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PTP1B

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https://www.readbyqxmd.com/read/28323380/sarcophytrols-g-l-novel-minor-metabolic-components-from-south-china-sea-soft-coral-sarcophyton-trocheliophorum-marenzeller
#1
Lin-Fu Liang, Wen-Ting Chen, Ernesto Mollo, Li-Gong Yao, He-Yao Wang, Wei Xiao, Yue-Wei Guo
Minor metabolic components, six new cembranoids sarcophytrols G - L (1 - 6) along with two known related analogues 7 and 8, were isolated from the South China Sea soft coral Sarcophyton trocheliophorum. Their structures were elucidated by extensive spectroscopic analyses (1D- and 2D-NMR, and ESI-MS.) as well as comparison with literature data. As part of our ongoing research project for discovering bioactive substances from Chinese marine invertebrates, compounds 1 - 8 were tested for their inhibitory activity against protein tyrosine phosphatase 1B (PTP1B), a key target for the treatment of Type-II diabetes and obesity...
March 21, 2017: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/28322990/xanthones-from-the-twigs-of-garcinia-oblongifolia-and-their-antidiabetic-activity
#2
Binh T D Trinh, Tam T T Quach, Dung N Bui, Dan Staerk, Lien-Hoa D Nguyen, Anna K Jäger
Three new xanthones, oblongixanthone F-H (1-3), along with eight known xanthones (4-11), were isolated from an EtOAc extract of the twigs of Garcinia oblongifolia. Their structures were elucidated by spectroscopic analysis including 1D- and 2D-NMR spectroscopy and mass spectrometry. The antidiabetic effects of all isolated compounds were evaluated by in vitro α-glucosidase and PTP1B inhibition assays. Compound 11 was the most active compound, and inhibited α-glucosidase and PTP1B with IC50 values of 1.7±0...
March 16, 2017: Fitoterapia
https://www.readbyqxmd.com/read/28318895/competitive-protein-tyrosine-phosphatase-1b-ptp1b-inhibitors-prenylated-caged-xanthones-from-garcinia-hanburyi-and-their-inhibitory-mechanism
#3
Xue Fei Tan, Zia Uddin, Chanin Park, Yeong Hun Song, Minky Son, Keun Woo Lee, Ki Hun Park
Protein tyrosine phosphatase 1B (PTP1B) plays important role in diabetes, obesity and cancer. The methanol extract of the gum resin of Garcinia hanburyi (G. hanburyi) showed potent PTP1B inhibition at 10µg/ml. The active compounds were identified as prenylated caged xanthones (1-9) which inhibited PTP1B in dose-dependent manner. Carboxybutenyl group within caged motif (A ring) was found to play a critical role in enzyme inhibition such as 1-6 (IC50s=0.47-4.69µM), whereas compounds having hydroxymethylbutenyl 7 (IC50=70...
March 6, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28294503/exploring-protein-structure-and-dynamics-through-a-project-oriented-biochemistry-laboratory-module
#4
James M Lipchock, Patrick S Ginther, Bonnie B Douglas, Kelly E Bird, J Patrick Loria
Here, we present a 10-week project-oriented laboratory module designed to provide a course-based undergraduate research experience in biochemistry that emphasizes the importance of biomolecular structure and dynamics in enzyme function. This module explores the impact of mutagenesis on an important active site loop for a biomedically-relevant human enzyme, protein tyrosine phosphatase 1B (PTP1B). Over the course of the semester students guide their own mutant of PTP1B from conception to characterization in a cost-effective manner and gain exposure to fundamental techniques in biochemistry, including site-directed DNA mutagenesis, bacterial recombinant protein expression, affinity column purification, protein quantitation, SDS-PAGE, and enzyme kinetics...
March 13, 2017: Biochemistry and Molecular Biology Education
https://www.readbyqxmd.com/read/28272165/reduced-insulin-resistance-contributes-to-the-beneficial-effect-of-protein-tyrosine-phosphatase-1b-deletion-in-a-mouse-model-of-sepsis
#5
Eugénie Delile, Rémi Nevière, Pierre-Alain Thiébaut, Julie Maupoint, Paul Mulder, David Coquerel, Sylvanie Renet, Jennifer Rieusset, Vincent Richard, Fabienne Tamion
Hyperglycemia is a common feature of septic patients and has been associated with poor outcome and high mortality. In contrast, insulin has been shown to decrease mortality and to prevent the incidence of multi-organ failure but is often associated with deleterious hypoglycemia. Protein Tyrosine Phosphatase 1B (PTP1B) is a negative regulator of both insulin signaling and NO production, and has been shown to be an aggravating factor in septic shock. To evaluate the potential therapeutic effect of PTP1B blockade on glucose metabolism and insulin resistance in an experimental model of sepsis, we assessed the effect of PTP1B gene deletion in a cecal ligation and puncture (CLP) model of sepsis...
