keyword
MENU ▼
Read by QxMD icon Read
search

V2R

keyword
https://www.readbyqxmd.com/read/28419717/ligand-recognition-properties-of-the-vasopressin-v2-receptor-studied-under-qsar-and-molecular-modeling-strategies
#1
Marlet Martínez-Archundia, Brenda Colín-Astudillo, L M Moreno-Vargas, G Ramírez-Galicia, R Garduño-Juárez, O Deeb, Martha C Contreras-Romo, A Quintanar-Stephano, Edgar Abarca-Rojano, José Correa-Basurto
The design of new drugs that target vasopressin 2 receptor (V2R) is of vital importance to develop new therapeutic alternatives to treat diseases such as heart failure, polycystic kidney disease, etc. To get structural insights related to V2R-ligand recognition, we have used a combined approach of docking, molecular dynamics simulations (MD) and quantitative structure-activity relationship (QSAR) to elucidate the detailed interaction of the V2R with 119 of its antagonists. The three-dimensional model of V2R was built by threading methods refining its structure through MD simulations upon which the 119 ligands were subjected to docking studies...
April 17, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28416805/a-new-inhibitor-of-the-%C3%AE-arrestin-ap2-endocytic-complex-reveals-interplay-between-gpcr-internalization-and-signalling
#2
Alexandre Beautrait, Justine S Paradis, Brandon Zimmerman, Jenna Giubilaro, Ljiljana Nikolajev, Sylvain Armando, Hiroyuki Kobayashi, Lama Yamani, Yoon Namkung, Franziska M Heydenreich, Etienne Khoury, Martin Audet, Philippe P Roux, Dmitry B Veprintsev, Stéphane A Laporte, Michel Bouvier
In addition to G protein-coupled receptor (GPCR) desensitization and endocytosis, β-arrestin recruitment to ligand-stimulated GPCRs promotes non-canonical signalling cascades. Distinguishing the respective contributions of β-arrestin recruitment to the receptor and β-arrestin-promoted endocytosis in propagating receptor signalling has been limited by the lack of selective analytical tools. Here, using a combination of virtual screening and cell-based assays, we have identified a small molecule that selectively inhibits the interaction between β-arrestin and the β2-adaptin subunit of the clathrin adaptor protein AP2 without interfering with the formation of receptor/β-arrestin complexes...
April 18, 2017: Nature Communications
https://www.readbyqxmd.com/read/28412033/antagonism-of-vasopressin-v2-receptor-improves-albuminuria-at-the-early-stage-of-diabetic-nephropathy-in-a-mouse-model-of-type-2-diabetes
#3
Ray El Boustany, Christopher Taveau, Catherine Chollet, Gilberto Velho, Lise Bankir, François Alhenc-Gelas, Ronan Roussel, Nadine Bouby
AIMS: Vasopressin is increased in diabetes and was shown to contribute to development of diabetic nephropathy through V2 receptor (V2R) activation in an experimental model of type 1 diabetes. The role of V2R in type 2 diabetes remains undocumented. This study addresses the issue in a mouse model of type 2 diabetes. METHODS: Male obese diabetic db/db mice were treated for 12weeks with a selective V2R antagonist (SR121463) and compared to non-treated db/db and non-diabetic db/m mice...
April 6, 2017: Journal of Diabetes and its Complications
https://www.readbyqxmd.com/read/28381458/protein-phosphatase-2c-pp2c-is-responsible-for-vp-induced-dephosphorylation-of-aqp2-serine-261
#4
Pui W Cheung, Lars Ueberdiek, Jack Day, Richard Bouley, Dennis Brown
AQP2 trafficking is regulated by phosphorylation and dephosphorylation of serine residues in the AQP2 c-terminus. Vasopressin (VP) binding to its receptor (V2R) leads to a cascade of events that result in the phosphorylation of serine 256 (S256), S264 and S269, but dephosphorylation of S261. To identify which phosphatase is responsible for VP-induced S261 dephosphorylation, we pretreated cells with different phosphatase inhibitors before VP stimulation. Only sanguinarine, a specific protein phosphatase 2C (PP2C) inhibitor, abolished VP-induced S261 dephosphorylation, but not inhibitors of PP1, PP2A (okadaic acid) or PP2B (cyclosporine)...
