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https://www.readbyqxmd.com/read/28239939/combining-the-gpr40-agonist-fasiglifam-with-sitagliptin-improves-glycemic-control-in-patients-with-type-2-diabetes-with-or-without-metformin-a-randomized-12-week-trial
#1
Xuejun V Peng, John F Marcinak, Marsha G Raanan, Charlie Cao
AIMS: To evaluate the efficacy and safety of fasiglifam, an orally active G protein-coupled receptor 40 agonist, in combination with the dipeptidyl peptidase-4 inhibitor sitagliptin, in patients with type 2 diabetes inadequately controlled with diet/exercise (± metformin). METHODS: In this randomized, double-blind, phase II study, 368 patients received once-daily placebo, sitagliptin 100 mg, fasiglifam 25 or 50 mg, or the combination of sitagliptin 100 mg plus fasiglifam 25 or 50 mg...
February 27, 2017: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/28239762/-1-h-13-c-and-15-n-backbone-chemical-shift-assignments-of-camelid-single-domain-antibodies-against-active-state-%C3%A2%C2%B5-opioid-receptor
#2
Remy Sounier, Yinshan Yang, Joanna Hagelberger, Sébastien Granier, Hélène Déméné
Nanobodies are single chain antibodies that have become a highly valuable and versatile tool for biomolecular and therapeutic research. One application field is the stabilization of active states of flexible proteins, among which G-protein coupled receptors represent a very important class of membrane proteins. Here we present the backbone and side-chain assignment of the (1)H, (13)C and (15)N resonances of Nb33 and Nb39, two nanobodies that recognize and stabilize the µ-opioid receptor to opioids in its active agonist-bound conformation...
February 26, 2017: Biomolecular NMR Assignments
https://www.readbyqxmd.com/read/28239424/non-covalent-interactions-in-controlling-ph-responsive-behaviors-of-self-assembled-nanosystems
#3
Yang Li, Zhaohui Wang, Qi Wei, Min Luo, Gang Huang, Baran D Sumer, Jinming Gao
Self-assembly and associated dynamic and reversible non-covalent interactions are the basis of protein biochemistry (e.g., protein folding) and development of sophisticated nanomaterial systems that can respond to and amplify biological signals. In this study, we report a systematic investigation of non-covalent interactions that affect the pH responsive behaviors and resulting supramolecular self-assembly of a series of ultra-pH sensitive (UPS) block copolymers. Increase of hydrophobic and π-π stacking interactions led to the decrease of pKa values...
October 14, 2016: Polymer Chemistry
https://www.readbyqxmd.com/read/28239340/dopamine-induced-changes-in-g%C3%AE-olf-protein-levels-in-striatonigral-and-striatopallidal-medium-spiny-neurons-underlie-the-genesis-of-l-dopa-induced-dyskinesia-in-parkinsonian-mice
#4
Ryoma Morigaki, Shinya Okita, Satoshi Goto
The dopamine precursor, l-3,4-dihydroxyphenylalanine (l-DOPA), exerts powerful therapeutic effects but eventually generates l-DOPA-induced dyskinesia (LID) in patients with Parkinson's disease (PD). LID has a close link with deregulation of striatal dopamine/cAMP signaling, which is integrated by medium spiny neurons (MSNs). Olfactory type G-protein α subunit (Gαolf), a stimulatory GTP-binding protein encoded by the GNAL gene, is highly concentrated in the striatum, where it positively couples with dopamine D1 (D1R) receptor and adenosine A2A receptor (A2AR) to increase intracellular cAMP levels in MSNs...
2017: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/28237701/regulator-of-g-protein-signaling-20-correlates-with-clinicopathological-features-and-prognosis-in-triple-negative-breast-cancer
#5
Quan Li, Wenxu Jin, Yefeng Cai, Fang Yang, Endong Chen, Danrong Ye, Qingxuan Wang, Xiaoxiang Guan
Triple-negative breast cancer (TNBC) is a highly aggressive tumor subtype lacking effective prognostic indicators or therapeutic targets. Therefore, finding a novel molecular biomarker for TNBC to achieve target therapy and predict its prognosis is crucial in preventing inappropriate treatment. Regulator of G-protein signaling (RGS) families of protein can negatively regulate signaling of heterotrimeric G proteins and are known to be upregulated in various tumors. In this study, we demonstrated that RGS20 was more highly expressed in TNBC tumor tissue than in adjacent normal tissue by analyzing the cancer genome atlas (TCGA) database...