March 7, 2017: Shock
https://www.readbyqxmd.com/read/28261970/inhibitors-of-protein-tyrosine-phosphatase-1b-from-marine-natural-products
#6
REVIEW
Yue Zhou, Weirui Zhang, Xiaoyu Liu, Haobing Yu, Xiaoling Lu, Binghua Jiao
The ocean is a huge treasure trove of natural products, from where 11 drugs has been developed for various diseases. (Table 1).Protein tyrosine phosphatase 1B (PTP1B) belongs to the protein tyrosine phosphatase family, which specifically hydrolyses the aromatic phosphate. On one hand, in insulin signaling, it plays a key role as a negative regulator through dephosphorylating activated insulin receptor (IR) and insulin receptor substrate (1IRS-1) This article is protected by copyright. All rights reserved.
March 6, 2017: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/28250350/aglaiabbrevins-a-d-new-prenylated-bibenzyls-from-the-leaves-of-aglaia-abbreviata-with-potent-ptp1b-inhibitory-activity
#7
Pan Sun, Chang-Sheng Jiang, Yi Zhang, Ai-Hong Liu, Tong-Jun Liang, Jia Li, Yue-Wei Guo, Jian-Mei Jiang, Shui-Chun Mao, Bin Wang
Four new prenylated bibenzyls, named aglaiabbrevins A-D (2, 4-6), were isolated from the leaves of Aglaia abbreviata, along with two known related analogues, 3,5-dihydroxy-2-[3,7-dimethyl-2(E),6-octadienyl]bibenzyl (7) and 3,5-dihydroxy-2-(3-methyl-2-butenyl)bibenzyl (8). The structures of the new compounds were elucidated on the basis of extensive spectroscopic experiments, mainly one and two dimensional (1D- and 2D)-NMR, and the absolute configuration of 5 was determined by the measurement of specific rotation...
2017: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28229972/early-life-stress-experience-may-blunt-hypothalamic-leptin-signalling
#8
J H Lee, S B Yoo, J Y Kim, J Y Lee, B T Kim, K Park, J W Jahng
The aim of this study was to investigate whether neonatal maternal separation (MS) - chronic stress experience in early life - affects the anorectic efficacy of leptin in the offspring at adolescence. Sprague-Dawley pups were separated from the dam daily for 3 h during postnatal day 1-14 or left undisturbed as non-handled controls (NH). NH and MS male pups received an intraperitoneal leptin (100 μg/kg) or saline on postnatal day (PND) 28, and then food intake and body weight gain were recorded. The hypothalamic levels of leptin-signalling-related genes, phosphorylated signal transducer and activator of transcription-3 (pSTAT3) and protein-tyrosine phosphatase 1B (PTP1B) were examined at 40 min after a single injection of leptin on PND 39 by immunohistochemistry and Western blot analysis...
March 2017: Journal of Biosciences
https://www.readbyqxmd.com/read/28228082/recent-advances-in-protein-tyrosine-phosphatase-1b-targeted-drug-discovery-for-type-ii-diabetes-and-obesity
#9
Neelesh Maheswari, Chandrabose Karthikeyan, Piyush Trivedi, N S Hari Narayana Moorthy
Protein tyrosine phosphatase 1B (PTP1B) is an important therapeutic target for type II diabetes and obesity because of its pivotal role as a negative modulator in both insulin and leptin signalling pathways. Consequently, the discovery of PTP1B inhibitors has been the focus of researchers in both academia and pharmaceutical industry over the last two decades. Though, intense pharmaceutical research in this area has resulted in many potent PTP1B inhibitors, a vast majority of them possessed pTyr mimetic group such as phosphonates, carboxylic acids and sulphamic acids, which led to poor PTP1B selectivity and insufficient in vivo efficacy due to low cell permeability and bioavailability...
February 22, 2017: Current Drug Targets
https://www.readbyqxmd.com/read/28216905/green-biosynthesis-characterization-in-vitro-antidiabetic-activity-and-investigational-acute-toxicity-studies-of-some-herbal-mediated-silver-nanoparticles-on-animal-models
#10
Kalakotla Shanker, Gottumukkala Krishna Mohan, Md Ashwaq Hussain, Naradala Jayarambabu, Poka Lakshmi Pravallika
Diabetes is a metabolic disorder characterized by hyperglycemia, altered carbohydrate, lipid and protein metabolism. In recent studies, Nanoscience and nanotechnology are blazing fields for researchers; for researchers; of late there has been a prodigious excitement in the field of nanopharmacology to study silver nanoparticle (SNP) synthesis using natural products. Biological methods have been used to synthesize SNPs using medicinally active plants having an antidiabetic role, and this made us to assess the biologically synthesized SNPs from the seed extract of Psoralea corylifolia using 1 mM silver nitrate solution...
