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https://www.readbyqxmd.com/read/29791207/activation-of-trpv4-stimulates-transepithelial-ion-flux-in-a-porcine-choroid-plexus-cell-line
#1
Daniel Preston, Stefanie Simpson, Dan Halm, Alexandra Hochstetler, Christian Schwerk, Horst Schroten, Bonnie L Blazer-Yost
The choroid plexus (CP) epithelium plays a major role in the production of cerebrospinal fluid (CSF). A polarized cell line, the porcine choroid plexus - Riems (PCP-R) line, that exhibits many of the characteristics of the native epithelium, was used to study the effect of activation of the transient receptor potential vanilloid 4 (TRPV4) cation channel found in the PCP-R cells as well as in the native epithelium. Ussing-style electrophysiological experiments showed that activation of TRPV4 with a specific agonist, GSK 1016790A, resulted in an immediate increase in both transepithelial ion flux and conductance...
May 23, 2018: American Journal of Physiology. Cell Physiology
https://www.readbyqxmd.com/read/29789636/cypripedin-diminishes-an-epithelial-to-mesenchymal-transition-in-non-small-cell-lung-cancer-cells-through-suppression-of-akt-gsk-3%C3%AE-signalling
#2
Surassawadee Treesuwan, Boonchoo Sritularak, Pithi Chanvorachote, Varisa Pongrakhananon
Lung cancer appears to have the highest rate of mortality among cancers due to its metastasis capability. To achieve metastasis, cancer cells acquire the ability to undergo a switch from epithelial to mesenchymal behaviour, termed the epithelial-to-mesenchymal transition (EMT), which is associated with poor clinical outcomes. Drug discovery attempts have been made to find potent compounds that will suppress EMT. Cypripedin, a phenanthrenequinone isolated from Thai orchid, Dendrobium densiflorum, exhibits diverse pharmacological activities...
May 22, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29788004/juvenile-traumatic-brain-injury-results-in-cognitive-deficits-associated-with-impaired-endoplasmic-reticulum-stress-and-early-tauopathy
#3
Michael J Hylin, Ryan C Holden, Aidan C Smith, Aric F Logsdon, Rabia Qaiser, Brandon P Lucke-Wold
The leading cause of death in the juvenile population is trauma, and in particular neurotrauma. The juvenile brain response to neurotrauma is not completely understood. Endoplasmic reticulum (ER) stress has been shown to contribute to injury expansion and behavioral deficits in adult rodents and furthermore has been seen in adult postmortem human brains diagnosed with chronic traumatic encephalopathy. Whether endoplasmic reticulum stress is increased in juveniles with traumatic brain injury (TBI) is poorly delineated...
May 22, 2018: Developmental Neuroscience
https://www.readbyqxmd.com/read/29786763/mir-124-promotes-proliferation-and-neural-differentiation-of-neural-stem-cells-through-targeting-dact1-and-activating-wnt-%C3%AE-catenin-pathways
#4
Shujie Jiao, Yaling Liu, Yaobing Yao, Junfang Teng
Neural stem cells (NSCs) are multipotent and undifferentiated cells with the potential to differentiate into neuronal lineages and gliocytes. NSCs have the ability to generate and regenerate the brain, indicating the possibility of cell-based therapies for neurological disorders. miR-124 has been demonstrated as a modulator in the survival, expansion, and differentiation of NSCs. However, the underlying molecular mechanisms of miR-124 in NSC development are still far from being understood. The expressions of miR-124, dishevelled binding antagonist of beta-catenin 1 (DACT1), ki-67, Nestin, β-tubulin III, glial fibrillary acidic protein (GFAP), β-catenin, cyclinD1, and glycogen synthase kinase-3β (GSK-3β) were examined by qRT-PCR or western blot...
