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G protein coupled receptor

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https://www.readbyqxmd.com/read/27933606/relaxin-like-peptides-in-male-reproduction-a-human-perspective
#1
REVIEW
Richard Ivell, Alexander I Agoulnik, Ravinder Anand-Ivell
The relaxin family of peptide hormones and their cognate G-protein coupled receptors are becoming physiologically well characterized in the cardiovascular system and particularly in female reproductive processes. Much less is known about the physiology and pharmacology of these peptides in male reproduction, particularly as regards the human. H2-relaxin is involved in prostate function and growth, while INSL3 is a major product of the testicular Leydig cells and in the adult appears to modulate steroidogenesis and germ cell survival...
December 9, 2016: British Journal of Pharmacology
https://www.readbyqxmd.com/read/27932497/intraflagellar-transport-a-complex-mediates-ciliary-entry-as-well-as-retrograde-trafficking-of-ciliary-g-protein-coupled-receptors
#2
Tomoaki Hirano, Yohei Katoh, Kazuhisa Nakayama
Cilia serve as cellular antennae, where proteins involved in sensory and developmental signaling, including G protein-coupled receptors (GPCRs), are specifically localized. Intraflagellar transport (IFT)-A and -B complexes are known to mediate retrograde and anterograde ciliary protein trafficking, respectively. By the visible immunoprecipitation assay to detect protein-protein interactions, we here demonstrated that the IFT-A complex is divided into the core subcomplex, which is composed of IFT122/IFT140/IFT144 and is associated with TULP3, and the peripheral subcomplex composed of IFT43/IFT121/IFT139, where IFT139 is most distally located...
December 8, 2016: Molecular Biology of the Cell
https://www.readbyqxmd.com/read/27930943/analyzing-biased-responses-of-gpcr-ligands
#3
REVIEW
Besma Benredjem, Paul Dallaire, Graciela Pineyro
G protein-coupled receptors (GPCRs) are valuable targets for drug discovery. They exist in interconverting states differentially stabilized by diverse signaling partners. A ligand's capacity to distinguish among receptors associated with different partners is the basis of bias. This feature of GPCR signaling may allow development of ligands which specifically modulate effectors supporting desired actions. However, bias is time-dependent and cell-dependent such that in vitro bias may not predict bias displayed in vivo...
December 5, 2016: Current Opinion in Pharmacology
https://www.readbyqxmd.com/read/27930690/structural-mapping-and-functional-characterization-of-zebrafish-class-b-g-protein-coupled-receptor-gpcr-with-dual-ligand-selectivity-towards-glp-1-and-glucagon
#4
Deena A Oren, Yang Wei, Luce Skrabanek, Billy K C Chow, Thomas Mommsen, Svetlana Mojsov
GLP-1 and glucagon regulate glucose metabolism through a network of metabolic pathways initiated upon binding to their specific receptors that belong to class B G-protein coupled receptors (GPCRs). The therapeutic potential of glucagon is currently being evaluated, while GLP-1 is already used in the treatment of type 2 diabetes and obesity. Development of a second generation of GLP-1 based therapeutics depends on a molecular and structural understanding of the interactions between the GLP-1 receptor (GLP-1R) and its ligand GLP-1...
2016: PloS One
https://www.readbyqxmd.com/read/27927955/gpr126-adgrg6-has-schwann-cell-autonomous-and-nonautonomous-functions-in-peripheral-nerve-injury-and-repair
#5
Amit Mogha, Breanne L Harty, Dan Carlin, Jessica Joseph, Nicholas E Sanchez, Ueli Suter, Xianhua Piao, Valeria Cavalli, Kelly R Monk
: Schwann cells (SCs) are essential for proper peripheral nerve development and repair, although the mechanisms regulating these processes are incompletely understood. We previously showed that the adhesion G protein-coupled receptor Gpr126/Adgrg6 is essential for SC development and myelination. Interestingly, the expression of Gpr126 is maintained in adult SCs, suggestive of a function in the mature nerve. We therefore investigated the role of Gpr126 in nerve repair by studying an inducible SC-specific Gpr126 knock-out mouse model...
December 7, 2016: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/27927913/two-janus-cannabinoids-that-are-both-cb2-agonists-and-cb1-antagonists
#6
Amey Dhopeshwarkar, Natalia Murataeva, Alex Makriyannis, Alex Straiker, Ken P Mackie
The cannabinoid signaling system includes two G protein coupled receptors, CB1 and CB2. These receptors are widely distributed throughout the body and have each been implicated in many physiologically important processes. Though the cannabinoid signaling system has therapeutic potential, a persistent hurdle has remained the development of receptor-selective ligands. Because CB1 and CB2 are involved in diverse processes, it would be advantageous develop ligands that differentially engaging CB1 and CB2. We now report that GW405833 and AM1710, described as selective CB2 agonists, can antagonize CB1 receptor signaling...
