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https://www.readbyqxmd.com/read/28501141/trpv6-from-identification-to-function
#1
REVIEW
Claudia Fecher-Trost, Ulrich Wissenbach, Petra Weissgerber
No abstract text is available yet for this article.
April 28, 2017: Cell Calcium
https://www.readbyqxmd.com/read/28498349/desalted-duck-egg-white-peptides-promote-calcium-uptake-and-modulate-bone-formation-in-the-retinoic-acid-induced-bone-loss-rat-and-caco-2-cell-model
#2
Tao Hou, Yanshuang Liu, Nikolai Kolba, Danjun Guo, Hui He
Desalted duck egg white peptides (DPs) have been proven to promote calcium uptake in Caco-2 cells and rats treated with a calcium-deficient diet. The retinoic acid-induced bone loss model was used to evaluate the effect of DPs on calcium absorption and bone formation. Three-month-old Wistar female rats were treated with 0.9% saline, DPs (800 mg/kg), or alendronate (5 mg/kg) for three weeks immediately after retinoic acid treatment (80 mg/kg) once daily for two weeks. The model group was significantly higher in serum bone alkaline phosphatase than the other three groups (p < 0...
May 12, 2017: Nutrients
https://www.readbyqxmd.com/read/28416203/the-s4-s5-linker-gearbox-of-trp-channel-gating
#3
REVIEW
Laura Hofmann, Hongmei Wang, Wang Zheng, Stephan E Philipp, Patricia Hidalgo, Adolfo Cavalié, Xing-Zhen Chen, Andreas Beck, Veit Flockerzi
Transient receptor potential (TRP) channels are cation channels which participate in a wide variety of physiological processes in organisms ranging from fungi to humans. They fulfill roles in body homeostasis, are sensors for noxious chemicals and temperature in the mammalian somatosensory system and are activated by light stimulated phospholipase C activity in Drosophila or by hypertonicity in yeast. The transmembrane topology of TRP channels is similar to that of voltage-gated cation channels. TRP proteins assemble as tetramers with each subunit containing six transmembrane helices (S1-S6) and intracellular N- and C-termini...
April 4, 2017: Cell Calcium
https://www.readbyqxmd.com/read/28389981/erratum-to-first-in-human-phase-i-study-of-sor-c13-a-trpv6-calcium-channel-inhibitor-in-patients-with-advanced-solid-tumors
#4
S Fu, H Hirte, S Welch, T T Ilenchuk, T Lutes, C Rice, N Fields, A Nemet, D Dugourd, S Piha-Paul, V Subbiah, L Liu, J Gong, D Hong, J M Stewart
No abstract text is available yet for this article.
June 2017: Investigational New Drugs
https://www.readbyqxmd.com/read/28374795/a-gate-hinge-controls-the-epithelial-calcium-channel-trpv5
#5
Jenny van der Wijst, Elizabeth H Leunissen, Maxime G Blanchard, Hanka Venselaar, Sjoerd Verkaart, Candice E Paulsen, René J Bindels, Joost G Hoenderop
TRPV5 is unique within the large TRP channel family for displaying a high Ca(2+) selectivity together with Ca(2+)-dependent inactivation. Our study aims to uncover novel insights into channel gating through in-depth structure-function analysis. We identify an exceptional tryptophan (W583) at the terminus of the intracellular pore that is unique for TRPV5 (and TRPV6). A combination of site-directed mutagenesis, biochemical and electrophysiological analysis, together with homology modeling, demonstrates that W583 is part of the gate for Ca(2+) permeation...
April 4, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28270862/the-polypharmacology-browser-a-web-based-multi-fingerprint-target-prediction-tool-using-chembl-bioactivity-data
#6
Mahendra Awale, Jean-Louis Reymond
BACKGROUND: Several web-based tools have been reported recently which predict the possible targets of a small molecule by similarity to compounds of known bioactivity using molecular fingerprints (fps), however predictions in each case rely on similarities computed from only one or two fps. Considering that structural similarity and therefore the predicted targets strongly depend on the method used for comparison, it would be highly desirable to predict targets using a broader set of fps simultaneously...
