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https://www.readbyqxmd.com/read/28635658/asperentin-b-a-new-inhibitor-of-the-protein-tyrosine-phosphatase-1b
#1
Jutta Wiese, Hülya Aldemir, Rolf Schmaljohann, Tobias A M Gulder, Johannes F Imhoff
In the frame of studies on secondary metabolites produced by fungi from deep-sea environments we have investigated inhibitors of enzymes playing key roles in signaling cascades of biochemical pathways relevant for the treatment of diseases. Here we report on a new inhibitor of the human protein tyrosine phosphatase 1B (PTP1B), a target in the signaling pathway of insulin. A new asperentin analog is produced by an Aspergillussydowii strain isolated from the sediment of the deep Mediterranean Sea. Asperentin B (1) contains an additional phenolic hydroxy function at C-6 and exhibits an IC50 value against PTP1B of 2 μM in vitro, which is six times stronger than the positive control, suramin...
June 21, 2017: Marine Drugs
https://www.readbyqxmd.com/read/28625849/leveraging-reciprocity-to-identify-and-characterize-unknown-allosteric-sites-in-protein-tyrosine-phosphatases
#2
Danica S Cui, Victor Beaumont, Patrick S Ginther, James M Lipchock, J Patrick Loria
Drug-like molecules targeting allosteric sites in proteins are of great therapeutic interest, however identification of potential sites is not trivial. A straightforward approach to identify hidden allosteric sites is demonstrated in protein tyrosine phosphatases (PTP) by creation of single alanine mutations in the catalytic acid loop of PTP1B and VHR. This approach relies on the reciprocal interactions between an allosteric site and its coupled orthosteric site. The resulting NMR chemical shift perturbations of each mutant reveal clusters of distal residues affected by acid loop mutation...
June 15, 2017: Journal of Molecular Biology
https://www.readbyqxmd.com/read/28624142/anti-diabetic-xanthones-from-the-bark-of-garcinia-xanthochymus
#3
Chi N Nguyen, Binh T D Trinh, Toan B Tran, Le-Thu T Nguyen, Anna K Jäger, Lien-Hoa D Nguyen
An ethyl acetate extract the bark of Garcinia xanthochymus exhibited strong inhibition towards α-glucosidase and PTP1B with IC50 values of 0.3±0.1μg/mL and 2.3±0.4μg/mL, respectively. Chemical constituents of the extract were therefore examined, and two new compounds, xanthochymusxanthones A (1) and B (2), along with ten known xanthones (3-12), were isolated. Their structures were determined using spectroscopic methods, mainly 1D and 2D NMR. Inhibitory activity of the isolated compounds was then tested, and subelliptenone F (12) showed significant effect towards α-glucosidase with IC50 value of 4...
June 8, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28608833/potential-of-icariin-metabolites-from-epimedium-koreanum-nakai-as-antidiabetic-therapeutic-agents
#4
Da Hye Kim, Hyun Ah Jung, Hee Sook Sohn, Jin Woong Kim, Jae Sue Choi
The therapeutic properties of Epimediumkoreanum are presumed to be due to the flavonoid component icariin, which has been reported to have broad pharmacological potential and has demonstrated anti-diabetic, anti-Alzheimer's disease, anti-tumor, and hepatoprotective activities. Considering these therapeutic properties of icariin, its deglycosylated icaritin and glycosylated flavonoids (icaeriside II, epimedin A, epimedin B, and epimedin C) were evaluated for their ability to inhibit protein tyrosine phosphatase 1B (PTP1B) and α-glucosidase...
June 13, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28592157/correlation-between-nasal-epithelial-injury-and-in-vitro-cytotoxicity-using-a-series-of-small-molecule-protein-tyrosine-phosphatase-1b-inhibitors-investigated-for-reversal-of-leptin-resistance-in-obesity
#5
Alan P Brown, Chandrassegar Saravanan, Patrick Devine, Maria Magnifico, Jiaping Gao, Valerie Beaulieu, Fupeng Ma, Kayo Yasoshima, David Barnes-Seeman, Ken Yamada
This research provides a cautionary example when evaluating changes in behavioral end points with respect to postulated pharmacologic activity. Various small molecule substrate mimetic protein tyrosine phosphatase 1B (PTP1B) inhibitors were investigated as pharmacologic agents for decreasing food consumption using intranasal (IN) dosing as a means for direct nose-to-brain delivery along the olfactory/trigeminal nerve pathways. Although food consumption was decreased in diet-induced obese (DIO) mice, nasal discharge was observed...
January 1, 2017: International Journal of Toxicology
https://www.readbyqxmd.com/read/28585531/small-extracellular-vesicles-secreted-from-senescent-cells-promote-cancer-cell-proliferation-through-epha2
#6
Masaki Takasugi, Ryo Okada, Akiko Takahashi, David Virya Chen, Sugiko Watanabe, Eiji Hara
Cellular senescence prevents the proliferation of cells at risk for neoplastic transformation. However, the altered secretome of senescent cells can promote the growth of the surrounding cancer cells. Although extracellular vesicles (EVs) have emerged as new players in intercellular communication, their role in the function of senescent cell secretome has been largely unexplored. Here, we show that exosome-like small EVs (sEVs) are important mediators of the pro-tumorigenic function of senescent cells. sEV-associated EphA2 secreted from senescent cells binds to ephrin-A1, that is, highly expressed in several types of cancer cells and promotes cell proliferation through EphA2/ephrin-A1 reverse signalling...