January 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/28212750/conformational-rigidity-and-protein-dynamics-at-distinct-timescales-regulate-ptp1b-activity-and-allostery
#11
Meng S Choy, Yang Li, Luciana E S F Machado, Micha B A Kunze, Christopher R Connors, Xingyu Wei, Kresten Lindorff-Larsen, Rebecca Page, Wolfgang Peti
Protein function originates from a cooperation of structural rigidity, dynamics at different timescales, and allostery. However, how these three pillars of protein function are integrated is still only poorly understood. Here we show how these pillars are connected in Protein Tyrosine Phosphatase 1B (PTP1B), a drug target for diabetes and cancer that catalyzes the dephosphorylation of numerous substrates in essential signaling pathways. By combining new experimental and computational data on WT-PTP1B and ≥10 PTP1B variants in multiple states, we discovered a fundamental and evolutionarily conserved CH/π switch that is critical for positioning the catalytically important WPD loop...
February 16, 2017: Molecular Cell
https://www.readbyqxmd.com/read/28209599/role-of-shp2-protein-tyrosine-phosphatase-in-sert-inhibition-by-enteropathogenic-e-coli-epec
#12
Megha Singhal, Christopher Manzella, Vinay Soni, Waddah A Alrefai, Seema Saksena, Gail A Hecht, Pradeep K Dudeja, Ravinder K Gill
Enteropathogenic E. coli (EPEC), one of the diarrheagenic E. coli pathotypes, is among the most important food-borne pathogens infecting children worldwide. Inhibition of serotonin transporter (SERT), that regulates extracellular availability of serotonin (5-HT), has been previously implicated in EPEC-associated diarrhea. EPEC was shown to inhibit SERT via activation of protein tyrosine phosphatases (PTPase), albeit the specific PTPase involved is not known. Current studies aimed to identify EPEC activated PTPase and its role in SERT inhibition...
February 16, 2017: American Journal of Physiology. Gastrointestinal and Liver Physiology
https://www.readbyqxmd.com/read/28202316/an-epigenetic-modifier-induces-production-of-10-s-verruculide-b-an-inhibitor-of-protein-tyrosine-phosphatases-by-phoma-sp-nov-lg0217-a-fungal-endophyte-of-parkinsonia-microphylla
#13
Juliana R Gubiani, E M Kithsiri Wijeratne, Taoda Shi, Angela R Araujo, A Elizabeth Arnold, Eli Chapman, A A Leslie Gunatilaka
Incorporation of the histone deacetylase (HDAC) inhibitor, suberoylanilide hydroxamic acid (SAHA), to a culture broth of the endophytic fungus Phoma sp. nov. LG0217 isolated from Parkinsonia microphylla changed its metabolite profile and resulted in the production of (10'S)-verruculide B (1), vermistatin (2) and dihydrovermistatin (3). When cultured in the absence of the epigenetic modifier, it produced a new metabolite, (S,Z)-5-(3',4'-dihydroxybutyldiene)-3-propylfuran-2(5H)-one (4) together with nafuredin (5)...
March 15, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28199951/a-dioxidovanadium-v-complex-of-nno-donor-schiff-base-as-a-selective-inhibitor-of-protein-tyrosine-phosphatase-1b-synthesis-characterization-and-biological-activities
#14
Yuqi Jia, Liping Lu, Miaoli Zhu, Caixia Yuan, Shu Xing, Xueqi Fu
A new dioxidovanadium (V) complex, VO2(HPPCH) (1) (H2PPCH = N'-picolinoylpyridin-1-ium-2-carbohydrazonate) has been synthesized and characterized by elemental analysis, IR, X-ray diffraction analysis and electrospray ionization mass spectra. Complex 1 crystallized in the monoclinic system with space group P21/c. It potently inhibited PTP1B with IC50 of 0.13 μM, about 7, 15 and 125-fold stronger against PTP1B than over TCPTP, SHP-1 and SHP-2, displaying obvious selectivity against PTP1B. Western blotting analysis indicated that complex 1 effectively increased the phosphorylation of PTP1B substrates, especially the phosphorylation of IR/IGF 1R and IRS-1...
February 6, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28199837/an-endosomal-naadp-sensitive-two-pore-ca-2-channel-regulates-er-endosome-membrane-contact-sites-to-control-growth-factor-signaling
#15
Bethan S Kilpatrick, Emily R Eden, Leanne N Hockey, Elizabeth Yates, Clare E Futter, Sandip Patel
Membrane contact sites are regions of close apposition between organelles that facilitate information transfer. Here, we reveal an essential role for Ca(2+) derived from the endo-lysosomal system in maintaining contact between endosomes and the endoplasmic reticulum (ER). Antagonizing action of the Ca(2+)-mobilizing messenger NAADP, inhibiting its target endo-lysosomal ion channel, TPC1, and buffering local Ca(2+) fluxes all clustered and enlarged late endosomes/lysosomes. We show that TPC1 localizes to ER-endosome contact sites and is required for their formation...
