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Limitations of our study are the following we
2022-02-18

Limitations of our study are the following: we did not measure central energy metabolism in parallel, so we can only hypothesize that GLUT1 hypermethylation may be associated with alterations in central glucose metabolism. We did not measure GLUT1/GLUT4 gene expression or glucose uptake, so that we
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Extensive pharmacological and structural analysis shows
2022-02-18

Extensive pharmacological and structural analysis shows GCGR antibody REMD-477 competitively blocks GLC binding to the GCGR with 30-pM binding affinity, and can fully inhibit the receptor activity at low nanomolar concentrations in nitric oxide synthase inhibitor 14, 17, 20. Functionally identical t
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A model substance often used in the studies of
2022-02-18

A model substance often used in the studies of oxidative processes in erythrocytes is tert-butyl hydroperoxide (t-BHP), which, being lipophilic, passes easily across the erythrocyte membrane [9]. In erythrocytes treated with t-BHP (0.1–3mM) for less than 1h, a dramatic decline in the reduced glutath
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br FXR FGF in the control of BAs synthesis The
2022-02-18

FXR–FGF15/19 in the control of BAs synthesis The nuclear receptor FXR is the master regulator of BAs homeostasis, modulating their synthesis, Aloperine synthesis and uptake [15]. FXR decreases BA de novo hepatic biosynthesis by reducing the expression of CYP7A1. At the canalicular membrane, newl
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900 80 In summary we have discovered
2022-02-18

In summary, we have discovered the first examples of movement of Asp189 upon binding to fXa inhibitors. A series of novel and potent fXa inhibitors with a phenyltriazolinone P moiety were identified. Although the general binding mode compared to our previously-reported fXa inhibitors was maintained,
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It has been shown that mice lacking
2022-02-18

It has been shown that mice lacking SMAD2 in T cells do not develop spontaneous lymphoproliferative autoimmunity (Malhotra et al., 2010). Further, FOXO1 is known to activate proinflammatory MCP-1 and IL-6 (Ito et al., 2009). To this end, we also validated the downstream target FOXO1 and SMAD2 after
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PKC potentiates insulin release in beta cells however it
2022-02-18

PKC potentiates insulin release in beta cells; however, it is currently not clear how this is mechanistically accomplished in living fluvastatin sodium [15]. First, we discuss PKC structure, regulation, and activation in beta cells. Then, we address two fundamental questions: (1) what is the specifi
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Introduction Post translational modifications to the
2022-02-18

Introduction Post-translational modifications to the N-terminal tails of the histone proteins play crucial roles in genome regulation [1]. These modifications (e.g. acetylation, methylation, phosphorylation) are deposited by so-called ‘writer’ enzymes and dynamically removed by the action of ‘erase
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Metal organic frameworks MOFs have emerged over the past two
2022-02-17

Metal–organic frameworks (MOFs) have emerged over the past two decades with the potentials to act as promising materials in gas storage, chemical separation, catalyst, magnetism, sensing, and drug delivery etc (Du et al., 2013, Zhou and Kitagawa, 2014). Additionally, the secondary interactions, such
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apexbio dilution Different crystal structures of both HOs we
2022-02-17

Different crystal structures of both HOs were reported and showed that the three-dimensional structures of proteins (HO-1: PDB code 1N45, HO-2: PDB code 2QPP) are predominantly in an α-helical conformation, with the heme packed between two helices (distal and proximal), and present a remarkable stru
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More recently Vismodegib was administered in combination
2022-02-17

More recently, Vismodegib was administered in combination with Gemcitabine in a pilot clinical trial that enrolled 23 patients affected by metastatic pancreatic adenocarcinoma. This type of malignancy is the most frequent form of pancreas cancer and is ranked in fourth place for cancer mortality in
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Apo E is defined as a polym
2022-02-17

Apo E is defined as a polymorphic protein arising from three alleles. The human Apo E gene was widely studied and described to be located on chromosome 19, closely linked to the Apo C-I/C-II gene complex [9]. The three major alleles, termed Epsilon-2, Epsilon-3 and Epsilon-4 have been reported [10].
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Here we investigate the structural and biochemical propertie
2022-02-17

Here we investigate the structural and biochemical properties of the N-GTPase domain of p190RhoGAP-A. We determine the crystal structure and find that N-GTPase adopts an extended GTPase-like fold with six unique inserts that seem to preclude its ability to bind typical GAP, GEF, or molar volume calc
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Having identified initial leads and further lead optimizatio
2022-02-17

Having identified initial leads and (), further lead optimization was initiated on B- and C-rings to afford compounds with improved potency. Initial set of substituted imidazole-biphenyl-carboxylic SKF 86002 dihydrochloride derivatives – and () were evaluated for GSNOR potency. Among this, fluor
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LPC OMe LPC LPC and OMe LPC were shown
2022-02-17

LPC 14:0, 2-OMe-LPC 14:0, LPC 16:0 and 2-OMe-LPC 16:0 were shown to be most potent stimulators of intracellular calcium flux in the β cell model, which is one of key processes leading to insulin exocytosis. Yet, species with myristoyl residue initiate calcium influx through voltage-gated (R)-baclofe
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