May 21, 2018: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/29784906/the-anti-cancer-activity-of-an-andrographolide-analogue-functions-through-a-gsk-3%C3%AE-independent-wnt-%C3%AE-catenin-signaling-pathway-in-colorectal-cancer-cells
#5
Somrudee Reabroi, Rungnapha Saeeng, Nittaya Boonmuen, Teerapich Kasemsuk, Witchuda Saengsawang, Kanoknetr Suksen, Weiming Zhu, Pawinee Piyachaturawat, Arthit Chairoungdua
The Wnt/β-catenin signaling pathway plays a key role in the progression of human colorectal cancers (CRCs) and is one of the leading targets of chemotherapy agents developed for CRC. The present study aimed to investigate the anti-cancer effects and molecular mechanisms of 19-O-triphenylmethyl andrographolide (RS-PP-050), an andrographolide analogue and determine its activity in the Wnt/β-catenin pathway. RS-PP-050 was found to potently inhibit the proliferation and survival of HT-29 CRC cells. It induces cell cycle arrest and promotes apoptotic cell death which was associated with the activation of PARP-1 and p53...
May 21, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29782894/screening-of-the-mmv-and-gsk-open-access-chemical-boxes-using-a-viability-assay-developed-against-the-kinetoplastid-crithidia-fasciculata
#6
Wakisa Kipandula, Simon A Young, Stuart A MacNeill, Terry K Smith
Diseases caused by the pathogenic kinetoplastids continue to incapacitate and kill hundreds of thousands of people annually throughout the tropics and sub-tropics. Unfortunately, in the countries where these neglected diseases occur, financial obstacles to drug discovery and technical limitations associated with biochemical studies impede the development of new, safe, easy to administer and effective drugs. Here we report the development and optimisation of a Crithidia fasciculata resazurin viability assay, which is subsequently used for screening and identification of anti-crithidial compounds in the MMV and GSK open access chemical boxes...
May 18, 2018: Molecular and Biochemical Parasitology
https://www.readbyqxmd.com/read/29781534/lncrna-meg3-repressed-malignant-melanoma-progression-via-inactivating-wnt-signaling-pathway
#7
Peng Li, Ying Gao, Jun Li, Yu Zhou, Jing Yuan, Huiwen Guan, Peng Yao
Accumulating evidence has indicated that MEG3 can serve as a tumor suppressive lncRNA in various tumors. It is aberrantly expressed in multiple cancers. However, the biological roles of MEG3 in melanoma are poorly understood. Therefore, in our study, we concentrated on the biological mechanism of MEG3 in melanoma progression. First, we observed that MEG3 was obviously decreased in melanoma cells including A375, SK-MEL-1, B16, and A2058 cells compared to human epidermal melanocytes HEMa-LP. MEG3 was restored by transfecting LV-MEG3 in to A375 and A2058 cells...
May 21, 2018: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/29781013/design-and-synthesis-of-aza-indolyl-maleimide-based-covalent-inhibitors-of-glycogen-synthase-kinase-3%C3%AE
#8
Zhimin Yang, Hui Liu, Botao Pan, Fengli He, Zhengying Pan
As an important kinase in multiple signal transduction pathways, GSK-3β has been an attractive target for chemical probe discovery and drug development. Compared to numerous reversible inhibitors that have been developed, covalent inhibitors of GSK-3β are noticeably lacking. Here, we report the discovery of a series of covalent GSK-3β inhibitors by optimizing both non-covalent interactions and reactive groups. Among these covalent inhibitors, compound 38b with a mild α-fluoromethyl amide reactive group emerges as a selective and covalent inhibitor against GSK-3β, effectively inhibits the phosphorylation of glycogen synthase and tau protein, and increases β-catenin's levels in living cells...
May 21, 2018: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/29779329/-mechanisms-of-recombinant-adenovirus-mediated-sd-ha-fusion-protein-proliferation-inhibition-and-induced-apoptosis-of-k562-cells
#9
Y Huang, P Zhang, L Du, M Gui, W L Feng, Z Peng
Objective: To investigate whether fusion protein SD-HA could regulate its downstream signaling molecule activity by competing with the phospho-BCR-ABL Y177 site, and its mechanisms to inhibit proliferation and induce apoptosis of K562 cells. Methods: Co-immunoprecipitation interaction technology analysis of fusion protein SD-HA functioned by potently binding to the phospho-BCR-ABL Y177 site, Ras, MAPK and Akt activities were observed in the Ad5F35-SD-HA-treated cells. Western blot analyses of SD-HA fusion protein on cell membrane receptor pathway to death cascade caspase-8, caspase-3 and PRAP were performed...
