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PTP1B

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https://www.readbyqxmd.com/read/28551626/lipoic-acid-decreases-the-viability-of-breast-cancer-cells-and-activity-of-ptp1b-and-shp2
#1
Alicja Kuban-Jankowska, Magdalena Gorska-Ponikowska, Michal Wozniak
BACKGROUND: Protein tyrosine phosphatases PTP1B and SHP2 are potential targets for anticancer therapy, because of the essential role they play in the development of tumors. PTP1B and SHP2 are overexpressed in breast cancer cells, thus inhibition of their activity can be potentially effective in breast cancer therapy. Lipoic acid has been previously reported to inhibit the proliferation of colon, breast and thyroid cancer cells. MATERIALS AND METHODS: We investigated the effect of alpha-lipoic acid (ALA) and its reduced form of dihydrolipoic acid (DHLA) on the viability of MCF-7 cancer cells and on the enzymatic activity of PTP1B and SHP2 phosphatases...
June 2017: Anticancer Research
https://www.readbyqxmd.com/read/28544778/differential-regulation-of-protein-tyrosine-kinase-signaling-by-dock-and-the-ptp61f-variants
#2
Lee F Willoughby, Jan Manent, Kirsten Allan, Han Lee, Marta Portela, Florian Wiede, Coral Warr, Tzu-Ching Meng, Tony Tiganis, Helena E Richardson
Tyrosine phosphorylation-dependent signalling is coordinated by the opposing actions of protein tyrosine kinases (PTKs) and protein tyrosine phosphatases (PTPs). There is a growing list of adaptor proteins that interact with PTPs and facilitate the dephosphorylation of substrates. The extent to which any given adaptor confers selectivity for any given substrate in vivo remains unclear. Here we have taken advantage of Drosophila melanogaster as a model organism to explore the influence of the SH3/SH2 adaptor protein Dock on the abilities of the membrane (PTP61Fm)- and nuclear (PTP61Fn)-targeted variants of PTP61F (the Drosophila othologue of the mammalian enzymes PTP1B and TCPTP respectively) to repress PTK signaling pathways in vivo...
May 23, 2017: FEBS Journal
https://www.readbyqxmd.com/read/28539383/glomerulosclerosis-induced-by-deficiency-of-membrane-associated-guanylate-kinase-inverted-2-in-kidney-podocytes
#3
Naritoshi Shirata, Kan-Ichiro Ihara, Kanae Yamamoto-Nonaka, Takuto Seki, Shin-Ichi Makino, Juan Alejandro Oliva Trejo, Takafumi Miyake, Hiroyuki Yamada, Kirk Nicholas Campbell, Takahiko Nakagawa, Kiyoshi Mori, Motoko Yanagita, Peter Mundel, Katsuhiko Nishimori, Katsuhiko Asanuma
Membrane-associated guanylate kinase inverted 2 (MAGI-2) is a component of the slit diaphragm (SD) of glomerular podocytes. Here, we investigated the podocyte-specific function of MAGI-2 using newly generated podocyte-specific MAGI-2-knockout (MAGI-2-KO) mice. Compared with podocytes from wild-type mice, podocytes from MAGI-2-KO mice exhibited SD disruption, morphologic abnormalities of foot processes, and podocyte apoptosis leading to podocyte loss. These pathologic changes manifested as massive albuminuria by 8 weeks of age and glomerulosclerosis and significantly higher plasma creatinine levels at 12 weeks of age; all MAGI-2-KO mice died by 20 weeks of age...
