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https://www.readbyqxmd.com/read/29650969/akaps-pka-disruptors-increase-aqp2-activity-independently-of-vasopressin-in-a-model-of-nephrogenic-diabetes-insipidus
#1
Fumiaki Ando, Shuichi Mori, Naofumi Yui, Tetsuji Morimoto, Naohiro Nomura, Eisei Sohara, Tatemitsu Rai, Sei Sasaki, Yoshiaki Kondo, Hiroyuki Kagechika, Shinichi Uchida
Congenital nephrogenic diabetes insipidus (NDI) is characterized by the inability of the kidney to concentrate urine. Congenital NDI is mainly caused by loss-of-function mutations in the vasopressin type 2 receptor (V2R), leading to impaired aquaporin-2 (AQP2) water channel activity. So far, treatment options of congenital NDI either by rescuing mutant V2R with chemical chaperones or by elevating cyclic adenosine monophosphate (cAMP) levels have failed to yield effective therapies. Here we show that inhibition of A-kinase anchoring proteins (AKAPs) binding to PKA increases PKA activity and activates AQP2 channels in cortical collecting duct cells...
April 12, 2018: Nature Communications
https://www.readbyqxmd.com/read/29600629/-effect-of-zhenwu-tang-on-regulating-of-avp-v2r-aqp2-pathway-in-nrk-52e-cells
#2
Xiao-Jie Zhou, Yu-Ting Bao, Hong-Shu Chen, Ling Xuan, Xue-Ming Chen, Jie-Ying Zhang, Yuan-Xiao Yang, Chang-Yu Li
This study was aimed to investigate the effect and mechanism of Zhenwu Tang on AVP-V2R-AQP2 pathway in NRK-52E cells in vitro . Forty eight male SD rats were randomly divided into eight groups with 6 animals in each group. Distilled water or 22.68 g·kg⁻¹·d⁻¹ Zhenwu Tang(calculated by raw drug dosage meter) was given by gavage. Blood samples were collected by cardiac puncture, and the medicated serum was centrifuged from the blood by 3 000 r·min⁻¹. NRK-52E cells were treated with different medicated serum or dDAVP...
February 2018: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/29589487/search-of-vasopressin-analogs-with-antiproliferative-activity-on-small-cell-lung-cancer-drug-design-based-on-two-different-approaches
#3
Marina Pifano, Juan Garona, Natasha T Sobol, Marina Albertó, Daniel F Alonso, Giselle V Ripoll
AIM: Development of compounds with therapeutic application requires the interaction of different disciplines. Several tumors express vasopressin (AVP; arginine vasopressin) receptors with contrasting effects depending on receptor subtype. Desmopressin (dDAVP) is an AVP-selective analog with antiproliferative properties. In this work, an evolutionary approach and a rational strategy were applied in order to design novel AVP analogs. RESULTS: We designed two novel analogs; dDInotocin (dDINT, insect analog), and [V4 Q5 ]dDAVP, and demonstrated the importance of the dDAVP conformational loop for its antiproliferative activity...
March 28, 2018: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29572717/ventricular-arrhythmias-originating-from-the-cardiac-crux-and-the-basal-inferior-segment-of-the-interventricular-septum-in-the-patients-with-structural-heart-diseases-characteristics-mapping-and-electrophysiological-properties
#4
Chung-Hsing Lin, Li-Wei Lo, Yenn-Jiang Lin, Shih-Lin Chang, Yu-Feng Hu, Ta-Chuan Tuan, Hung-Kai Huang, Cheng-Hung Chiang, Suresh Allamsetty, Jo-Nan Liao, Fa-Po Chung, Yao-Ting Chang, Chin-Yu Lin, Abigail Louise D Te, Shinya Yamada, Rohit Walia, Yuan Hung, Shih-Ann Chen
PURPOSE: There are few reports describing ventricular arrhythmias (VAs) from the crux and the corresponding endocardial site, i.e., the basal inferior segment of the interventricular septum (IVS). We aimed to investigate a distinct clinical group of VAs arising from the endocardium at this area in patients with structural heart diseases (SHD). METHODS: We included 17 patients with SHD and clinically documented VAs. Thirteen patients underwent endocardial mapping only...