April 5, 2017: American Journal of Physiology. Renal Physiology
https://www.readbyqxmd.com/read/28326667/the-v2-receptor-antagonist-tolvaptan-raises-cytosolic-calcium-and-prevents-aqp2-trafficking-and-function-an-in-vitro-and-in-vivo-assessment
#5
Grazia Tamma, Annarita Di Mise, Marianna Ranieri, Ari Geller, Roberto Tamma, Alberta Zallone, Giovanna Valenti
Tolvaptan, a selective vasopressin V2 receptor antagonist, is a new generation diuretic. Its clinical efficacy is in principle due to impaired vasopressin-regulated water reabsorption via aquaporin-2 (AQP2). Nevertheless, no direct in vitro evidence that tolvaptan prevents AQP2-mediated water transport, nor that this pathway is targeted in vivo in patients with syndrome of inappropriate antidiuresis (SIAD) has been provided. The effects of tolvaptan on the vasopressin-cAMP/PKA signalling cascade were investigated in MDCK cells expressing endogenous V2R and in mouse kidney...
March 21, 2017: Journal of Cellular and Molecular Medicine
https://www.readbyqxmd.com/read/28258576/diabetes-insipidus
#6
H A Jenny Lu
Disruption of water and electrolyte balance is frequently encountered in clinical medicine. Regulating water metabolism is critically important. Diabetes insipidus (DI) presented with excessive water loss from the kidney is a major disorder of water metabolism. To understand the molecular and cellular mechanisms and pathophysiology of DI and rationales of clinical management of DI is important for both research and clinical practice. This chapter will first review various forms of DI focusing on central diabetes insipidus (CDI) and nephrogenic diabetes insipidus (NDI ) ...
2017: Advances in Experimental Medicine and Biology
https://www.readbyqxmd.com/read/28228552/core-engagement-with-%C3%AE-arrestin-is-dispensable-for-agonist-induced-vasopressin-receptor-endocytosis-and-erk-activation
#7
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 by which 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 sets of interactions, one involving phosphorylated receptor tail and the other mediated by the receptor core...
April 15, 2017: Molecular Biology of the Cell
https://www.readbyqxmd.com/read/28194370/peptide-agonists-of-vasopressin-v2-receptor-reduce-expression-of-neuroendocrine-markers-and-tumor-growth-in-human-lung-and-prostate-tumor-cells
#8
Marina Pifano, Juan Garona, Carla S Capobianco, Nazareno Gonzalez, Daniel F Alonso, Giselle V Ripoll
Neuroendocrine tumors (NETs) comprise a heterogeneous group of malignancies that express neuropeptides as synaptophysin, chromogranin A (CgA), and specific neuronal enolase (NSE), among others. Vasopressin (AVP) is a neuropeptide with an endocrine, paracrine, and autocrine effect in normal and pathological tissues. AVP receptors are present in human lung, breast, pancreatic, colorectal, and gastrointestinal tumors. While AVP V1 receptors are associated with stimulation of cellular proliferation, AVP V2 receptor (V2r) is related to antiproliferative effects...
2017: Frontiers in Oncology
https://www.readbyqxmd.com/read/28192441/cyclic-amp-regulates-postnatal-development-of-neural-and-behavioral-responses-to-nacl-in-rats
#9
Jie Qian, Shobha Mummalaneni, Tam-Hao T Phan, Gerard L Heck, John A DeSimone, David West, Sunila Mahavadi, Deanna Hojati, Karnam S Murthy, Mee-Ra Rhyu, Andrew I Spielman, Mehmet Hakan Özdener, Vijay Lyall
During postnatal development rats demonstrate an age-dependent increase in NaCl chorda tympani (CT) responses and the number of functional apical amiloride-sensitive epithelial Na+ channels (ENaCs) in salt sensing fungiform (FF) taste receptor cells (TRCs). Currently, the intracellular signals that regulate the postnatal development of salt taste have not been identified. We investigated the effect of cAMP, a downstream signal for arginine vasopressin (AVP) action, on the postnatal development of NaCl responses in 19-23 day old rats...
2017: PloS One
https://www.readbyqxmd.com/read/28179252/aquaporin-2-membrane-targeting-still-a-conundrum
#10
Emma Tina Bisgaard Olesen, Robert A Fenton
The targeting of the water channel aquaporin-2 (AQP2) to the apical plasma membrane of kidney collecting duct principal cells is regulated mainly by the antidiuretic peptide hormone arginine vasopressin (AVP). This process is of crucial importance for the maintenance of body water homeostasis. In this brief review we assess the role of cyclic adenosine monophosphate (cAMP) and discuss the emerging concept that V2R-mediated AQP2 trafficking is cAMP-independent.