2017: Journal of Cheminformatics
https://www.readbyqxmd.com/read/28152538/two-cases-of-mistaken-polyuria-and-nephrocalcinosis-in-infants-with-glucose-galactose-malabsorption-a-possible-role-of-1-25-oh-2d3%C3%A2
#7
Melissa Fiscaletti, Marie-Jeanne Lebel, Nathalie Alos, Geneviève Benoit, Prévost Jantchou
BACKGROUND/AIMS: Glucose-galactose malabsorption (GGM) is a rare and potentially fatal disorder. The autosomal recessive mutation of the SGLT1 gene interferes with the active glucose transport in the gut resulting in osmotic diarrhea and failure to thrive (FTT). Two nonrelated infants with GGM are presented as well as a novel mutation in SGLT1. CASE PRESENTATION: The first case consulted for FTT and presented with hypercalcemia and hypercalciuria. His mother had self-medicated with high doses of vitamin D...
February 2, 2017: Hormone Research in Pædiatrics
https://www.readbyqxmd.com/read/28150073/first-in-human-phase-i-study-of-sor-c13-a-trpv6-calcium-channel-inhibitor-in-patients-with-advanced-solid-tumors
#8
S Fu, H Hirte, S Welch, T T Ilenchuk, T Lutes, C Rice, N Fields, A Nemet, D Dugourd, S Piha-Paul, V Subbiah, L Liu, J Gong, D Hong, J M Stewart
Introduction This was an open-label, dose escalation (3 + 3 design), Phase I study of SOR-C13 in patients with advanced tumors of epithelial origin. Primary objectives were to assess safety/tolerability and pharmacokinetics. Secondary goals were to assess pharmacodynamics and efficacy of SOR-C13. Methods SOR-C13 was administered IV QD on days 1-3 and 8-10 of a 21-day cycle. Doses were 2.75 and 5.5 mg/kg (20-min infusion) and 1.375, 2.75, 4.13 and 6.2 mg/kg (90-min infusion). Toxicity was assessed by National Cancer Institute (NCI) Common Terminology Criteria for Adverse Events (CTCAE) version 4...
June 2017: Investigational New Drugs
https://www.readbyqxmd.com/read/28107527/effects-of-the-administration-of-25-oh-vitamin-d3-in-an-experimental-model-of-chronic-kidney-disease-in-animals-null-for-1-alpha-hydroxylase
#9
Noelia Torremadé, Milica Bozic, David Goltzman, Elvira Fernandez, José M Valdivielso
The final step in vitamin D activation is catalyzed by 1-alpha-hydroxylase (CYP27B1). Chronic kidney disease (CKD) is characterized by low levels of both 25(OH)D3 and 1,25(OH)2D3 provoking secondary hyperparathyroidism (2HPT). Therefore, treatments with active or native vitamin D compounds are common in CKD to restore 25(OH)D3 levels and also to decrease PTH. This study evaluates the dose of 25(OH)D3 that restores parathyroid hormone (PTH) and calcium levels in a model of CKD in CYP27B1-/- mice. Furthermore, we compare the safety and efficacy of the same dose in CYP27B1+/+ animals...
2017: PloS One
https://www.readbyqxmd.com/read/28077439/the-functional-expression-of-transient-receptor-potential-channels-in-the-mouse-endometrium
#10
Katrien De Clercq, Charlotte Van den Eynde, Aurélie Hennes, Rieta Van Bree, Thomas Voets, Joris Vriens
STUDY QUESTION: Does mouse endometrial epithelial cells and stromal cells have a similar transient receptor potential (TRP)-channel expression profile and to that found in the human endometrium? SUMMARY ANSWER: Mouse endometrial epithelial and stromal cells have a distinct TRP channel expression profile analogous to what has been found in human endometrium, and hence suggests the mouse a good model to investigate the role of TRP channels in reproduction. WHAT IS KNOWN ALREADY: An optimal intercellular communication between epithelial and stromal endometrial cells is crucial for successful reproduction...
March 1, 2017: Human Reproduction
https://www.readbyqxmd.com/read/28063212/regulation-of-chondrocyte-functions-by-transient-receptor-potential-cation-channel-v6-in-osteoarthritis
#11
Tengfei Song, Jun Ma, Lei Guo, Peng Yang, Xuhui Zhou, Tianwen Ye
Transient receptor potential vanilloid (TRPV) channels function to maintain the dynamic balance of calcium signaling and calcium metabolism in bones. The goal of this study was to determine the potential role of TRPV6 in regulation of chondrocytes. The level of TRPV6 expression was analyzed by western blot in articular cartilage derived from the knee joints of osteoarthritis (OA) rat models and OA patients. Bone structure and osteoarthritic changes in the knee joints of TRPV6 knockout mice were examined using micro-computed and histological analysis at the age of 6 and 12 months old...