March 23, 2018: Journal of Interventional Cardiac Electrophysiology: An International Journal of Arrhythmias and Pacing
https://www.readbyqxmd.com/read/29546600/focus-on-neonatal-and-infantile-onset-of-nephrogenic-syndrome-of-inappropriate-antidiuresis-12-years-later
#5
REVIEW
Flaminia Bardanzellu, Maria Cristina Pintus, Valentina Masile, Vassilios Fanos, Maria Antonietta Marcialis
Nephrogenic syndrome of inappropriate antidiuresis (NSIAD), first described in 2005, is a rare genetic X-linked disease, presenting with hyponatremia, hyposmolarity, euvolemia, inappropriately concentrated urine, increased natriuresis, and undetectable or very low arginine-vasopressine (AVP) circulating levels. It can occur in neonates, infants, or later in life. NSIAD must be early recognized and treated to prevent severe hyponatremia, which can show a dangerous impact on neonatal outcome. In fact, it potentially leads to death or, in case of survival, neurologic sequelae...
March 15, 2018: Pediatric Nephrology: Journal of the International Pediatric Nephrology Association
https://www.readbyqxmd.com/read/29524884/steviol-slows-renal-cyst-growth-by-reducing-aqp2-expression-and-promoting-aqp2-degradation
#6
Rattikarn Noitem, Chaowalit Yuajit, Sunhapas Soodvilai, Chatchai Muanprasat, Varanuj Chatsudthipong
Overexpression of aquaporin 2 (AQP2) was observed and suggested to be involved in fluid secretion leading to cyst enlargement in polycystic kidney disease (PKD). The cyst expansion deteriorates the renal function and, therefore, therapies targeting cyst enlargement are of clinical interest. Of note, inhibition of vasopressin function using vasopressin 2 receptor (V2R) antagonist which decreased cAMP production along with AQP2 production and function can slow cyst growth in ADPKD. This finding supports the role of AQP2 in cyst enlargement...
March 7, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29487210/monitoring-ligand-dependent-assembly-of-receptor-ternary-complexes-in-live-cells-by-bretfect
#7
David Cotnoir-White, Mohamed El Ezzy, Pierre-Luc Boulay, Marieke Rozendaal, Michel Bouvier, Etienne Gagnon, Sylvie Mader
There is currently an unmet need for versatile techniques to monitor the assembly and dynamics of ternary complexes in live cells. Here we describe bioluminescence resonance energy transfer with fluorescence enhancement by combined transfer (BRETFect), a high-throughput technique that enables robust spectrometric detection of ternary protein complexes based on increased energy transfer from a luciferase to a fluorescent acceptor in the presence of a fluorescent intermediate. Its unique donor-intermediate-acceptor relay system is designed so that the acceptor can receive energy either directly from the donor or indirectly via the intermediate in a combined transfer, taking advantage of the entire luciferase emission spectrum...
February 27, 2018: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/29478202/activation-of-aqp2-water-channels-without-vasopressin-therapeutic-strategies-for-congenital-nephrogenic-diabetes-insipidus
#8
REVIEW
Fumiaki Ando, Shinichi Uchida
Congenital nephrogenic diabetes insipidus (NDI) is characterized by defective urine concentrating ability. Symptomatic polyuria is present from birth, even with normal release of the antidiuretic hormone vasopressin by the pituitary. Over the last two decades, the aquaporin-2 (AQP2) gene has been cloned and the molecular mechanisms of urine concentration have been gradually elucidated. Vasopressin binds to the vasopressin type II receptor (V2R) in the renal collecting ducts and then activates AQP2 phosphorylation and trafficking to increase water reabsorption from urine...
February 24, 2018: Clinical and Experimental Nephrology
https://www.readbyqxmd.com/read/29465786/subpopulations-of-vomeronasal-sensory-neurons-with-coordinated-coexpression-of-type-2-vomeronasal-receptor-genes-are-differentially-dependent-on-vmn2r1
#9
Sachiko Akiyoshi, Tomohiro Ishii, Zhaodai Bai, Peter Mombaerts
The mouse vomeronasal organ is specialized in the detection of pheromones. Vomeronasal sensory neurons (VSNs) express chemosensory receptors of two large gene repertoires, V1R and V2R, which encode G-protein coupled receptors. Phylogenetically four families of V2R genes can be discerned: A, B, C, and D. VSNs located in the basal layer of the vomeronasal epithelium coordinately coexpress V2R genes from two families: approximately half of basal VSNs coexpress Vmn2r1 of family C with a single V2R gene of family A8-10, B, or D ("C1 type of V2Rs"), and the other half coexpress Vmn2r2 through Vmn2r7 of family C with a single V2R gene of family A1-6 ("C2 type V2Rs")...
February 21, 2018: European Journal of Neuroscience
https://www.readbyqxmd.com/read/29436285/m%C3%A3-ni%C3%A3-re-s-disease-pathophysiology-endolymphatic-sac-immunohistochemical-study-of-aquaporin-2-v2r-vasopressin-receptor-nkcc2-and-trpv4
#10
Marc-Henri Asmar, Louis Gaboury, Issam Saliba
Objectives Endolymphatic sac (ELS) pathophysiology in Ménière's disease (MD) remains poorly understood. We identified from the literature a group of proteins expressed on the ELS and involved in endolymph volume regulation: aquaporin-2 (AQP2), vasopressin receptor V2R, sodium potassium chloride cotransporter 2 (NKCC2), and transient receptor potential cation channel V4 (TRPV4). Our objective was to determine whether their ELS expression was altered in MD, to better understand the pathophysiology of endolymphatic hydrops...