February 8, 2017: American Journal of Physiology. Renal Physiology
https://www.readbyqxmd.com/read/28145450/development-of-a-human-vasopressin-v1a-receptor-antagonist-from-an-evolutionary-related-insect-neuropeptide
#11
Maria Giulia Di Giglio, Markus Muttenthaler, Kasper Harpsøe, Zita Liutkeviciute, Peter Keov, Thomas Eder, Thomas Rattei, Sarah Arrowsmith, Susan Wray, Ales Marek, Tomas Elbert, Paul F Alewood, David E Gloriam, Christian W Gruber
Characterisation of G protein-coupled receptors (GPCR) relies on the availability of a toolbox of ligands that selectively modulate different functional states of the receptors. To uncover such molecules, we explored a unique strategy for ligand discovery that takes advantage of the evolutionary conservation of the 600-million-year-old oxytocin/vasopressin signalling system. We isolated the insect oxytocin/vasopressin orthologue inotocin from the black garden ant (Lasius niger), identified and cloned its cognate receptor and determined its pharmacological properties on the insect and human oxytocin/vasopressin receptors...
February 1, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28116432/-partial-recovery-of-thermal-sensory-functions-in-skeletal-class-%C3%A2-patients-undergoing-orthognathic-surgery
#12
Xin-Yu Gu, Jing-Lu Zhang, Dong Lv, Wen-Jing Chen
PURPOSE: To clarify whether trigeminal somatosensory function will be changed after orthodontic treatment as well as after orthognathic surgery. METHODS: A series of 20 patients with a mean age of 20.9±1.74 years were recruited. Thermal quantitative sensory tests were conducted before orthodontic treatment (T0), before orthognathic surgery (T1), 2 months after orthognathic surgery (T2), and 6 months after orthognathic surgery (T3). The cold detection threshold (CDT), cold pain threshold (CPT), warm detection threshold (WDT) and heat pain threshold (HPT) were determined...
October 2016: Shanghai Kou Qiang Yi Xue, Shanghai Journal of Stomatology
https://www.readbyqxmd.com/read/28074292/reliability-of-the-nociceptive-blink-reflex-evoked-by-electrical-stimulation-of-the-trigeminal-nerve-in-humans
#13
Yuri Martins Costa, Lene Baad-Hansen, Leonardo Rigoldi Bonjardim, Paulo César Rodrigues Conti, Peter Svensson
OBJECTIVE: The nociceptive blink reflex (nBR) can be useful to investigate trigeminal nociceptive function. The aim of this study was to estimate the reliability of the nBR evoked by electrical stimulation of the three branches of the trigeminal nerve under the following conditions: over time (test-retest and intrarater reliability) and by two examiners (interrater reliability). MATERIALS AND METHODS: Twenty-one healthy participants were evaluated in two sessions (24 h apart)...
January 10, 2017: Clinical Oral Investigations
https://www.readbyqxmd.com/read/27990576/coordinated-shift-of-olfactory-amino-acid-responses-and-v2r-expression-to-an-amphibian-water-nose-during-metamorphosis
#14
Adnan S Syed, Alfredo Sansone, Thomas Hassenklöver, Ivan Manzini, Sigrun I Korsching
All olfactory receptors identified in teleost fish are expressed in a single sensory surface, whereas mammalian olfactory receptor gene families segregate into different olfactory organs, chief among them the main olfactory epithelium expressing ORs and TAARs, and the vomeronasal organ expressing V1Rs and V2Rs. A transitional stage is embodied by amphibians, with their vomeronasal organ expressing more 'modern', later diverging V2Rs, whereas more 'ancient', earlier diverging V2Rs are expressed in the main olfactory epithelium...
December 18, 2016: Cellular and Molecular Life Sciences: CMLS
https://www.readbyqxmd.com/read/27912243/vomeronasal-receptors-in-vertebrates-and-the-evolution-of-pheromone-detection
#15
Liliana Silva, Agostinho Antunes
Pheromones were identified as chemical signals used for intraspecific communication in insects (e.g., sexual attraction) in the 1950s. However, only almost 40 years later the vomeronasal receptors type-1 (V1R) and type-2 (V2R) were identified, usually associated with the presence of a vomeronasal organ (VNO). VRs are widespread in amphibians, reptiles, and mammals, but birds lost the VNO. Similarly, fishes lack VRs and a VNO but can still detect pheromones, instead using the olfactory receptors related to class A and class C G protein-coupled receptors...
February 8, 2017: Annual Review of Animal Biosciences
https://www.readbyqxmd.com/read/27689822/transcriptomic-profiles-of-the-upper-olfactory-rosette-in-cultured-and-wild-senegalese-sole-solea-senegalensis-males
#16
E Fatsini, R Bautista, M Manchado, N J Duncan
The aims of this study were the characterization of the upper olfactory epithelium of cultured and wild Senegalese sole mature males at histological and transcriptomic (using RNA-Seq) level. No significant differences in tissue structure, cell types and cellular distribution pattern (olfactory sensory neurons) were identified between cultured and wild specimens. Deep transcriptomic analysis showed 2387 transcripts were differentially expressed between cultured and wild groups. A detailed analysis identified the differentially expressed transcripts included some olfactory receptors (OR, TAAR and V2R-like) and transcripts related with the control of reproduction such as the brain aromatase cytochrome P450 and tachykinin-3...