May 24, 2017: Journal of the American Society of Nephrology: JASN
https://www.readbyqxmd.com/read/28527898/triterpenes-and-meroterpenes-from-ganoderma-lucidum-with-inhibitory-activity-against-hmgs-reductase-aldose-reductase-and-%C3%AE-glucosidase
#4
Baosong Chen, Jin Tian, Jinjin Zhang, Kai Wang, Li Liu, Bo Yang, Li Bao, Hongwei Liu
Seven new compounds including four lanostane triterpenoids, lucidenic acids Q-S (1-3) and methyl ganoderate P (4), and three triterpene-farnesyl hydroquinone conjugates, ganolucinins A-C (5-7), one new natural product ganomycin J (8), and 73 known compounds (9-81) were isolated from fruiting bodies of Ganoderma lucidum. The structures of the compounds 1-8 were determined by spectroscopic methods. Bioactivities of compounds isolated were assayed against HMG-CoA reductase, aldose reductase, α-glucosidase, and PTP1B...
May 17, 2017: Fitoterapia
https://www.readbyqxmd.com/read/28522265/screening-for-bioactive-natural-products-from-a-67-compound-library-of-glycyrrhiza-inflata
#5
Yan Lin, Yi Kuang, Kai Li, Shuang Wang, Wei Song, Xue Qiao, Gulnar Sabir, Min Ye
Licorice shows a variety of pharmacological activities. This work aims to discover bioactive natural products from one botanical source of licorice, Glycyrrhiza inflata. A total of 67 free phenolics were isolated to form a compound library. Based on the bioactivities of licorice, these compounds were screened using cell- or enzyme-based bioassay methods. A total of 11 compounds exhibited potent cytotoxic activities against three human cancer cell lines (HepG2, SW480 and MCF7), while showed little toxicity on human normal cell lines LO2 and HEK293T...
May 6, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28511130/design-synthesis-and-biological-evaluation-of-uncharged-catechol-derivatives-as-selective-inhibitors-of-ptp1b
#6
Xiang-Qian Li, Qi Xu, Jiao Luo, Li-Jun Wang, Bo Jiang, Ren-Shuai Zhang, Da-Yong Shi
Protein tyrosine phosphatases 1B (PTP1B) is a promising and validated therapeutic target to effectively treat T2DM and obesity. However, the development of charged PTP1B inhibitors was restricted due to their low cell permeability and poor bioavailability. Based on active natural products, two series of uncharged catechol derivatives were identified as PTP1B inhibitors by targeting a secondary aryl phosphate-binding site as well as the catalytic site. The most potent inhibitor 22 showed an IC50 of 0.487 μM against PTP1B and strong selectivity (27-fold) over TCPTP...
May 3, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28508666/biotransformation-of-total-coumarins-of-radix-glehniae-by-lecanicillium-attenuatum-w-1-9
#7
Qi Dong, Ye Yuan, Yue Zhou, Yi-Xin Zhang, Jian-Peng Zhang, Hao-Bing Yu, Bing-Hua Jiao, Xiao-Yu Liu, Xiao-Ling Lu
The biotransformation of total coumarins of Radix Glehniae by Lecanicillium attenuatum W-1-9 yielded three new products, lecaniside A (1), lecaniside B (2), and lecaniside C (3). The chemical structures of these metabolites were elucidated based on extensive spectral data, including 2D NMR and HRMS. The hydrogenation, dealkylation, glycosylation, and O-methylation reactions of these metabolites were observed in the present study. In the in vitro assays, compound 1 displayed a little PTP1B inhibitory activity...
May 16, 2017: Journal of Asian Natural Products Research
https://www.readbyqxmd.com/read/28499190/ellagitannin-and-flavonoid-constituents-from-agrimonia-pilosa-ledeb-with-their-protein-tyrosine-phosphatase-and-acetylcholinesterase-inhibitory-activities
#8
Duc Hung Nguyen, U Min Seo, Bing Tian Zhao, Duc Dat Le, Su Hui Seong, Jae Sue Choi, Byung Sun Min, Mi Hee Woo
A new ellagitannin, agritannin (1), a new flavone glycoside, agriflavone (2), and another flavone glycoside with spectroscopic data reported for the first time, kaempferol-3-O-[(S)-3-hydroxy-3-methylglutaryl (1→6)]-β-d-glucoside (3), along with 16 known compounds were isolated from the aerial parts of Agrimonia pilosa Ledeb. These compounds were evaluated for PTP1B inhibitory activity. Among them, compounds 9 and 18 displayed potential inhibitory activity against PTP1B with IC50 values of 7.14±1.75 and 7...