February 1, 2018: Otolaryngology—Head and Neck Surgery
https://www.readbyqxmd.com/read/29335859/arginine-vasopressin-aquaporin-2-pathway-mediated-dehydration-effects-of-electroacupuncture-in-guinea-pig-model-of-avp-induced-endolymphatic-hydrops
#11
Li-Yuan Jiang, Jiao-Jun He, Xi-Xi Chen, Xue-Jiao Sun, Xue-Zhong Wang, Shan Zhong, Hua-de Chen
OBJECTIVE: To investigate the effects of electroacupuncture (EA) on endolymphatic hydrops (EH) and the regulation of arginine vasopressin (AVP)-aquaporin-2 (AQP2) pathway in guinea pigs. METHODS: EH was induced in male guinea pigs by an intraperitoneal injection of AVP. For the treatment, EA was delivered to Baihui (GV 20) and Tinggong (SI 19) acupoints, once per day for 10 consecutive days. In histomorphological studies, cochlear hydrops degree was evaluated by hematoxylin-eosin (HE) staining, and then the ratio of scala media (SM) area to SM + scala vestibuli (SV) area (R value) was calculated...
January 15, 2018: Chinese Journal of Integrative Medicine
https://www.readbyqxmd.com/read/29226502/s-r-difference-in-v1-v2-is-a-novel-criterion-for-differentiating-the-left-from-right-ventricular-outflow-tract-arrhythmias
#12
Onur Kaypakli, Hasan Koca, Durmus Yıldıray Sahin, Fadime Karataş, Suleyman Ozbicer, Mevlüt Koç
AIM: The correct estimation of the VA origin as RVOT or LVOT results in reduced ablation duration reduced radiation exposure and decreased number of vascular access. In our study, we aimed to detect the predictive value of S-R difference in V1-V2 for differentiating the left from right ventricular outflow tract arrhythmias. METHODS: We included 123 patients with symptomatic frequent premature ventricular outflow tract contractions who underwent successful catheter ablation (70 male, 53 female; mean age 46...
December 10, 2017: Annals of Noninvasive Electrocardiology
https://www.readbyqxmd.com/read/29138356/the-soluble-pro-renin-receptor-does-not-influence-lithium-induced-diabetes-insipidus-but-does-provoke-beiging-of-white-adipose-tissue-in-mice
#13
Kevin T Yang, Fei Wang, Xiaohan Lu, Kexin Peng, Tianxin Yang, J David Symons
Earlier we reported that the recombinant soluble (pro) renin receptor sPRR-His upregulates renal aquoporin-2 (AQP2) expression, and attenuates polyuria associated with nephrogenic diabetes insipidus (NDI) induced by vasopressin type 2 receptor (V2R) antagonism. Patients that receive lithium therapy develop polyuria associated NDI that might be secondary to downregulation of renal AQP2. We hypothesized that sPRR-His attenuates indices of NDI associated with lithium treatment. Eight-week-old male C57/BL6 mice consumed chow supplemented with LiCl (40 mmol/kg diets) for 14 days...
November 2017: Physiological Reports
https://www.readbyqxmd.com/read/28767678/pharmacoperone-rescue-of-vasopressin-2-receptor-mutants-reveals-unexpected-constitutive-activity-and-coupling-bias
#14
Jo Ann Janovick, Timothy P Spicer, Thomas D Bannister, Louis Scampavia, P Michael Conn
Pharmacoperones are small molecules that diffuse into cells and rescue misfolded, mistrafficked protein mutants, restoring their function. These substances act with high target specificity, serving as templates to fold (or refold) receptors, enzymes, ion channels or other proteins and enable them to pass the scrutiny of the cellular quality control system ("rescue"). In the present study we demonstrate that a rescued mutant (L83Q) of the vasopressin type 2 receptor (V2R), shows a strong bias for Gs coupling unlike the WT V2 receptor, which couples to both Gs and Gq/11...
