-independent, β-arrestin dependent stretch transduction. However, the cellular origin of this stretch transduction and the details of its interaction with apelin signaling remain unknown. We generated mice with conditional elimination of APJ in the endothelium (APJendo-/- ) and myocardium (APJmyo-/- )...
May 18, 2018: American Journal of Physiology. Heart and Circulatory Physiology
https://www.readbyqxmd.com/read/29774633/a-simple-and-cost-efficient-adherent-culture-platform-for-human-gastric-primary-cells-as-an-in-vitro-model-for-helicobacter-pylori-infection
#19
Samaneh Saberi, Behshad Pournasr, Zahra Farzaneh, Maryam Esmaeili, Mahmoud Eshagh Hosseini, Hossein Baharvand, Marjan Mohammadi
BACKGROUND: Most two- dimensional in vitro models for studying host- H. pylori interactions rely on tumor-derived cell lines, which harbor malignant alterations. The recent development of human gastric organoids has overcome this limitation and provides a highly sophisticated, yet costly, short-term model for H. pylori infection, with restricted use in low-budget centers. METHOD: Tissue specimens from upper, middle, and lower stomachs of H. pylori-negative volunteers were collectively dispersed and cultured on mouse embryonic fibroblast (MEF) or collagen-coated plates...
May 17, 2018: Helicobacter
https://www.readbyqxmd.com/read/29773871/the-somatostatin-secreting-pancreatic-%C3%AE-cell-in-health-and-disease
#20
REVIEW
Patrik Rorsman, Mark O Huising
The somatostatin-secreting δ-cells comprise ~5% of the cells of the pancreatic islets. The δ-cells have complex morphology and might interact with many more islet cells than suggested by their low numbers. δ-Cells contain ATP-sensitive potassium channels, which open at low levels of glucose but close when glucose is elevated. This closure initiates membrane depolarization and electrical activity and increased somatostatin secretion. Factors released by neighbouring α-cells or β-cells amplify the glucose-induced effects on somatostatin secretion from δ-cells, which act locally within the islets as paracrine or autocrine inhibitors of insulin, glucagon and somatostatin secretion...
May 17, 2018: Nature Reviews. Endocrinology
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