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Enlarging the ligand binding pocket by
2020-01-03
Enlarging the ligand-binding pocket by reduction of the size of the residue F435 switched DES to an agonist indicating that F435 is involved in mediating the antagonistic effect of DES (Fig. 7E) [13]. The conformation of the smaller side chain of L435 was either not altered by DES or was too small t
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br Acknowledgement We acknowledge for funding
2020-01-03
Acknowledgement We acknowledge for funding support from Maryada Foundation, a DoD/Army Contract No. W911NF-06-1-0095, and National Institutes of Health through the New England Center of Excellence for Biodefense (Grant AI057159-01). Introduction The Gram-negative bacterium Lysobacter sp. XL1
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br Conflict of interest statement br Introduction Endothelin
2020-01-02
Conflict of interest statement Introduction Endothelins (ETs) are a family of multifunctional, naturally occurring peptides with long-lasting vasoconstrictor and pressor effects (Zhou et al., 2004). They are synthesized as a large protein, the pre-proET-1 or Big ET-1, which is subsequently cle
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In the context of E ligase drug
2020-01-02
In the context of E3 ligase drug discovery, it is critical to identify the appropriate E2/E3 substrate pairing to ensure the development and use of the most physiologically relevant screening assay. There have been many reports of limited E2/E3 activity profiling with a small number of E2 and E3 VA
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br Introduction Type Diabetes mellitus T DM is a metabolic
2020-01-02
Introduction Type 2 Diabetes mellitus (T2DM) is a metabolic disorder that raises blood glucose level for a prolonged time. T2DM is associated with acute complications like ketoacidosis, hyposmolar coma, chronic complications include heart disease, stroke, kidney failure, foot ulcers and damage to
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Given the widespread occurrence of oncogene induced RS and t
2020-01-02
Given the widespread occurrence of oncogene-induced RS and the increasing clinical interest in small molecule inhibitors that further exacerbate RS in human cancers (such as ATR inhibitors), our findings point to a protective role for RAD52 in the maintenance of cancer cell viability. As such, RAD52
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Introduction Nucleic acids are polyanionic and their negativ
2020-01-02
Introduction Nucleic acids are polyanionic and their negatively charged nucleotides allow the binding of cationic dyes, such as acridine orange (3,6-dimethylaminoacridine). Acridine orange (AO) was first synthesized in 1889, but its ability to bind nucleic acids was only reported in 1940, with grea
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The preferences for source of FAs for DGAT and
2020-01-02
The preferences for source of FAs for DGAT1 and DGAT2 are related to their membrane topologies, subcellular locations, interactions with other proteins or organelles (discussed in the former section), and their differential expression, substrate specificities, and enzyme kinetics. According to UniPr
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The fibrillogenesis process of collagen is
2020-01-02
The fibrillogenesis process of collagen is understood to initiate in the extracellular space near the plasma membrane where secretory vesicles form regions of deep invagination. However, it is not clear how and when collagen-binding proteins interact with collagen molecules during fibrillogenesis or
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br Acknowledgements This work was supported by
2020-01-02
Acknowledgements This work was supported by grants from Agence Nationale de la Recherche (ANR CAPHE) and from Ligue contre le Cancer. We acknowledge the continuous support of CNRS and the University of Strasbourg. We thank the technical assistance of the “Plateforme de Chimie Intégrative de Stras
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br an anaerobic gram positive spore forming bacterium
2020-01-02
, an P005091 gram-positive, spore-forming bacterium that can induce fatal intestinal inflammatory disease, is the most prevalent cause of antibiotic-associated diarrhea and pseudomembranous colitis in nosocomial settings. Two exotoxins, toxin A (TcdA) and toxin B (TcdB), secreted by the bacterium,
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Compounds and administered orally to fasted Harlan
2020-01-02
Compounds , , and administered orally to fasted Harlan Sprague-Dawley rats 1h prior to trigeminal stimulation, decreased extravasation in this model in a dose-related manner, with an estimated ID of 1, 10 and 100μg/kg, respectively (determined 15min after stimulation, ). For comparison, the clinica
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BAY 61-3606 br Deregulation of CDK Many neurotoxic or stress
2020-01-02
Deregulation of CDK5 Many neurotoxic or stress conditions like ischemic BAY 61-3606 damage, oxidative stress, mitochondrial dysfunctions, excitotoxicity, Aβ exposure lead to disruption of the tight regulation of Cdk5 (De Strooper et al., 2010). Calpain-mediated cleavage of p35 to p25 is activate
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Phylogenetically three related CXC chemokines are classified
2020-01-02
Phylogenetically three related CXC chemokines are classified as the possible ligands for the teleost CXCR1 and CXCR2. They are referred to as CXCL8_L1 (CXCL8/IL-8/CXCa), CXCL8_L2 (CXCc) and CXCL8_L3 (Alejo and Tafalla, 2011, Chen et al., 2013, Laing et al., 2002, Laing and Secombes, 2004, Nomiyama e
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The thermal behavior of the UV sensitive
2019-12-31
The thermal behavior of the UV-sensitive nanocomposites was investigated by DSC before and after irradiation in an extended temperature range (from −40 to 250 °C). Fig. 4a shows the thermograms of the non-irradiated GNP-DNA/PDMS nanocomposites in comparison with a neat PDMS sample. The filler-loaded
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