PTP1B inhibitors
Synthesis and Evaluation of Benzimidazole Derivatives as Protein Tyrosine Phosphatase (PTP1B) Inhibitors
... include PTP1B, LAR, PTPa and SHP-2. Among these, PTP1B has been most intensively studied as a target for the development of inhibitors aiming at the treatment of type 2 diabetes and ...with ...
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Molecular docking studies of quinoline 3 carbohydrazide as novel PTP1B inhibitors as potential antihyperglycemic agents
... 1B) inhibitors have been identified by molecular modeling ...these inhibitors with PTP 1B enzyme. As per our literature, we found that PTP1B is highly ...potent PTP1B inhibitors as ...
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Pharmacological inhibition of protein tyrosine phosphatase 1B protects against atherosclerotic plaque formation in the LDLR −/− mouse model of atherosclerosis
... chronic PTP1B inhibitor (trodusquemine) treatment of LDLR -/- mice decreased weight gain and adiposity, improved glucose homeostasis and attenuated atherosclerotic plaque ...that PTP1B inhibitors ...
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Effects of hepatic protein tyrosine phosphatase 1B and methionine restriction on hepatic and whole-body glucose and lipid metabolism in mice.
... of Ptp1b from birth results in improved glucose homeostasis caused by enhanced hepatic insulin signaling [2] and tamoxifen-inducible hepatic Ptp1b knockdown in adult mice leads to the reversal of high-fat ...
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PTP1B: a new therapeutic target for Rett syndrome
... in PTP1B inhibitors as antidiabetic drugs over the past 15 years, few compounds have progressed to clinical trials, and so far none of these have advanced beyond phase II ...PTP inhibitors were ...
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Chimeric design, synthesis, and biological assays of a new nonpeptide insulin-mimetic vanadium compound to inhibit protein tyrosine phosphatase 1B
... ous solution, in presence or absence of sodium citrate as a biologically relevant and ubiquitous chelator, TSAG0101 undergoes neither ligand exchange nor reduction of its central vanadium atom during 24 hours. TSAG0101 ...
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Volume 4 | Issue 1 - 2014
... phosphatase, PTP1B, in liver leads to a host of improvements in metabolic parameters, including improved hepatic insulin sensitivity, reduced liver triglycerides, lower serum and hepatic cholesterol levels, and ...
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Dataset on the kinetics of the inhibition of PTP1B by the flavonoids and pheophytin A from Allophylus cominia
... The data presented in this article are related to the research article under the title “in vitro anti-diabetic activity of flavonoids and pheophytins from Allophylus cominia Sw. on PTP1B, DPPIV, alpha- glucosidase ...
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Synthesis, Antimicrobial Study and Molecular Docking Simulation of 3,4-Dimethoxy-β-nitrostyrene Derivatives as Candidate of PTP1B Inhibitor
... of PTP1B inhibitory mechanisms, several classes of synthetic compounds and natural products have been characterized for developing as therapeutic agents ...selective PTP1B inhibitors that possesses ...
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Evaluation of 147 Kampo prescriptions as novel protein tyrosine phosphatase 1B (PTP1B) inhibitory agents
... [9]. PTP1B inhibition has been shown in vivo to increase insulin and leptin activity and results in normalized blood glucose levels and reduced adiposity ...addition, PTP1B inhibition may protect against ...
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In vitro anti-diabetic activity of flavonoids and pheophytins from Allophylus cominia Sw . on PTP1B, DPPIV, alpha-glucosidase and alpha-amylase enzymes
... DPPIV inhibitors to improve glucose control in T2-DM, has led to the examination of natural products with DPPIV inhibitory properties (Mardanyan et ...of PTP1B enzyme with Ki values of ...of PTP1B ...
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Ion channel TRPV1 dependent activation of PTP1B suppresses EGFR associated intestinal tumorigenesis
... Functional PTP1B activity was previously reported to medi- ate differential responses to ligand-induced activation versus transactivation of the EGFR in IEC lines ...of PTP1B in primary IECs is unknown. We ...
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A novel role for protein tyrosine phosphatase 1B as a positive regulator of neuroinflammation
... which PTP1B potentiated the LPS-induced inflammatory activation of ...of PTP1B in microglia because Src has a negative regula- tory phosphorylation site (tyrosine 527, ...Y527). PTP1B may ...
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Nck1 depletion induces activation of the PI3K/Akt pathway by attenuating PTP1B protein expression
... that PTP1B pro- tein levels are drastically decreased in Nck1-depleted HepG2 cells and liver of Nck1 −/− ...that PTP1B −/− mice fed a NCD or HFD, both display significantly lower levels of Nck1 in skeletal ...
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Small Molecule Inhibitors of PTP1B and TCPTP
... for PTP1B/TCPTP inhibitors and short listed 50 compounds for in-vitro pNPP assay to check the ...for PTP1B and TCPTP catalyzed hydrolysis of pNPP were done using the buffer which contain ...
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Inhibitory potential of polyhydroxylated fullerenes against protein tyrosine phosphatase 1B
... of PTP1B with closed WPD-loop (PDB code ...of PTP1B with open WPD loop), the fullerenol may be located at allosteric site at the distance of about 20 Å from the catalytically important Cys215 ...
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Regional Roles of Central Trkb Receptors in Energy Balance and Regulation by Ptp1b
... Biochemical and structural studies have revealed a substrate recognition motif that, in addition to being present in known targets of PTP1B (Kenner, Anyanwu et al. 1996, Flint, Tiganis et al. 1997, Myers, Andersen ...
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Myeloid-cell protein tyrosine phosphatase-1B deficiency in mice protects against high-fat diet and lipopolysaccharide-induced inflammation, hyperinsulinemia, and endotoxemia through an IL-10 STAT3-dependent mechanism.
... in PTP1B global knock-out mice (15- 17, ...myeloid-specific PTP1B deletion and interrogated their whole body physiology and signalling in isolated ...lacking PTP1B in ...lacking PTP1B were ...
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Activation of oncogenic tyrosine kinase signaling promotes insulin receptor-mediated cone photoreceptor survival
... phosphatase, PTP1B [18], and growth factor receptor-bound protein 14 (Grb14) ...The PTP1B dephosphorylates IR, and the un- phosphorylated form of Grb14 inactivates IR by direct binding to the catalytic loop ...
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Application of the Multiple Solvent Crystal Structures Method to Analyze the Protein Binding Surface of H-Ras Protein
... In contrast, PTP1B (Denu and Tanner, 1998), which forms a sulfenyl-amide in the oxidized form, and the LMW phosphatase (Chiarugi et al., 2001), which forms an intramolecular disulfide [r] ...
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