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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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Introduction Inorganic arsenic InAs species such as arsenite
2022-04-11

Introduction Inorganic arsenic (InAs) species such as arsenite (AsIII) and arsenate (AsV) are present in groundwater. Arsenic contaminated drinking water is a global public health issue because of its natural prevalence and toxicity. Long exposure to arsenic results in chronic effect in humans, inc
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br Conclusion B esterases and reproductive parameters
2022-04-11

Conclusion B-esterases and reproductive parameters can be used as effect biomarkers of the aquatic contamination with chlorpyrifos. In P. corneus exposed for 14 days to the insecticide, the carboxylesterases determined with p-NFB proved to be the most sensitive biomarker. However, exposure to env
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In the Toc Regulator Mode Fig recognition of the transit
2022-04-11

In the “Toc34 Regulator Mode” (Fig. 6), recognition of the transit peptide by Toc159 monomer (step 4) leads to heterodimer-formation [18]. Subsequently, preprotein interaction with the Toc34G homodimer (step 1) regulates the Toc34G homodimer (step 2, 3). However, this mode requires a parallel induct
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Flaviviruses consist of a nucleocapsid composed of multiple
2022-04-11

Flaviviruses consist of a nucleocapsid, composed of multiple copies of the capsid protein (C) and the single-stranded, positive-sense RNA genome. The nucleocapsid is surrounded by a lipid bilayer in which two transmembrane proteins are inserted, the envelope glycoprotein E and the membrane protein M
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We noticed that the spontaneous
2022-04-11

We noticed that the spontaneous openings of the D97R α1 GlyR appeared to be quite similar to those elicited by a maximally-effective glycine concentration on wildtype GlyR; both generated similar open and shut dwell-time histograms, both exhibited openings grouped into clusters with Popen values gre
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br Materials and methods br Results br Discussion
2022-04-11

Materials and methods Results Discussion The glucose transporter GLUT1 can be acutely activated or inhibited in L929 fibroblast AICAR phosphate by a wide variety of reagents or nutrient conditions [[9], [10], [11], [12],36,50]. This abrupt change in the activity of GLUT1 occurs within minut
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