February 22, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28237651/gip-3-30-nh2-is-a-potent-competitive-antagonist-of-the-gip-receptor-and-effectively-inhibits-gip-mediated-insulin-glucagon-and-somatostation-release
#6
A H Sparre-Ulrich, M N Gabe, L S Gasbjerg, C B Christiansen, B Svendsen, B Hartmann, J J Holst, M M Rosenkilde
Alternative processing of the precursor protein pro-GIP results in endogenously produced GIP(1-30)NH2, that by DPP-4 cleavage in vivo results in the metabolite GIP(3-30)NH2. We showed previously that GIP(3-30)NH2 is a high affinity antagonist of the human GIPR in vitro. Here we determine whether it is suitable for studies of GIP physiology in rats since effects of GIP agonists and antagonists are strictly species-dependent. Transiently transfected COS-7 cells were assessed for cAMP accumulation upon ligand stimulation or assayed in competition binding using human (125)I-GIP(1-42) as radioligand...
February 22, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28237334/functional-involvement-of-protein-kinase-c-rho-kinase-and-trpc3-decreases-while-plc-increases-with-advancement-of-pregnancy-in-mediating-oxytocin-induced-myometrial-contractions-in-water-buffaloes-bubalus-bubalis
#7
Abhishek Sharma, Udayraj P Nakade, Soumen Choudhury, Satish Kumar Garg
Present study unravels the involvement of different calcium signaling pathways in oxytocin-induced contractions in myometrium of non-pregnant and pregnant buffaloes during early and mid-pregnancy stages. Uteri of pregnant animals were more sensitive than of non-pregnant buffaloes. Phasic contractions and frequency of contraction significantly increased with advancement of pregnancy, while tonic contractions non-significantly and amplitude significantly decreased from six months pregnancy onward. Oxytocin produced concentration-dependent-contraction on isolated myometrial strips of pregnant and non-pregnant buffaloes and the dose response curves (DRCs) of oxytocin were significantly (P < 0...
April 1, 2017: Theriogenology
https://www.readbyqxmd.com/read/28236092/expression-and-functional-activity-of-bitter-taste-receptors-in-primary-renal-tubular-epithelial-cells-and-m-1-cells
#8
Jie Liang, Fuxue Chen, Fu Gu, Xin Liu, Feng Li, Dongshu Du
The kidney is essential in the maintenance of in vivo homeostasis by body fluid and electrolyte conservation and metabolic waste removal. Previously, we reported the expression of a novel G protein family (Tas2rs), which includes bitter taste receptors, in the kidney tubule system, including the nephrons and the collecting duct system. Bitter taste receptors could affect kidney function via Ca(2+) intake. Alkaloids such as phenylthiocarbamide stimulate these receptors and cause an increase in Ca(2+) intake...
February 24, 2017: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/28235863/normal-thymocyte-egress-t-cell-trafficking-and-cd4-t-cell-homeostasis-require-interactions-between-rgs-proteins-and-g%C3%AE-i2
#9
Il-Young Hwang, Chung Park, Kathleen Harrison, John H Kehrl
Adaptive immunity depends on mature thymocytes leaving the thymus to enter the bloodstream and the trafficking of T cells through lymphoid organs. Both of these require heterotrimeric Gαi protein signaling, whose intensity and duration are controlled by the regulator of G protein signaling (RGS) proteins. In this study, we show that RGS protein/Gαi2 interactions are essential for normal thymocyte egress, T cell trafficking, and homeostasis. Mature thymocytes with a Gαi2 mutation that disables RGS protein binding accumulated in the perivascular channels of thymic corticomedullary venules...
February 24, 2017: Journal of Immunology: Official Journal of the American Association of Immunologists
https://www.readbyqxmd.com/read/28235469/role-of-the-c-terminal-basic-amino-acids-and-the-lipid-anchor-of-the-g%C3%AE-2-protein-in-membrane-interactions-and-cell-localization
#10
Maria A Noguera-Salvà, Francisca Guardiola-Serrano, M Laura Martin, Amaia Marcilla-Etxenike, Martin O Bergo, Xavier Busquets, Pablo V Escribá
Heterotrimeric G proteins are peripheral membrane proteins that frequently localize to the plasma membrane where their presence in molar excess over G protein coupled receptors permits signal amplification. Their distribution is regulated by protein-lipid interactions, which has a clear influence on their activity. Gβγ dimer drives the interaction between G protein heterotrimers with cell membranes. We focused our study on the role of the C-terminal region of the Gγ2 protein in G protein interactions with cell membranes...