December 7, 2016: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/27926858/g-protein-coupled-receptor-2-interacting-protein-1-controls-stalk-cell-fate-by-inhibiting-delta-like-4-notch1-signaling
#7
Syamantak Majumder, GuoFu Zhu, Xiangbin Xu, Sharon Senchanthisai, Dongyang Jiang, Hao Liu, Chao Xue, Xiaoqun Wang, Heidi Coia, Zhaoqiang Cui, Elaine M Smolock, Richard T Libby, Bradford C Berk, Jinjiang Pang
The spatiotemporal localization and expression of Dll4 are critical for sprouting angiogenesis. However, the related mechanisms are poorly understood. Here, we show that G-protein-coupled receptor-kinase interacting protein-1 (GIT1) is a robust endogenous inhibitor of Dll4-Notch1 signaling that specifically controls stalk cell fate. GIT1 is highly expressed in stalk cells but not in tip cells. GIT1 deficiency remarkably enhances Dll4 expression and Notch1 signaling, resulting in impaired retinal sprouting angiogenesis, which can be rescued by treatment with the Notch inhibitor or Dll4 neutralizing antibody...
December 6, 2016: Cell Reports
https://www.readbyqxmd.com/read/27926736/structure-of-cc-chemokine-receptor-2-with-orthosteric-and-allosteric-antagonists
#8
Yi Zheng, Ling Qin, Natalia V Ortiz Zacarías, Henk de Vries, Gye Won Han, Martin Gustavsson, Marta Dabros, Chunxia Zhao, Robert J Cherney, Percy Carter, Dean Stamos, Ruben Abagyan, Vadim Cherezov, Raymond C Stevens, Adriaan P IJzerman, Laura H Heitman, Andrew Tebben, Irina Kufareva, Tracy M Handel
CC chemokine receptor 2 (CCR2) is one of 19 members of the chemokine receptor subfamily of human class A G-protein-coupled receptors. CCR2 is expressed on monocytes, immature dendritic cells, and T-cell subpopulations, and mediates their migration towards endogenous CC chemokine ligands such as CCL2 (ref. 1). CCR2 and its ligands are implicated in numerous inflammatory and neurodegenerative diseases including atherosclerosis, multiple sclerosis, asthma, neuropathic pain, and diabetic nephropathy, as well as cancer...
December 7, 2016: Nature
https://www.readbyqxmd.com/read/27926729/intracellular-allosteric-antagonism-of-the-ccr9-receptor
#9
Christine Oswald, Mathieu Rappas, James Kean, Andrew S Doré, James C Errey, Kirstie Bennett, Francesca Deflorian, John A Christopher, Ali Jazayeri, Jonathan S Mason, Miles Congreve, Robert M Cooke, Fiona H Marshall
Chemokines and their G-protein-coupled receptors play a diverse role in immune defence by controlling the migration, activation and survival of immune cells. They are also involved in viral entry, tumour growth and metastasis and hence are important drug targets in a wide range of diseases. Despite very significant efforts by the pharmaceutical industry to develop drugs, with over 50 small-molecule drugs directed at the family entering clinical development, only two compounds have reached the market: maraviroc (CCR5) for HIV infection and plerixafor (CXCR4) for stem-cell mobilization...
December 7, 2016: Nature
https://www.readbyqxmd.com/read/27925669/biochemical-biophysical-and-cellular-techniques-to-study-the-guanine-nucleotide-exchange-factor-giv-girdin
#10
Pradipta Ghosh, Nicolas Aznar, Lee Swanson, I-Chung Lo, Inmaculada Lopez-Sanchez, Jason Ear, Cristina Rohena, Nicholas Kalogriopoulos, Linda Joosen, Ying Dunkel, Nina Sun, Peter Nguyen, Deepali Bhandari
Canonical signal transduction via heterotrimeric G proteins is spatiotemporally restricted, i.e., triggered exclusively at the plasma membrane, only by agonist activation of G protein-coupled receptors via a finite process that is terminated within a few hundred milliseconds. Recently, a rapidly emerging paradigm has revealed a noncanonical pathway for activation of heterotrimeric G proteins via the nonreceptor guanidine-nucleotide exchange factor, GIV/Girdin. Biochemical, biophysical, and functional studies evaluating this pathway have unraveled its unique properties and distinctive spatiotemporal features...
