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A recent analysis of urine samples collected
2019-12-30
A recent analysis of 2721 urine samples collected from 245 men and 408 women across the US general population between 2005 and 2010 showed that MP, PP and BuP were measurable in 99.9%, 98.3% and 73.6% of samples from women and 99.3%, 90.2% and 35.9% of samples from men, respectively (Smith et al., 2
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Another milestone in the field is
2019-12-30
Another milestone in the field is the de novo discovery of EPAC2 and EPAC1 specific inhibitors through fluorescence-based HTS assays. Due to the excellent EPAC/PKA selectivity of 5-(N,N-dimethyl)-Amiloride hydrochloride , it has been widely applied as a useful chemical probe to discriminate EPAC rel
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The prospects of the use of this novel
2019-12-30
The prospects of the use of this novel approach for the selective local thermo-activation of enzymes include biomedical and biotechnological applications. As NPs could be engineered to gain access to YM201636 through the endosomal compartment [47] or through non-endocytotic pathways [48], [49], [50]
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Ubiquitination can occur on a single monoubiquitination or s
2019-12-30
Ubiquitination can occur on a single (monoubiquitination) or several (multiubiquitination) lysine residues, or the same lysine residue can be subjected to several rounds of Ub conjugation (polyubiquitination). Ub bonds within polyUb chains are formed through 1 of 7 lysine residues in Ub, and the typ
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The inhibition of mRFP Ub E formation
2019-12-30
The inhibition of mRFP-Ub–E1 formation by ginsenosides Re was not in time-dependent in vitro (Fig. 4B). Fifty micrometres ginsenoside Rg1 decreased E1 activity to 0.24- to 0.36-fold over 30min. This finding suggests that ginsenoside Rg1 may irreversibly inhibit mRFP-Ub–E1 formation or a tight-bindin
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br DDR in atherosclerosis and
2019-12-30
DDR1 in atherosclerosis and vascular disease The Canadian group of Bendeck, explored the role of DDR1 in repair following arterial injury in rats [30]. DDR1 protein levels, assessed via Western blots prepared from arterial extracts taken at various times after injury, showed DDR1 protein dramatic
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br Effects of estrogens on bone Estrogens play an important
2019-12-29
Effects of estrogens on bone Estrogens play an important role in bone remodeling, as demonstrated by studies in mice in which the ER genes were deleted [21], [22]. ERβ compensates for the Mevastatin australia of ERα, and vice versa, but when both ERs are deleted a profound decrease in trabecular
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The T cell receptor TCR pathway is associated
2019-12-29
The T cell receptor (TCR) pathway is associated with T cell activation and differentiation. When specific antigen peptides are recognized by the TCR, lymphocyte-specific protein tyrosine kinase (lck) phosphorylates the immune-receptor tyrosine-based activation motifs (ITAMs) of the TCR-CD3 complex a
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Several effective strategies have been developed to design a
2019-12-29
Several effective strategies have been developed to design activatable MR probes according to the Solomon, Bloembergen and Morgan (SBM) theory, including modulation of the number of inner-sphere water molecules (q), the rotational tumbling time (τ) and the residence lifetime of inner-sphere water mo
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Herein we explored by docking studies the
2019-12-29
Herein, we explored by docking studies the effectiveness of replacing the dimethyl substitution at C (6) of dihydrotriazine with a folded azaspiro-containing substituent, along with the introduction of differently substituted phenyl- and benzyl-rings or alkyl chains, linked at the position 1 of the
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The first purpose of the
2019-12-29
The first purpose of the current study was to characterize a standardized experimental model of postprandial hyperlipidemia in various rodent species. To our knowledge this study provides the most comprehensive and systematic evaluation of rodent models of postprandial hyperlipidemia to date. We ada
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Collagen alignment can contribute to tissue
2019-12-29
Collagen alignment can contribute to tissue stiffening (Malik et al., 2015, Paszek et al., 2005), and ECM stiffness in turn is a powerful activator of integrin function (Levental et al., 2009). These findings highlight the contribution of the mechanical properties of the ECM to signal transduction.
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Previous study showed that CXCR plays an
2019-12-29
Previous study showed that CXCR plays an important role in viral infection and that CXCR1, as an important molecule in CXCR, also plays important roles in viral pathogenesis [[39], [40], [41], [42]]. In mammals, CXCR1 plays an important role in resisting viral infection [43,44], and CXCR1 plays an i
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We next examined the effects of substituents
2019-12-29
We next examined the effects of substituents around the carboxylic oxygenase moiety on CRTH2 binding (Table 4). The carboxylic acid moiety shared by the representative CRTH2 antagonists and is essential for the CRTH2 activity. Germinal dimethylation of the methylene moiety next to the carboxylic aci
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Cilnidipine Our structures also provide new insights
2019-12-29
Our structures also provide new insights into CRTH2 drug development. The ligand binding pocket revealed by our structures comprises many aromatic residues and a few polar residues at the distal end. Correspondingly, most CRTH2 antagonists share a similar structural feature characterized by an aceta
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