September 20, 2016: Comparative Biochemistry and Physiology. Part D, Genomics & Proteomics
https://www.readbyqxmd.com/read/27684435/in-depth-physiological-analysis-of-defined-cell-populations-in-acute-tissue-slices-of-the-mouse-vomeronasal-organ
#17
Tobias Ackels, Daniela R Drose, Marc Spehr
In most mammals, the vomeronasal organ (VNO) is a chemosensory structure that detects both hetero- and conspecific social cues. Vomeronasal sensory neurons (VSNs) express a specific type of G protein-coupled receptor (GPCR) from at least three different chemoreceptor gene families allowing sensitive and specific detection of chemosensory cues. These families comprise the V1r and V2r gene families as well as the formyl peptide receptor (FPR)-related sequence (Fpr-rs) family of putative chemoreceptor genes. In order to understand the physiology of vomeronasal receptor-ligand interactions and downstream signaling, it is essential to identify the biophysical properties inherent to each specific class of VSNs...
2016: Journal of Visualized Experiments: JoVE
https://www.readbyqxmd.com/read/27605630/dosimetric-impact-of-an-air-passage-on-intraluminal-brachytherapy-for-bronchus-cancer
#18
Hiroyuki Okamoto, Akihisa Wakita, Satoshi Nakamura, Shie Nishioka, Ako Aikawa, Toru Kato, Yoshihisa Abe, Kazuma Kobayashi, Koji Inaba, Naoya Murakami, Jun Itami
The brachytherapy dose calculations used in treatment planning systems (TPSs) have conventionally been performed assuming homogeneous water. Using measurements and a Monte Carlo simulation, we evaluated the dosimetric impact of an air passage on brachytherapy for bronchus cancer. To obtain the geometrical characteristics of an air passage, we analyzed the anatomical information from CT images of patients who underwent intraluminal brachytherapy using a high-dose-rate (192)Ir source (MicroSelectron V2r®, Nucletron)...
November 2016: Journal of Radiation Research
https://www.readbyqxmd.com/read/27601473/analysis-of-the-v2-vasopressin-receptor-v2r-mutations-causing-partial-nephrogenic-diabetes-insipidus-highlights-a-sustainable-signaling-by-a-non-peptide-v2r-agonist
#19
Noriko Makita, Tomohiko Sato, Yuki Yajima-Shoji, Junichiro Sato, Katsunori Manaka, Makiko Eda-Hashimoto, Masanori Ootaki, Naoki Matsumoto, Masaomi Nangaku, Taroh Iiri
Disease-causing mutations in G protein-coupled receptor (GPCR) genes, including the V2 vasopressin receptor (V2R) gene, often cause misfolded receptors, leading to a defect in plasma membrane trafficking. A novel V2R mutation, T273M, identified in a boy with partial nephrogenic diabetes insipidus (NDI), shows intracellular localization and partial defects similar to the two mutants we described previously (10). Although non-peptide V2R antagonists have been shown to rescue the membrane localization of V2R mutants, their level of functional rescue is weak...
October 21, 2016: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/27558562/the-vasopressin-type-2-receptor-and-prostaglandin-receptors-ep2-and-ep4-can-increase-aquaporin-2-plasma-membrane-targeting-through-a-camp-independent-pathway
#20
Emma Tina Bisgaard Olesen, Hanne Bjerregaard Moeller, Mette Assentoft, Nanna MacAulay, Robert A Fenton
Apical membrane targeting of the collecting duct water channel aquaporin-2 (AQP2) is essential for body water balance. As this event is regulated by Gs coupled 7-transmembrane receptors such as the vasopressin type 2 receptor (V2R) and the prostanoid receptors EP2 and EP4, it is believed to be cAMP-dependent. However, on the basis of recent reports, it was hypothesized in the current study that increased cAMP levels are not necessary for AQP2 membrane targeting. The role and dynamics of cAMP signaling on AQP2 membrane targeting in Madin-Darby Canine Kidney and mouse cortical collecting duct (mpkCCD14) cells was examined using selective agonists against the V2R (dDAVP), EP2 (butaprost) and EP4 (CAY10580)...
August 24, 2016: American Journal of Physiology. Renal Physiology
keyword
keyword
90019
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"