February 21, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28231302/bioinformatic-prediction-of-g-protein-coupled-receptor-encoding-sequences-from-the-transcriptome-of-the-foreleg-including-the-haller-s-organ-of-the-cattle-tick-rhipicephalus-australis
#11
Sergio Munoz, Felix D Guerrero, Anastasia Kellogg, Andrew M Heekin, Ming-Ying Leung
The cattle tick of Australia, Rhipicephalus australis, is a vector for microbial parasites that cause serious bovine diseases. The Haller's organ, located in the tick's forelegs, is crucial for host detection and mating. To facilitate the development of new technologies for better control of this agricultural pest, we aimed to sequence and annotate the transcriptome of the R. australis forelegs and associated tissues, including the Haller's organ. As G protein-coupled receptors (GPCRs) are an important family of eukaryotic proteins studied as pharmaceutical targets in humans, we prioritized the identification and classification of the GPCRs expressed in the foreleg tissues...
2017: PloS One
https://www.readbyqxmd.com/read/28230370/coarse-grained-prediction-of-peptide-binding-to-g-protein-coupled-receptors
#12
Bartholomé Delort, Pedro Renault, Landry Charlier, Florent Raussin, Jean Martinez, Nicolas Floquet
In this study, we used the Martini Coarse-Grained model with no applied restraints to predict the binding mode of some peptides to G-Protein Coupled Receptors (GPCRs). Both the Neurotensin-1 and the chemokine CXCR4 receptors were used as test cases. Their ligands, NTS8-13 and CVX15 peptides, respectively, were initially positioned in the surrounding water box. Using a protocol based on Replica Exchange Molecular Dynamics (REMD), both opening of the receptors and entry of the peptides into their dedicated pockets were observed on the μs time-scale...
February 23, 2017: Journal of Chemical Information and Modeling
https://www.readbyqxmd.com/read/28229982/circulating-free-dna-mutation-associated-with-response-of-targeted-therapy-in-human-epidermal-growth-factor-receptor-2-positive-metastatic-breast-cancer
#13
Qing Ye, Fan Qi, Li Bian, Shao-Hua Zhang, Tao Wang, Ze-Fei Jiang
BACKGROUND: The addition of anti-human epidermal growth factor receptor 2 (HER2)-targeted drugs, such as trastuzumab, lapatinib, and trastuzumab emtansine (T-DM1), to chemotherapy significantly improved prognosis of HER2-positive breast cancer patients. However, it was confused that metastatic patients vary in the response of targeted drug. Therefore, methods of accurately predicting drug response were really needed. To overcome the spatial and temporal limitations of biopsies, we aimed to develop a more sensitive and less invasive method of detecting mutations associated with anti-HER2 therapeutic response through circulating-free DNA (cfDNA)...
2017: Chinese Medical Journal
https://www.readbyqxmd.com/read/28229904/regulation-of-g-protein-coupled-receptor-signalling-underpinning-neurobiology-of-mood-disorders-and-depression
#14
Dimitris K Grammatopoulos
G-protein coupled receptors (GPCRs) have long been at the centre of investigations of the neurobiology of depression and mood disorders. Different facets of GPCR signalling pathways, including those controlling monoaminergic and neuropeptidergic hormonal systems are believed to be dysregulated in major depressive and bipolar disorders. Although these receptors are key molecular targets for a variety of therapeutic agents and continue to be the focus of intense pharmaceutical development, the molecular mechanisms activated by these GPCRs and underpin the pathological basis of mood disorders remain poorly understood...
February 13, 2017: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/28229253/the-biology-of-uveal-melanoma
#15
Adriana Amaro, Rosaria Gangemi, Francesca Piaggio, Giovanna Angelini, Gaia Barisione, Silvano Ferrini, Ulrich Pfeffer
Uveal melanoma (UM), a rare cancer of the eye, is distinct from cutaneous melanoma by its etiology, the mutation frequency and profile, and its clinical behavior including resistance to targeted therapy and immune checkpoint blockers. Primary disease is efficiently controlled by surgery or radiation therapy, but about half of UMs develop distant metastasis mostly to the liver. Survival of patients with metastasis is below 1 year and has not improved in decades. Recent years have brought a deep understanding of UM biology characterized by initiating mutations in the G proteins GNAQ and GNA11...
February 22, 2017: Cancer Metastasis Reviews
https://www.readbyqxmd.com/read/28228611/anti-diabetic-action-of-all-trans-retinoic-acid-and-the-orphan-g-protein-coupled-receptor-gprc5c-in-pancreatic-%C3%AE-cells
#16
Stefan Amisten, Israa Mohammad Al-Amily, Arvind Soni, Ross Hawkes, Patricio Atanes, Shanta Jean Persaud, Patrik Rorsman, Albert Salehi
Pancreatic islets express high levels of the orphan G-protein coupled receptor C5C (GPRC5C), the function of which remains to be established. Here we have examined the role of GPRC5C in the regulation of insulin secretion and β-cell survival and proliferation using human and mouse pancreatic islets. The expression of GPRC5C was analysed by RNA-sequencing, qPCR, western blotting and confocal microscopy. Insulin secretion and cell viability were determined by RIA and MTS assays, respectively. GPRC5C mRNA expression and protein level were reduced in the islets from type-2 diabetic donors...