April 30, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28499188/ptp1b-inhibitors-from-selaginella-tamariscina-beauv-spring-and-their-kinetic-properties-and-molecular-docking-simulation
#9
Duc Dat Le, Duc Hung Nguyen, Bing Tian Zhao, Su Hui Seong, Jae Sue Choi, Seok Kyu Kim, Jeong Ah Kim, Byung Sun Min, Mi Hee Woo
Diabetes is one of the most popular worldwide diseases, regulated by the defects in insulin secretion, insulin action, or both. The overexpression of protein tyrosine phosphatase 1B (PTP1B) was found to down-regulate the insulin-receptor activation. PTP1B has been known as a strategy for the treatment of diabetes via the regulation of insulin signal transduction pathway. Herein, we investigated the PTP1B inhibitors isolated from natural sources. The chemical investigation of Selaginella tamariscina (Beauv.) Spring revealed seven unsaturated alkynyl phenols 1-7, four new selaginellins T-W 1-4 together with three known compounds 5-7 isolated from the aerial parts...
May 2, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28497962/potential-of-polygonum-cuspidatum-root-as-an-antidiabetic-food-dual-high-resolution-%C3%AE-glucosidase-and-ptp1b-inhibition-profiling-combined-with-hplc-hrms-and-nmr-for-identification-of-antidiabetic-constituents
#10
Yong Zhao, Martin Xiaoyong Chen, Kenneth Thermann Kongstad, Anna Katharina Jäger, Dan Staerk
The worldwide increasing incidence of type 2 diabetes has fueled an intensified search for food and herbal remedies with preventive and/or therapeutic properties. Polygonum cuspidatum Siebold & Zucc. (Polygonaceae) is used as a functional food in Japan and South Korea, and it is also a well-known traditional antidiabetic herb used in China. In this study, dual high-resolution α-glucosidase and protein-tyrosine phosphatase 1B (PTP1B) inhibition profiling was used for the identification of individual antidiabetic constituents directly from the crude ethyl acetate extract and fractions of P...
May 24, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28492548/inhibition-of-ptp1b-disrupts-cell-cell-adhesion-and-induces-anoikis-in-breast-epithelial-cells
#11
Bylgja Hilmarsdottir, Eirikur Briem, Skarphedinn Halldorsson, Jennifer Kricker, Sævar Ingthorsson, Sigrun Gustafsdottir, Gunhild M Mælandsmo, Magnus K Magnusson, Thorarinn Gudjonsson
Protein tyrosine phosphatase 1B (PTP1B) is a well-known inhibitor of insulin signaling pathways and inhibitors against PTP1B are being developed as promising drug candidates for treatment of obesity. PTP1B has also been linked to breast cancer both as a tumor suppressor and as an oncogene. Furthermore, PTP1B has been shown to be a regulator of cell adhesion and migration in normal and cancer cells. In this study, we analyzed the PTP1B expression in normal breast tissue, primary breast cells and the breast epithelial cell line D492...
May 11, 2017: Cell Death & Disease
https://www.readbyqxmd.com/read/28479249/ptp1b-deficiency-improves-hypothalamic-insulin-sensitivity-resulting-in-the-attenuation-of-agrp-mrna-expression-under-high-fat-diet-conditions
#12
Mariko Sugiyama, Ryoichi Banno, Akira Mizoguchi, Takashi Tominaga, Taku Tsunekawa, Takeshi Onoue, Daisuke Hagiwara, Yoshihiro Ito, Yoshiaki Morishita, Shintaro Iwama, Motomitsu Goto, Hidetaka Suga, Hiroshi Arima
Hypothalamic insulin receptor signaling regulates energy balance and glucose homeostasis via agouti-related protein (AgRP). While protein tyrosine phosphatase 1B (PTP1B) is classically known to be a negative regulator of peripheral insulin signaling by dephosphorylating both insulin receptor β (IRβ) and insulin receptor substrate, the role of PTP1B in hypothalamic insulin signaling remains to be fully elucidated. In the present study, we investigated the role of PTP1B in hypothalamic insulin signaling using PTP1B deficient (KO) mice in vivo and ex vivo...