January 7, 2017: Journal of Cellular Physiology
https://www.readbyqxmd.com/read/28057718/calcium-mediated-oxidative-stress-a-common-mechanism-in-tight-junction-disruption-by-different-types-of-cellular-stress
#12
Ruchika Gangwar, Avtar Meena, Pradeep Shukla, Archana Nagaraja, Piotr Dorniak, Sandeep Pallikuth, Christopher Waters, Anil Sood, Radhakrishna Rao
The role of reactive oxygen species (ROS) in osmotic stress, dextran sulfate sodium (DSS) and cyclic stretch-induced tight junction disruption was investigated in Caco-2 cell monolayers in vitro , and restraint stress-induced barrier dysfunction in mouse colon in vivo Live cell imaging showed that osmotic stress, cyclic stretch and DSS triggered rapid production of ROS in Caco-2 cell monolayers, which was blocked by depletion of intracellular Ca(2+) by BAPTA. Knockdown of CaV1.3 or TRPV6 channels blocked osmotic stress and DSS-induced ROS production and attenuated tight junction disruption and barrier dysfunction...
January 5, 2017: Biochemical Journal
https://www.readbyqxmd.com/read/28039038/transient-receptor-potential-vanilloid-6-trpv6-in-the-mouse-brain-distribution-and-estrous-cycle-related-changes-in-the-hypothalamus
#13
Santosh Kumar, Uday Singh, Omprakash Singh, Chandan Goswami, Praful S Singru
Transient receptor potential vanilloid (TRPV) subfamily of cationic channels have emerged as novel players in neural regulation. Unlike other members of TRPV subfamily, TRPV5 and TRPV6 are highly Ca(2+)-selective. Although TRPV5/TRPV6 transcripts are expressed in mouse brain, understanding the full functional spectrum of these ion channels in the brain is however limited due to the lack of information on their neuroanatomical distribution. We have studied TRPV6 in mouse brain in further detail. In the hypothalamus, while Western blot analysis using TRPV6 specific antiserum showed a distinct ∼95 kDa band corresponding to the molecular weight of TRPV6, transcripts for TRPV6 were detected with RT-PCR...
March 6, 2017: Neuroscience
https://www.readbyqxmd.com/read/28029385/a-conserved-gating-element-in-trpv6-channels
#14
REVIEW
Laura Hofmann, Hongmei Wang, Andreas Beck, Ulrich Wissenbach, Veit Flockerzi
The Ca(2+)-selective tetrameric Transient Receptor Potential Vanilloid 6 (TRPV6) channel is an inwardly rectifying ion channel. The constitutive current endures Ca(2+)-induced inactivation as a result of the activation of phospholipase C followed depletion of phosphatidylinositol 4,5-bisphosphate, and calmodulin binding. Replacing a glycine residue within the cytosolic S4-S5 linker of the human TRPV6 protein, glycine 516, which is conserved in all TRP channel proteins, by a serine residue forces the channels into an open conformation thereby enhancing constitutive Ca(2+) entry and preventing inactivation...
October 28, 2016: Cell Calcium
https://www.readbyqxmd.com/read/28008282/expression-and-functionality-of-trpv1-in-breast-cancer-cells
#15
Lea V Weber, Klaudia Al-Refae, Gerhard Wölk, Gabriele Bonatz, Janine Altmüller, Christian Becker, Günter Gisselmann, Hanns Hatt
Transient receptor potential (TRP) channels contribute to the regulation of intracellular calcium, which can promote cancer hallmarks in cases of dysregulation of gene transcription and calcium-dependent pro-proliferative or anti-apoptotic mechanisms. Several studies have begun to elucidate the roles of TRPV1, TRPV6, TRPM8, and TRPC1 in cancer progression; however, no study has examined the expression profiles of human TRP channels in breast cancer on a large scale. This study focused on the expression and functionality of TRPV1, a nonselective cation channel that was found to be expressed in different carcinoma tissues...
2016: Breast Cancer: Targets and Therapy
https://www.readbyqxmd.com/read/27958326/calcium-channels-and-oxidative-stress-mediate-a-synergistic-disruption-of-tight-junctions-by-ethanol-and-acetaldehyde-in-caco-2-cell-monolayers
#16
Geetha Samak, Ruchika Gangwar, Avtar S Meena, Roshan G Rao, Pradeep K Shukla, Bhargavi Manda, Damodaran Narayanan, Jonathan H Jaggar, RadhaKrishna Rao
Ethanol is metabolized into acetaldehyde in most tissues. In this study, we investigated the synergistic effect of ethanol and acetaldehyde on the tight junction integrity in Caco-2 cell monolayers. Expression of alcohol dehydrogenase sensitized Caco-2 cells to ethanol-induced tight junction disruption and barrier dysfunction, whereas aldehyde dehydrogenase attenuated acetaldehyde-induced tight junction disruption. Ethanol up to 150 mM did not affect tight junction integrity or barrier function, but it dose-dependently increased acetaldehyde-mediated tight junction disruption and barrier dysfunction...