2017: PloS One
https://www.readbyqxmd.com/read/28652375/evolution-of-immune-chemoreceptors-into-sensors-of-the-outside-world
#15
Quentin Dietschi, Joël Tuberosa, Lone Rösingh, Gregory Loichot, Manuel Ruedi, Alan Carleton, Ivan Rodriguez
Changes in gene expression patterns represent an essential source of evolutionary innovation. A striking case of neofunctionalization is the acquisition of neuronal specificity by immune formyl peptide receptors (Fprs). In mammals, Fprs are expressed by immune cells, where they detect pathogenic and inflammatory chemical cues. In rodents, these receptors are also expressed by sensory neurons of the vomeronasal organ, an olfactory structure mediating innate avoidance behaviors. Here we show that two gene shuffling events led to two independent acquisitions of neuronal specificity by Fprs...
July 11, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28630289/green-mamba-peptide-targets-type-2-vasopressin-receptor-against-polycystic-kidney-disease
#16
Justyna Ciolek, Helen Reinfrank, Loïc Quinton, Say Viengchareun, Enrico A Stura, Laura Vera, Sabrina Sigismeau, Bernard Mouillac, Hélène Orcel, Steve Peigneur, Jan Tytgat, Laura Droctové, Fabrice Beau, Jerome Nevoux, Marc Lombès, Gilles Mourier, Edwin De Pauw, Denis Servent, Christiane Mendre, Ralph Witzgall, Nicolas Gilles
Polycystic kidney diseases (PKDs) are genetic disorders that can cause renal failure and death in children and adults. Lowering cAMP in cystic tissues through the inhibition of the type-2 vasopressin receptor (V2R) constitutes a validated strategy to reduce disease progression. We identified a peptide from green mamba venom that exhibits nanomolar affinity for the V2R without any activity on 155 other G-protein-coupled receptors or on 15 ionic channels. Mambaquaretin-1 is a full antagonist of the V2R activation pathways studied: cAMP production, beta-arrestin interaction, and MAP kinase activity...
July 3, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28577072/regulation-of-renal-na-k-cl-cotransporters-by-vasopressin
#17
REVIEW
Sebastian Bachmann, Kerim Mutig
Vasopressin (AVP) induces antidiuresis, thus playing an essential role in body water and electrolyte homeostasis. Its antidiuretic effects are mediated chiefly by V2 vasopressin receptors (V2R) expressed along the distal nephron and collecting duct epithelia. NaCl reabsorption in the distal nephron, which includes the thick ascending limb (TAL) and distal convoluted tubule (DCT), largely depends on the activity of two structurally related Na-(K)-Cl cotransporters, NKCC2 in TAL and NCC in DCT. AVP-induced activation of these transporters contributes to urine concentration and renal electrolyte reabsorption...
August 2017: Pflügers Archiv: European Journal of Physiology
https://www.readbyqxmd.com/read/28458780/identification-of-olfactory-receptor-genes-in-the-japanese-grenadier-anchovy-coilia-nasus
#18
Guoli Zhu, Liangjiang Wang, Wenqiao Tang, Xiaomei Wang, Cong Wang
Olfaction is essential for fish to detect odorant elements in the environment and plays a critical role in navigating, locating food and detecting predators. Olfactory function is produced by the olfactory transduction pathway and is activated by olfactory receptors (ORs) through the binding of odorant elements. Recently, four types of olfactory receptors have been identified in vertebrate olfactory epithelium, including main odorant receptors (MORs), vomeronasal type receptors (VRs), trace-amine associated receptors (TAARs) and formyl peptide receptors (FPRs)...
2017: Genes & Genomics
https://www.readbyqxmd.com/read/28455745/expanding-the-role-of-vasopressin-antagonism-in-polycystic-kidney-diseases-from-adults-to-children
#19
Peter Janssens, Caroline Weydert, Stephanie De Rechter, Karl Martin Wissing, Max Christoph Liebau, Djalila Mekahli
Polycystic kidney disease (PKD) encompasses a group of genetic disorders that are common causes of renal failure. The two classic forms of PKD are autosomal recessive polycystic kidney disease (ARPKD) and autosomal dominant polycystic kidney disease (ADPKD). Despite their clinical differences, ARPKD and ADPKD share many similarities. Altered intracellular Ca(2+) and increased cyclic adenosine monophosphate (cAMP) concentrations have repetitively been described as central anomalies that may alter signaling pathways leading to cyst formation...
April 28, 2017: Pediatric Nephrology: Journal of the International Pediatric Nephrology Association
https://www.readbyqxmd.com/read/28419717/ligand-recognition-properties-of-the-vasopressin-v2-receptor-studied-under-qsar-and-molecular-modeling-strategies
#20
Marlet Martínez-Archundia, Brenda Colín-Astudillo, Liliana M Moreno-Vargas, Guillermo Ramírez-Galicia, Ramón Garduño-Juárez, Omar Deeb, Martha Citlalli Contreras-Romo, Andres 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. 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...
November 2017: Chemical Biology & Drug Design
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