June 17, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28473201/a-strategy-based-on-gas-chromatography-mass-spectrometry-and-virtual-molecular-docking-for-analysis-and-prediction-of-bioactive-composition-in-natural-product-essential-oil
#13
Haiyang Wang, Dongyu Gu, Miao Wang, Hong Guo, Huijuan Wu, Guangliang Tian, Qian Li, Yi Yang, Jing Tian
The discovery of leads from medicinal plants is crucial to drug development. The present study presents a strategy based on GC-MS coupled with molecular docking for analysis, identification and prediction of protein tyrosine phosphatase 1B inhibitors in the essential oil from Himalayan Cedar (HC). The essential oil with IC50 value of 120.71±0.26μg/mL exhibited potential activity against protein tyrosine phosphatase 1B (PTP1B) in vitro. After GC-MS analysis, 35 compounds were identified from this oil. The identified compounds were individually docked with PTP1B...
April 15, 2017: Journal of Chromatography. A
https://www.readbyqxmd.com/read/28455143/ire1%C3%AE-links-nck1-deficiency-to-attenuated-ptp1b-expression-in-hepg2-cells
#14
Hui Li, Bing Li, Louise Larose
PTP1B, a prototype of the non-receptor subfamily of the protein tyrosine phosphatase superfamily, plays a key role in regulating intracellular signaling from various receptor and non-receptor protein tyrosine kinases. Previously, we reported that silencing Nck1 in human hepatocellular carcinoma HepG2 cells enhances basal and growth factor-induced activation of the PI3K-Akt pathway through attenuating PTP1B expression. However, the underlying mechanism by which Nck1 depletion represses PTP1B expression remains unclear...
April 25, 2017: Cellular Signalling
https://www.readbyqxmd.com/read/28454670/structure-related-protein-tyrosine-phosphatase-1b-inhibition-by-naringenin-derivatives
#15
Hyun Ah Jung, Pradeep Paudel, Su Hui Seong, Byung-Sun Min, Jae Sue Choi
Naturally occurring flavonoids co-exist as glycoside conjugates, which dominate aglycones in their content. To unveil the structure-activity relationship of a naturally occurring flavonoid, we investigated the effects of the glycosylation of naringenin on the inhibition of enzyme systems related to diabetes (protein tyrosine phosphatase 1B (PTP1B) and α-glycosidase) and on glucose uptake in the insulin-resistant state. Among the tested naringenin derivatives, prunin, a single-glucose-containing flavanone glycoside, potently inhibited PTP1B with an IC50 value of 17...
April 18, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28447469/two-pairs-of-rare-naturally-occurring-4-hydroxy-4-methyl-2-5-heptanedione-derivatives-from-the-red-alga-chondria-crassicaulis
#16
Lin Tong, Yi Zhang, Ai-Hong Liu, Li-Gong Yao, Yue-Wei Guo, Shui-Chun Mao, Bin Wang
Two pairs of rare naturally occurring racemic lipids, (±)-4,7-dihydroxy-4-methyl-2,5-heptanedione (1), and (±)-7-butoxy-4-hydroxy-4-methyl-2,5-heptanedione (2) were isolated from the red alga Chondria crassicaulis Harv. The structures of the racemic mixtures of 1 and 2 were elucidated by detailed spectroscopic techniques, including 1D and 2D NMR ((1)H and (13)C NMR, (1)H-(1)H COSY, HSQC, and HMBC) as well as mass spectrometry and optical rotation experiments, and by comparison with data for related known analogs...