June 6, 2017: Nature Communications
https://www.readbyqxmd.com/read/28579122/design-synthesis-in-silico-and-in-vitro-evaluation-of-thiophene-derivatives-a-potent-tyrosine-phosphatase-1b-inhibitor-and-anticancer-activity
#7
Kali Charan Gulipalli, Srinu Bodige, Parameshwar Ravula, Srinivas Endoori, G R Vanaja, G Suresh Babu, J N Narendra Sharath Chandra, Nareshvarma Seelam
A series of novel methyl 4-(4-amidoaryl)-3-methoxythiophene-2-carboxylate derivatives were designed against the active site of protein tyrosine phosphatise 1B (PTP1B) enzyme using MOE.2008.10. These molecules are also subjected for in silico toxicity prediction studies and considering their corresponding drug scores, it implied that, the molecules are promising as anticancer agents. The designed compounds were synthesized by using suitable methods and characterized. They were subjected to inhibitory activity against PTP1B and in vitro anticancer activity by MTT assay...
May 24, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28572573/protein-tyrosine-phosphatase-1b-is-a-mediator-of-cyclic-adp-ribose-induced-ca-2-signaling-in-ventricular-myocytes
#8
Seon-Ah Park, Bing-Zhe Hong, Ki-Chan Ha, Uh-Hyun Kim, Myung-Kwan Han, Yong-Geun Kwak
Cyclic ADP-ribose (cADPR) releases Ca(2+) from ryanodine receptor (RyR)-sensitive calcium pools in various cell types. In cardiac myocytes, the physiological levels of cADPR transiently increase the amplitude and frequency of Ca(2+) (that is, a rapid increase and decrease of calcium within one second) during the cardiac action potential. In this study, we demonstrated that cADPR levels higher than physiological levels induce a slow and gradual increase in the resting intracellular Ca(2+) ([Ca(2+)]i) level over 10 min by inhibiting the sarcoendoplasmic reticulum Ca(2+) ATPase (SERCA)...
June 2, 2017: Experimental & Molecular Medicine
https://www.readbyqxmd.com/read/28569147/serendipitous-discovery-of-light-induced-in-situ-formation-of-an-azo-bridged-dimeric-sulfonated-naphthol-as-a-potent-ptp1b-inhibitor
#9
Robert D Bongard, Michael Lepley, Khushabu Thakur, Marat R Talipov, Jaladhi Nayak, Rachel A Jones Lipinski, Chris Bohl, Noreena Sweeney, Ramani Ramchandran, Rajendra Rathore, Daniel S Sem
BACKGROUND: Protein tyrosine phosphatases (PTPs) like dual specificity phosphatase 5 (DUSP5) and protein tyrosine phosphatase 1B (PTP1B) are drug targets for diseases that include cancer, diabetes, and vascular disorders such as hemangiomas. The PTPs are also known to be notoriously difficult targets for designing inihibitors that become viable drug leads. Therefore, the pipeline for approved drugs in this class is minimal. Furthermore, drug screening for targets like PTPs often produce false positive and false negative results...
May 31, 2017: BMC Biochemistry
https://www.readbyqxmd.com/read/28564652/roux-en-y-gastric-bypass-improves-hepatic-glucose-metabolism-involving-down-regulation-of-protein-tyrosine-phosphatase-1b-in-obese-rats
#10
Song Mu, Jiayu Liu, Wei Guo, Shuping Zhang, Xiaoqiu Xiao, Zhihong Wang, Jun Zhang
OBJECTIVE: This study was initiated to investigate the effects of Roux-en-Y gastric bypass (RYGB) surgery on hepatic glucose metabolism and hepatic expression of protein tyrosine phosphatase 1B (PTP1B) in obese rats. METHODS: Body weight, glucose, intraperitoneal glucose, insulin, and pyruvate tolerance tests were performed pre- and postoperatively, and plasma lipid, insulin and glucagon-like peptide 1 (GLP-1) were measured. The mRNA levels of G6Pase, Pepck, Gsk-3β and Gys-2, and the expression levels of PTP1B mRNA, protein, and other components of the insulin signaling pathway were measured by using RT-PCR and western blotting...
June 1, 2017: Obesity Facts
https://www.readbyqxmd.com/read/28559210/cinnamaldehyde-in-diabetes-a-review-of-pharmacology-pharmacokinetics-and-safety
#11
REVIEW
Ruyuan Zhu, Haixia Liu, Chenyue Liu, Lili Wang, Rufeng Ma, Beibei Chen, Lin Li, Jianzhao Niu, Min Fu, Dongwei Zhang, Sihua Gao
Cinnamaldehyde, one of the active components derived from Cinnamon, has been used as a natural flavorant and fragrance agent in kitchen and industry. Emerging studies have been performed over the past decades to evaluate its beneficial role in management of diabetes and its complications. This review highlights recent advances of cinnamaldehyde in its glucolipid lowering effects, its pharmacokinetics, and its safety by consulting the Pubmed, China Knowledge Resource Integrated, China Science and Technology Journal, National Science and Technology Library, Wanfang Data, and the Web of Science Databases...
May 27, 2017: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/28551626/lipoic-acid-decreases-the-viability-of-breast-cancer-cells-and-activity-of-ptp1b-and-shp2
#12
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
#13
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
#14
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
#15
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
#16
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
#17
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
#18
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
#19
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...
June 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28499188/ptp1b-inhibitors-from-selaginella-tamariscina-beauv-spring-and-their-kinetic-properties-and-molecular-docking-simulation
#20
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...
June 2017: Bioorganic Chemistry
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