December 7, 2016: Current Protocols in Chemical Biology
https://www.readbyqxmd.com/read/27925416/association-of-a-gain-of-function-variant-in-lgr4-with-central-obesity
#11
Yaoyu Zou, Tinglu Ning, Juan Shi, Maopei Chen, Lin Ding, Ya Huang, Sophie Kauderer, Min Xu, Bin Cui, Yufang Bi, Simin Liu, Jie Hong, Ruixin Liu, Guang Ning, Jiqiu Wang
OBJECTIVE: To determine the relationship of the gain-of-function variant A750T in leucine-rich repeat containing G protein-coupled receptor 4 (LGR4) with central obesity and related metabolic phenotypes. METHODS: The LGR4 A750T (c.2248 G > A) variant was detected by Sanger sequencing in a discovery young population and a validation community-based population with obesity from eastern China. Fat indices determined by anthropometry and computed tomography scans and clinical biochemical measurements were collected for association analysis...
December 7, 2016: Obesity
https://www.readbyqxmd.com/read/27924846/structure-and-dynamics-of-a-constitutively-active-neurotensin-receptor
#12
Brian E Krumm, Sangbae Lee, Supriyo Bhattacharya, Istvan Botos, Courtney F White, Haijuan Du, Nagarajan Vaidehi, Reinhard Grisshammer
Many G protein-coupled receptors show constitutive activity, resulting in the production of a second messenger in the absence of an agonist; and naturally occurring constitutively active mutations in receptors have been implicated in diseases. To gain insight into mechanistic aspects of constitutive activity, we report here the 3.3 Å crystal structure of a constitutively active, agonist-bound neurotensin receptor (NTSR1) and molecular dynamics simulations of agonist-occupied and ligand-free receptor. Comparison with the structure of a NTSR1 variant that has little constitutive activity reveals uncoupling of the ligand-binding domain from conserved connector residues, that effect conformational changes during GPCR activation...
December 7, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27924567/the-nuclear-translocation-of-erk
#13
Denise A Berti, Rony Seger
The ERK1 and ERK2 (ERK1/2) cascade is a central signaling pathway activated by a wide variety of extracellular agents that transmit the messages of G Protein Coupled Receptors (GPCRs) and Receptor Tyrosine Kinases (RTKs). Being such a central pathway, the activity of the cascade is well regulated, including by dynamic changes of the subcellular localization of components of the ERK1/2 cascade. In resting cells, ERK1/2 are localized in the cytosol due to their interactions with different anchoring proteins. After stimulation, ERK1/2 are phosphorylated by MEK1/2 on their regulatory TEY motif, which permits their detachment from the anchoring proteins...
2017: Methods in Molecular Biology
https://www.readbyqxmd.com/read/27924341/structure-activity-relationship-of-novel-macrocyclic-biased-apelin-receptor-agonists
#14
Alexandre Murza, Xavier Sainsily, Jérôme Côté, Laurent Bruneau-Cossette, Élie Besserer-Offroy, Jean-Michel Longpré, Richard Leduc, Robert Dumaine, Olivier Lesur, Mannix Auger-Messier, Philippe Sarret, Éric Marsault
Apelin is the endogenous ligand for the G protein-coupled receptor APJ and exerts a key role in regulating cardiovascular functions. We report herein a novel series of macrocyclic analogues of apelin-13 in which the N- and C-terminal residues as well as the macrocycle composition were chemically modified to modulate structure-activity relationships on the APJ receptor. To this end, the binding affinity and the ability to engage G protein-dependent and G protein-independent signalling pathways of the resulting analogues were assessed...
December 7, 2016: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/27924271/amino-acid-residues-of-bitter-taste-receptor-tas2r16-that-determine-sensitivity-in-primates-to-%C3%AE-glycosides
#15
Hiroo Imai, Nami Suzuki-Hashido, Yoshiro Ishimaru, Takanobu Sakurai, Lijie Yin, Wenshi Pan, Masaji Ishiguro, Katsuyoshi Masuda, Keiko Abe, Takumi Misaka, Hirohisa Hirai
In mammals, bitter taste is mediated by TAS2Rs, which belong to the family of seven transmembrane G protein-coupled receptors. Since TAS2Rs are directly involved in the interaction between mammals and their dietary sources, it is likely that these genes evolved to reflect species-specific diets during mammalian evolution. Here, we analyzed the amino acids responsible for the difference in sensitivities of TAS2R16s of various primates using a cultured cell expression system. We found that the sensitivity of TAS2R16 varied due to several amino acid residues...