April 27, 2017: Journal of Asian Natural Products Research
https://www.readbyqxmd.com/read/28436691/concise-synthesis-and-ptp1b-inhibitory-activity-of-r-and-s-dihydroresorcylide
#17
Cheng-Shi Jiang, Li Zhang, Jing-Xu Gong, Jing-Ya Li, Li-Gong Yao, Jia Li, Yue-Wei Guo
The present study was designed to develop a concise synthetic route for macrolide, with the purpose of confirming the absolute configuration of natural dihydroresorcylide (1) and making it more easily accessible for biological evaluation. The absolute configuration of C-3 in natural 1 was revised to be R by comparison of the rotation sign of synthetic (R)- and (S)-1. The synthetic (R)-1 was found to be a novel highly specific PTP1B inhibitor with an IC50 value of 17.06 μM.
April 24, 2017: Journal of Asian Natural Products Research
https://www.readbyqxmd.com/read/28411010/effects-of-vitamin-d-and-resveratrol-on-metabolic-associated-markers-in-liver-and-adipose-tissue-from-samp8-mice
#18
Yehua Rui, Jinbo Cheng, Liqiang Qin, Cheng Shan, Jie Chang, Guiping Wang, Zhongxiao Wan
SAMP8 mice exhibit multiple metabolic characteristics associated with age, and it is a suitable candidate for researching aging associated metabolic dysfunction. OBJECTIVES: We aimed to 1) explore how key metabolic markers will be altered in both liver and adipose tissue with aging in SAMP8 mice; and 2) how the combination of vitamin D (VD) with resveratrol (RSV) will affect aging associated metabolic impairment in liver and adipose tissue from SAMP8 mice. METHODS: SAMP8 mice and their control SAMR1 mice were divided into 5 groups, i...
July 2017: Experimental Gerontology
https://www.readbyqxmd.com/read/28403933/knocking-down-amygdalar-ptp1b-in-diet-induced-obese-rats-improves-insulin-signaling-action-decreases-adiposity-and-may-alter-anxiety-behavior
#19
Natalia Ferreira Mendes, Gisele Castro, Dioze Guadagnini, Natalia Tobar, Susana Quiros Cognuck, Lucila Leico Kagohara Elias, Patricia Aline Boer, Patricia Oliveira Prada
OBJECTIVE: Protein tyrosine phosphatase 1B (PTP1B) has been extensively implicated in the regulation of body weight, food intake, and energy expenditure. The role of PTP1B appears to be cell and brain region dependent. RESULTS: Herein, we demonstrated that chronic high-fat feeding enhanced PTP1B expression in the central nucleus of the amygdala (CeA) of rats compared to rats on chow. Knocking down PTP1B with oligonucleotide antisense (ASO) decreased its expression and was sufficient to improve the anorexigenic effect of insulin through IR/Akt signaling in the CeA...
May 2017: Metabolism: Clinical and Experimental
https://www.readbyqxmd.com/read/28400224/new-amides-from-seeds-of-silybum-marianum-with-potential-antioxidant-and-antidiabetic-activities
#20
Ning-Bo Qin, Cui-Cui Jia, Jun Xu, Da-Hong Li, Fan-Xing Xu, Jiao Bai, Zhan-Lin Li, Hui-Ming Hua
Two new amide compounds, mariamides A and B (1-2), were obtained together with fourteen known compounds from the seeds of milk thistle (Silybum marianum). Their structures were established on the basis of extensive 1D and 2D NMR analyses, as well as HR-ESI-MS data. Most of the compounds showed significant antioxidant activities than positive control in ABTS and FRAP assays. However, only amide compounds 1-4 showed moderate DPPH radical scavenging activity and compounds 7 and 16 showed the most potent activity against DPPH...
April 8, 2017: Fitoterapia
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