April 14, 2018: Zhonghua Xue Ye Xue za Zhi, Zhonghua Xueyexue Zazhi
https://www.readbyqxmd.com/read/29777831/microcystis-bloom-containing-microcystin-lr-induces-type-2-diabetes-mellitus
#10
Qiong Zhang, Wendi Qin, Liuyan Yang, Jing An, Xuxiang Zhang, Hao Hong, Lizhi Xu, Yaping Wang
Epidemiological data from Lake Taihu showed significantly higher incidences of type 2 diabetes mellitus (T2DM) than in other areas of China. This may be related to the occurrence of a Microcystis bloom in Lake Taihu in the summer and autumn every year. The objective of this study is to investigate whether the contaminated water from the Microcystis bloom and the derivative pollutant microcystin-LR (MC-LR) can explain the higher incidences of T2DM. Healthy male mice were fed with water from different regions of Lake Taihu, and were either acutely or chronically exposed to MC-LR through oral administration or intraperitoneal injection...
May 16, 2018: Toxicology Letters
https://www.readbyqxmd.com/read/29777057/glycogen-synthase-kinase-3-gsk-3-activity-regulates-mrna-methylation-in-mouse-embryonic-stem-cells
#11
Kelsie J Faulds, Jennifer N Egelston, Laura J Sedivy, Matthew K Mitchell, Sanjana Garimella, Hanna Kozlowski, Angelo D'Alessandro, Kirk C Hansen, Jeremy L Balsbaugh, Christopher J Phiel
Glycogen synthase kinase-3 (Gsk-3) activity regulates multiple signal transduction pathways, and is also a key component of the network responsible for maintaining stem cell pluripotency. Genetic deletion of Gsk-3α and Gsk-3β or inhibition of Gsk-3 activity via small molecules promotes stem cell pluripotency, yet the mechanism underlying the role for Gsk-3 in this process remains ambiguous. Another cellular process that has been shown to affect stem cell pluripotency is mRNA methylation (m6 A). Here, we describe an intersection between these components - the regulation of m6 A by Gsk-3...
May 18, 2018: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/29775701/lithium-posttreatment-alleviates-blood-brain-barrier-injury-after-intracerebral-hemorrhage-in-rats
#12
Weishan Li, Rui Li, Sha Zhao, Cheng Jiang, Zhen Liu, Xiaobo Tang
Vasogenic cerebral edema formation after blood brain barrier (BBB) damage aggravates the devastating consequences of intracerebral hemorrhage (ICH). The present study aims to probe into a therapeutic method on BBB preservation after ICH with a glycogen synthase kinase-3β (GSK-3β) inhibitor, lithium. Intrastriatal infusion of semicoagulated autologous whole blood or sham surgery was performed on male Sprague-Dawley (SD) rats (n = 208).Experimental animals received administration of 4,6-disubstitutedpyrrolo-pyrimidine (TWS119), lithium alone or in combination with a phosphatidylinositol 3-kinase inhibitor, wortmannin, after ICH...
May 15, 2018: Neuroscience
https://www.readbyqxmd.com/read/29775181/porous-lithium-doped-hydroxyapatite-scaffold-seeded-with-hypoxia-preconditioned-bone-marrow-mesenchymal-stem-cells-for-bone-tissue-regeneration
#13
Donghai Li, Huifang Liu, Jinhai Zhao, Zhouyuan Yang, Xiaowei Xie, Zhun Wei, Dongzhe Li, Pengde Kang
Hydroxyapatite (HA) is a commonly used biomaterial in bone-tissue engineering, but pure HA is deficient in osteoinduction. In this study, we fabricated scaffolds of lithium-doped HA (Li-HA) and assess the bone generation enhancement of Li-HA scaffolds seeded with hypoxia-preconditioned bone-marrow mesenchymal stem cells (BMMSCs). We found that 1.5%Li-HA obtained optimal cell proliferation activity in vitro. In an in vivo study, Li-HA/BMSCs enhanced new bone formation, reducing the GSK-3β and increasing the β-catenin, but the angiogenic effect was not modified significantly...