2016: Biophysics and Physicobiology
https://www.readbyqxmd.com/read/27923934/gpcrdb-an-information-system-for-g-protein-coupled-receptors
#16
Vignir Isberg, Stefan Mordalski, Christian Munk, Krzysztof Rataj, Kasper Harpsøe, Alexander S Hauser, Bas Vroling, Andrzej J Bojarski, Gert Vriend, David E Gloriam
No abstract text is available yet for this article.
December 6, 2016: Nucleic Acids Research
https://www.readbyqxmd.com/read/27923683/role-of-a-tachykinin-related-peptide-and-its-receptor-in-modulating-the-olfactory-sensitivity-in-the-oriental-fruit-fly-bactrocera-dorsalis-hendel
#17
Shun-Hua Gui, Hong-Bo Jiang, Li Xu, Yu-Xia Pei, Xiao-Qiang Liu, Guy Smagghe, Jin-Jun Wang
Insect tachykinin-related peptide (TRP), an ortholog of tachykinin in vertebrates, has been linked with regulation of diverse physiological processes, such as olfactory perception, locomotion, aggression, lipid metabolism and myotropic activity. In this study, we investigated the function of TRP (BdTRP) and its receptor (BdTRPR) in an important agricultural pest, the oriental fruit fly Bactrocera dorsalis. BdTRPR is a typical G-protein coupled-receptor (GPCR), and it could be activated by the putative BdTRP mature peptides with the effective concentrations (EC50) at the nanomolar range when expressed in Chinese hamster ovary cells...
December 3, 2016: Insect Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/27922692/mir-195-inhibits-the-proliferation-and-migration-of-chondrocytes-by-targeting-git1
#18
Yang-Lin Gu, Xiao-Xu Rong, Li-Ting Wen, Guo-Xing Zhu, Ming-Quan Qian
Previous studies have demonstrated that G-protein coupled receptor kinase interacting protein-1 (GIT1) and microRNAs (miRNAs) serve an important role in chondrocyte proliferation and migration. However, a limited number of studies conducted thus far have investigated the association between GIT1 and miRNAs. In the present study, putative miR‑195 binding sites in the GIT1 3'‑untranslated region were identified using common bioinformatic algorithms (miRanda, TargetScan, miRBase and miRWalk), and it was demonstrated that they may be involved in regulating GIT1 expression...
December 5, 2016: Molecular Medicine Reports
https://www.readbyqxmd.com/read/27922213/quantitative-maldi-ms-binding-assays-an-alternative-to-radiolabeling
#19
Maxime Rossato, Guillaume Miralles, Céline M'Kadmi, Mathieu Maingot, Muriel Amblard, Bernard Mouillac, Didier Gagne, Jean Martinez, Gilles Subra, Christine Enjalbal, Sonia Cantel
Radiolabeling of ligands is still the gold standard in the study of high-affinity receptor-ligand interactions. In an effort toward safer and simpler alternatives to the use of radioisotopes, we developed a quantitative and highly sensitive matrix-assisted laser desorption ionization mass spectrometry (MALDI-MS) method that relies on the use of chemically tagged ligands designed to be specifically detectable when present as traces in complex biological mixtures such as cellular lysates. This innovative technology allows easy, sensitive detection and accurate quantification of analytes at the sub-nanomolar level...
December 6, 2016: ChemMedChem
https://www.readbyqxmd.com/read/27920205/molecular-determinants-of-the-sensitivity-to-gq-11-phospholipase-c-dependent-gating-gd3-potentiation-and-ca2-permeability-in-the-transient-receptor-potential-canonical-type-5-trpc5-channel
#20
Xingjuan Chen, Wennan Li, Ashley M Riley, Mario Soliman, Saikat Chakraborty, Christopher W Stamatkin, Alexander G Obukhov
Transient Receptor Potential Canonical type 5 (TRPC5) is a Ca(2+) permeable cation channel that is highly expressed in the brain and is implicated in motor coordination, innate fear behavior, and seizure-genesis. The channel is activated by a signal downstream of the G-protein-coupled receptor (GPCR)-Gq/11-phospholipase C (PLC) pathway. In this study, we aimed to identify the molecular mechanisms involved in regulating TRPC5 activity. We report that R593, a residue located in the E4 loop near the TRPC5's extracellular Gd(3+)-binding site, is critical for conferring the sensitivity to GPCR-Gq/11-PLC-dependent gating on TRPC5...
December 5, 2016: Journal of Biological Chemistry
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