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During the tests in vitro SHP showed the
2022-04-12
During the tests in vitro, SHP289-04 showed the beneficial effect on both two important aspects. In human liver carcinoma cell line HepG2, it was found to improve glucose consumption significantly. Otherwise, in pancreas cell line NIT1, it could only promote insulin secretion significantly at high g
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br Experimental br Acknowledgments This project
2022-04-12
Experimental Acknowledgments This project was generously supported by Grünenthal GmbH and IECB. We also thank the staff members of the technical platform of IECB and Grünenthal GmbH for their availability and their skills. Introduction Glucocorticoids (GCs) are essential steroid hormones t
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br NLS and NES Mapping br Sequence
2022-04-12
NLS and NES Mapping Sequence Comparison of Gli NLSs—NLSs in ZF Domains Alignment of the Gli NLSs of representative metazoan animals suggests that the amino TC-E 5003 residues in the ZF domains are strongly conserved (Figure 4.2, Figure 4.3B). However, the length of the intervening amino acid
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This study compared PMS ascorbate
2022-04-12
This study compared PMS+ascorbate and t-BHP in terms of their effects on the volume-dependent parameters of normal human RBCs. Incubation with both oxidative systems resulted in the RBC density and osmotic resistance distribution shifts. Clotrimazole or Са2+ added into the medium, as well as high ex
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br Prospects The prospects for GABAergic pesticides can be
2022-04-12
Prospects The prospects for GABAergic ethionamide receptor can be projected from the rate at which new compounds have been introduced (Fig. 1) and the amounts used. More than three billion pounds of NCA-IA insecticides were used in the past seven decades. There was no target site cross-resistanc
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Interestingly transgenic mice that constitutively
2022-04-12
Interestingly, transgenic mice that constitutively express active FXR in the intestine (iVP16FXR) are protected from chemically-induced and genetically-induced cholestasis. This protective effect is attributed to the induction of intestinal FGF15 and repression of hepatic Cyp7a1 expression, downregu
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Hydantoin in region F bridging the phenoxybenzene
2022-04-12
Hydantoin in region F bridging the phenoxybenzene and benzimidazole moieties was replaced by cyclic building blocks, diketopiperazine (25) and imidazolidinone (26), and linear bonds, amide (27) and urea (28). Analogs 25–28 possessing the linkers other than hydantoin were not tolerated in LBD of FXR,
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uPAR promotes cell associated proteolysis
2022-04-12
uPAR promotes cell-associated proteolysis by binding to uPA which locally converts plasminogen into active plasmin [10]. Ligand-engaged uPAR also acts as a potent regulator of cell migration and matrix attachment. Being a membrane receptor, uPAR needs to interact with extracellular matrix (ECM) prot
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br Acknowledgements This work was in part
2022-04-11
Acknowledgements This work was in part supported by the FöFoLe program by Ludwig-Maximilians-Universität München (to T.S.), the Deutsche Forschungsgemeinschaft (DFG) CO 291/5-2, the Human Frontier Science Program (HFSP) RGP0013, the Helmholtz Validation Funds (Helmholtz Association of German Rese
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br Nanoscale Cortical Actin Remodeling in
2022-04-11
Nanoscale Cortical Actin Remodeling in Regulated Exocytosis The network of cortical LY 235959 is formed by numerous fine actin filaments, which are only about 10nm in diameter [52]. Although the microscale role of the cortical actin network in vesicle exocytosis is well established, the function
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Compounds that induce exocytosis in cultured cells
2022-04-11
Compounds that induce exocytosis in cultured MCC950 sodium include Ca2+-dependent [14] or Ca2+-independent [15] mechanisms. Ca2+-dependent exocytosis releases soluble enzyme content from lysosomes [16] operating by increasing the cytosolic concentration of Ca2+[13] by recruiting extracellular Ca2+[
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Two US FDA approved assays are commonly used for
2022-04-11
Two US FDA-approved assays are commonly used for VL monitoring: the COBAS AmpliPrep/COBAS® Taqman® HIV-1 version 2.0 (“CAP/CTM HIV-1 v2”; Roche Molecular Systems) [18], and the RealTime HIV-1 assay (“RealTime HIV-1”, Abbott Molecular) [19]. Several studies have shown good correlation between the ass
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TLRs were originally identified as pathogen
2022-04-11
TLRs were originally identified as pathogen-associated molecular pattern recognition receptors that recognized exogenous ligands in response to infection [31]. In cirrhotic mice or patients, the gastrointestinal tract produces and absorbs considerable bacterial LPS with increased permeability of the
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A compound structurally similar to PF has been
2022-04-11
A Dabrafenib structurally similar to PF-03654746 has been developed by Pfizer (PF-03654764), with a minor change in the substituent attached to the cyclobutanecarboxamide moiety (Wager et al., 2011). This compound, with the chemical name trans-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]-N
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br Conflict of interest br Funding br Introduction Heme is
2022-04-11
Conflict of interest Funding Introduction Heme is an essential molecule for cellular metabolism involving oxygen and electron transfer [1]. However, free heme is a potent pro-oxidant that catalyzes the generation of reactive oxygen species (ROS) leading to cellular damage [2]. Heme oxygenas
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