May 18, 2018: Biomedical Materials
https://www.readbyqxmd.com/read/29774334/a-comparative-study-of-epa-enriched-ethanolamine-plasmalogen-and-epa-enriched-phosphatidylethanolamine-on-a%C3%AE-42-induced-cognitive-deficiency-in-a-rat-model-of-alzheimer-s-disease
#14
Hongxia Che, Qian Li, Tiantian Zhang, Lin Ding, Lingyu Zhang, Haohao Shi, Teruyoshi Yanagita, Changhu Xue, Yaoguang Chang, Yuming Wang
Ethanolamine plasmalogen (pPE), a major phospholipid in neuronal membranes, is specifically reduced in postmortem brains from patients with Alzheimer's disease (AD). The purpose of the present study was to compare the effects of EPA-enriched ethanolamine plasmalogen (EPA-pPE) and EPA-enriched phosphatidylethanolamine (EPA-PE) on cognitive deficiency and illustrate the possible underlying mechanisms. SD rats were divided into four groups including the sham group injected with 0.9% saline and three amyloid-β (Aβ) infusion groups, Aβ42 group, EPA-pPE group and EPA-PE group...
May 18, 2018: Food & Function
https://www.readbyqxmd.com/read/29773969/cost-effectiveness-of-umeclidinium-compared-with-tiotropium-and-glycopyrronium-as-monotherapy-for-chronic-obstructive-pulmonary-disease-a-uk-perspective
#15
Dhvani Shah, Maurice Driessen, Nancy Risebrough, Timothy Baker, Ian Naya, Andrew Briggs, Afisi S Ismaila
Background: Cost-effectiveness of once-daily umeclidinium bromide (UMEC) was compared with once-daily tiotropium (TIO) and once-daily glycopyrronium (GLY) in patients with chronic obstructive pulmonary disease (COPD) from a UK National Health Service (NHS) perspective. Methods: A linked-equation model was implemented to estimate COPD progression, associated healthcare costs, exacerbations rates, life years (LY) and quality-adjusted LY (QALYs). Statistical risk equations for endpoints and resource use were derived from the ECLIPSE and TORCH studies, respectively...
2018: Cost Effectiveness and Resource Allocation: C/E
https://www.readbyqxmd.com/read/29772481/vascular-peroxide-1-promotes-ox-ldl-induced-programmed-necrosis-in-endothelial-cells-through-a-mechanism-involving-%C3%AE-catenin-signaling
#16
Yin-Zhuang Zhang, Lei Wang, Jie-Jie Zhang, Xiao-Ming Xiong, Di Zhang, Xuan-Meng Tang, Xiu-Ju Luo, Qi-Lin Ma, Jun Peng
BACKGROUND AND AIMS: Vascular peroxidase 1 (VPO1) plays a key role in mediation of cardiovascular oxidative injury. This study aims to determine whether VPO1 can promote programmed necrosis of endothelial cells and the underlying mechanisms. METHODS AND RESULTS: Human umbilical vein endothelial cells (HUVECs) were incubated with oxidized low-density lipoprotein (ox-LDL, 100 μg/mL) for 48 h to induce cell injury, which showed an elevation in cell necrosis (reflected by the increased propidium iodide (PI) positive-staining cells, LDH release and decreased cell viability), concomitant with an increase in programmed necrosis-relevant proteins including receptor-interacting protein kinase 1/3 (RIPK1/3), p-RIPK3 and mixed lineage kinase domain like (MLKL); these phenomena were attenuated by necrostatin-1(Nec-1) and RIPK3 siRNA...