February 22, 2017: Endocrine Journal
https://www.readbyqxmd.com/read/28228552/core-engagement-with-%C3%AE-arrestin-is-dispensable-for-agonist-induced-vasopressin-receptor-endocytosis-and-erk-activation
#17
Punita Kumari, Ashish Srivastava, Eshan Ghosh, Ravi Ranjan, Shalini Dogra, Prem N Yadav, Arun K Shukla
G Protein-Coupled Receptors (GPCRs) exhibit highly conserved activation and signaling mechanisms where agonist stimulation leads to coupling of heterotrimeric G proteins and generation of second messenger response. This is followed by receptor phosphorylation, primarily in the carboxyl-terminus but also in the cytoplasmic loops, and subsequent binding of arrestins. GPCRs typically recruit arrestins through two different set of interactions, one involving phosphorylated receptor tail and the other mediated by the receptor core...
February 22, 2017: Molecular Biology of the Cell
https://www.readbyqxmd.com/read/28228527/activation-mechanism-of-the-g-protein-coupled-sweet-receptor-heterodimer-with-sweeteners-and-allosteric-agonists
#18
Soo-Kyung Kim, Yalu Chen, Ravinder Abrol, William A Goddard, Brian Guthrie
The sweet taste in humans is mediated by the TAS1R2/TAS1R3 G protein-coupled receptor (GPCR), which belongs to the class C family that also includes the metabotropic glutamate and γ-aminobutyric acid receptors. We report here the predicted 3D structure of the full-length TAS1R2/TAS1R3 heterodimer, including the Venus Flytrap Domains (VFDs) [in the closed-open (co) active conformation], the cysteine-rich domains (CRDs), and the transmembrane domains (TMDs) at the TM56/TM56 interface. We observe that binding of agonists to VFD2 of TAS1R2 leads to major conformational changes to form a TM6/TM6 interface between TMDs of TAS1R2 and TAS1R3, which is consistent with the activation process observed biophysically on the metabotropic glutamate receptor 2 homodimer...
February 22, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28227365/integrated-quantification-based-on-confocal-imaging-cell-crowding-modulates-heterogeneity-in-gpcr-mediated-calcium-oscillation
#19
Jophin G Joseph, S Nanda, S Vennamalla, G Bhure, Ranjana Singh, Soumya Jana, Lopamudra Giri, Jophin G Joseph, S Nanda, S Vennamalla, G Bhure, Ranjana Singh, Soumya Jana, Lopamudra Giri, Soumya Jana, Lopamudra Giri, Jophin G Joseph, S Nanda, Ranjana Singh, G Bhure, S Vennamalla
Results from single cell imaging, facilitated by high resolution microscopy, have demonstrated cell-to-cell variability within the same cell population in contexts ranging from cell growth to cell migration. Recent studies suggest that such variability conveys important information about diseased states. However, manual analysis and interpretation of heterogeneous calcium oscillation based on time-lapsed images, as practiced today, is tedious, and essentially infeasible for large datasets. As a practical alternative, we present an integrated platform that includes calcium imaging using confocal microscope, algorithmic cell segmentation, and statistical analysis...
August 2016: Conference Proceedings: Annual International Conference of the IEEE Engineering in Medicine and Biology Society
https://www.readbyqxmd.com/read/28225778/gnb3-and-creb1-gene-polymorphisms-combined-with-negative-life-events-increase-susceptibility-to-major-depression-in-a-chinese-han-population
#20
Jingsong Ma, Lin Wang, Yanjie Yang, Zhengxue Qiao, Deyu Fang, Xiaohui Qiu, Xiuxian Yang, Xiongzhao Zhu, Jincai He, Hui Pan, Bo Ban, Yan Zhao, Hong Sui
BACKGROUND: Major depression (MD) is caused by a combination of genetic and environmental factors. In this study we investigated the interaction of variations in the G-protein beta 3 subunit (GNB3) and cAMP response element binding protein 1 (CREB1) genes with negative life events in the pathogenesis of MD. One GNB3 polymorphism (rs5443) and four CREB1 polymorphisms (rs2253206, rs2551941, rs6740584, rs11904814) were investigated based on known associations with MD. METHODS: 512 patients with MD and 513 control subjects were genotyped...
2017: PloS One
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