December 13, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27932504/expression-of-cav1-3-calcium-channel-in-the-human-and-mouse-colon-posttranscriptional-inhibition-by-ifn%C3%AE
#17
Vijayababu M Radhakrishnan, Maryam M Gilpatrick, Nour Alhoda Parsa, Pawel R Kiela, Fayez K Ghishan
It has been hypothesized that apically expressed L-type Ca(2+) channel Cav1.3 (encoded by CACNA1D gene) contributes toward an alternative TRPV6-independent route of intestinal epithelial Ca(2+) absorption, especially during digestion when high luminal concentration of Ca(2+) and other nutrients limit TRPV6 contribution. We and others have implicated altered expression and activity of key mediators of intestinal and renal Ca(2+) (re)absorption as contributors to negative systemic Ca(2+) balance and bone loss in intestinal inflammation...
January 1, 2017: American Journal of Physiology. Gastrointestinal and Liver Physiology
https://www.readbyqxmd.com/read/27913205/trp-channels-in-calcium-homeostasis-from-hormonal-control-to-structure-function-relationship-of-trpv5-and-trpv6
#18
REVIEW
Mark K C van Goor, Joost G J Hoenderop, Jenny van der Wijst
Maintaining plasma calcium levels within a narrow range is of vital importance for many physiological functions. Therefore, calcium transport processes in the intestine, bone and kidney are tightly regulated to fine-tune the rate of absorption, storage and excretion. The TRPV5 and TRPV6 calcium channels are viewed as the gatekeepers of epithelial calcium transport. Several calciotropic hormones control the channels at the level of transcription, membrane expression, and function. Recent technological advances have provided the first near-atomic resolution structural models of several TRPV channels, allowing insight into their architecture...
November 30, 2016: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/27747588/trpv6-is-a-prognostic-marker-in-early-stage-cervical-squamous-cell-carcinoma
#19
Fei Sun, Lu Xiao, Xin-Xing Jang, Ying Xiong, Qi Li, Xiao-Jing Yue, Yun-Jian Wei, Yan-Xing Wei, Yan-Lin Ma, Yan-Hong Yu
Transient receptor potential vanilloid 6 (TRPV6) has been shown to promote caner proliferation in several solid tumors, leading to unfavorable clinical outcomes. Our study aimed to elucidate the clinical significance of TRPV6 in patients with early-stage cervical squamous cell carcinoma (CSCC). The mRNA expression of TRPV6 was measured in 12 paired early-stage CSCC specimens and six cervical carcinoma cell lines using quantitative real-time PCR (qRT-PCR). Western blotting and immunohistochemistry (IHC) were employed to examine the protein expression level of TRPV6 in four paired specimens, 175 paraffin-embedded early-stage CSCC specimens, and 50 normal cervical tissues (NCTs), respectively...
October 17, 2016: Tumour Biology: the Journal of the International Society for Oncodevelopmental Biology and Medicine
https://www.readbyqxmd.com/read/27690074/effects-of-octylphenol-and-bisphenol-a-on-the-metal-cation-transporter-channels-of-mouse-placentas
#20
Jae-Hwan Lee, Changhwan Ahn, Hee Young Kang, Eui-Ju Hong, Sang-Hwan Hyun, Kyung-Chul Choi, Eui-Bae Jeung
Octylphenol (OP) and bisphenol A (BPA) are known as endocrine-disrupting chemicals (EDCs). During pregnancy, the expression of steroid hormone receptors is controlled by maternal and fetal nutrition. To evaluate the impact of EDCs during pregnancy, ethinyl estradiol (EE, 0.2 mg/kg/day), OP (50 mg/kg/day), and BPA (50 mg/kg/day) were administered to pregnant mice. The mRNA levels of TRPV6 (transient receptor potential cation channels in subfamily V, member 6) decreased significantly by EE and OP. The PMCA1 (ATPase, Ca(++) transporting, plasma membrane 1) mRNA and protein levels decreased significantly by EE, OP, and BPA...
September 28, 2016: International Journal of Environmental Research and Public Health
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