May 3, 2018: Atherosclerosis
https://www.readbyqxmd.com/read/29771541/plasmodial-kinase-inhibitors-license-to-cure
#17
Diego Gonzalez Cabrera, André Horatscheck, Colin Rylott Wilson, Gregory S Basarab, Charles J Eyermann, Kelly Chibale
Advances in the genetics, function and stage-specificity of Plasmodium kinases has driven robust efforts to identify targets for the design of antimalarial therapies. Reverse genomics following phenotypic screening against Plasmodia or related parasites has uncovered vulnerable kinase targets including PI4K, PKG and GSK-3, an approach bolstered by access to human disease-directed kinase libraries. Alternatively, screening compound libraries against Plasmodium kinases has successfully led to inhibitors with antiplasmodial activity...
May 17, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29769286/targeted-inhibition-of-histone-h3k27-demethylation-is-effective-in-high-risk-neuroblastoma
#18
Timothy L Lochmann, Krista M Powell, Jungoh Ham, Konstantinos V Floros, Daniel A R Heisey, Richard I J Kurupi, Marissa L Calbert, Maninderjit S Ghotra, Patricia Greninger, Mikhail Dozmorov, Madhu Gowda, Andrew J Souers, C Patrick Reynolds, Cyril H Benes, Anthony C Faber
High-risk neuroblastoma is often distinguished by amplification of MYCN and loss of differentiation potential. We performed high-throughput drug screening of epigenetic-targeted therapies across a large and diverse tumor cell line panel and uncovered the hypersensitivity of neuroblastoma cells to GSK-J4, a small-molecule dual inhibitor of lysine 27 of histone 3 (H3K27) demethylases ubiquitously transcribed tetratricopeptide repeat, X chromosome (UTX), and histone demethylase Jumonji D3 (JMJD3). Mechanistically, GSK-J4 induced neuroblastoma differentiation and endoplasmic reticulum (ER) stress, with accompanying up-regulation of p53 up-regulated modulator of apoptosis (PUMA) and induction of cell death...
May 16, 2018: Science Translational Medicine
https://www.readbyqxmd.com/read/29765479/protective-effects-of-evodiamine-in-experimental-paradigm-of-alzheimer-s-disease
#19
Dongmei Wang, Chenying Wang, Ling Liu, Sanqiang Li
Evodiamine, a major component of  Evodia rutaecarpa , has been reported to possess various pharmacological activities, including anti-inflammatory, antioxidative stress, and neuroprotective effects. Our previous study has shown that the potential effects of evodiamine on the learning and memory impairments in the transgenic mouse model of Alzheimer's disease (AD). The present study was designed to investigate neuroprotective mechanism and therapeutic potential of evodiamine against intracerebroventricular streptozotocin (ICV-STZ)-induced experimental sporadic Alzheimer's disease in mice...
June 2018: Cognitive Neurodynamics
https://www.readbyqxmd.com/read/29763908/connexin-43-modulates-osteogenic-differentiation-of-bone-marrow-stromal-cells-through-gsk-3beta-beta-catenin-signaling-pathways
#20
Fei-Xiang Lin, Gui-Zhou Zheng, Bo Chang, Rong-Chun Chen, Qi-Hao Zhang, Peng Xie, Da Xie, Guo-Yong Yu, Qin-Xiao Hu, De-Zhong Liu, Shi-Xin Du, Xue-Dong Li
BACKGROUND/AIMS: Bone marrow stromal cells (BMSCs) are multipotent precursors that give rise to osteoblasts, and contribute directly to bone formation. Connexin 43 (Cx43) is the most ubiquitous gap junction protein expressed in bone cell types, and plays crucial roles in regulating intercellular signal transmission for bone development, differentiation and pathology. However, the precise role and mechanism of Cx43 in BMSCs are less known. Here, we investigate the function of Cx43 in osteogenic differentiation of BMSCs in vitro...
May 10, 2018: Cellular Physiology and Biochemistry
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