February 14, 2017: Cell Reports
https://www.readbyqxmd.com/read/28197094/protein-tyrosine-phosphatase-1b-ptp1b-a-potential-target-for-alzheimer-s-therapy
#16
Marcelo N N Vieira, Natalia M Lyra E Silva, Sergio T Ferreira, Fernanda G De Felice
Despite significant advances in current understanding of mechanisms of pathogenesis in Alzheimer's disease (AD), attempts at drug development based on those discoveries have failed to translate into effective, disease-modifying therapies. AD is a complex and multifactorial disease comprising a range of aberrant cellular/molecular processes taking part in different cell types and brain regions. As a consequence, therapeutics for AD should be able to block or compensate multiple abnormal pathological events. Here, we examine recent evidence that inhibition of protein tyrosine phosphatase 1B (PTP1B) may represent a promising strategy to combat a variety of AD-related detrimental processes...
2017: Frontiers in Aging Neuroscience
https://www.readbyqxmd.com/read/28189086/pterocarpan-scaffold-a-natural-lead-molecule-with-diverse-pharmacological-properties
#17
REVIEW
Chelliah Selvam, Brian C Jordan, Sandhya Prakash, Daniel Mutisya, Ramasamy Thilagavathi
Phytoalexins are substances produced by plants that act as potent inhibitors of pathogens. Pterocarpans are biologically active isoflavonoids most commonly found in the family Fabaceae that have the ability to act as phytoalexins. It is made up of a tetracyclic ring system possessing benzofuran-benzopyran. A very great number of pterocarpans have been isolated from natural sources and they are proved to have significant biological activities such as anti-microbial, anti-cancerous, anti-inflammatory and anti-malarial activities...
January 17, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28173704/structural-and-stereochemical-studies-of-laurokamurols-a-c-uncommon-bis-sesquiterpenoids-from-the-chinese-red-alga-laurencia-okamurai-yamada
#18
Xiao-Lu Li, Tibor Kurtán, Jun-Chi Hu, Attila Mándi, Jia Li, Xu-Wen Li, Yue-Wei Guo
Three novel heterodimeric laurane-type sesquiterpenoids, laurokamurols A-C (1-3), along with eight known related monomeric ones (4-11) were isolated from the East China Sea red alga Laurencia okamurai Yamada. The absolute configurations of the new bis-sesquitepenoids, especially their axial chirality, were determined by extensive spectroscopic analyses and TDDFT-ECD method. All of the new compounds showed promising PTP1B inhibitory activities with IC50 values comparable to the positive control, indicating them as potential food additives or pharmaceutical drug leads toward obesity or diabetes...
February 16, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28140583/glycybridins-a-k-bioactive-phenolic-compounds-from-glycyrrhiza-glabra
#19
Kai Li, Shuai Ji, Wei Song, Yi Kuang, Yan Lin, Shunan Tang, Zexu Cui, Xue Qiao, Siwang Yu, Min Ye
In an attempt to discover bioactive agents from the herbal medicine Glycyrrhiza glabra (widely known as licorice), 11 new phenolic compounds, glycybridins A-K (1-11), along with 47 known phenolics (12-58) were isolated. Their structures were elucidated on the basis of extensive NMR and MS analyses as well as experimental and computed ECD data. According to the clinical therapeutic effects of licorice, enzyme or cell-based bioactivity screenings of 1-58 were conducted. A number of compounds significantly activate Nrf2, inhibit tyrosinase or PTP1B, inhibit LPS-induced NO production and NF-κB transcription, and inhibit the proliferation of human cancer cells (HepG2, SW480, A549, MCF7)...
February 24, 2017: Journal of Natural Products
https://www.readbyqxmd.com/read/28126289/synthesis-biological-evaluation-and-in-silico-studies-of-5-3-methoxybenzylidene-thiazolidine-2-4-dione-analogues-as-ptp1b-inhibitors
#20
Manoj Kumar Mahapatra, Rajnish Kumar, Manoj Kumar
PTP1B (protein tyrosine phosphatase 1B) dephosphorylates the insulin receptor substrate and thus acts as a negative regulator of the insulin and leptin signalling pathway. Recently, it has been considered as a new therapeutic target of intervention for the treatment of type2 diabetes. A series of aryl/alkylsulfonyloxy-5-(3-methoxybenzylidene)thiazolidine-2,4-dione derivatives were synthesized, screened in vitro for their PTP1B inhibitory activity and in vivo for anti-hyperglycaemic activity. Docking results further helped in understanding the nature of interactions governing the binding mode of ligands inside the active site of PTP1B...
January 17, 2017: Bioorganic Chemistry
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