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molarity to moles Our recent discovery M P H R A S of
2019-09-10
Our recent discovery (M.P., H.R., A.S.) of a highly selective and in vivo active DDR1 small-molecule inhibitor provides evidence that DDR1 is a druggable pharmaceutical target, and some details of our efforts are provided below. To avoid the repurposing of known kinase inhibitor structural motifs, w
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CYP A is involved in the
2019-09-10
CYP3A is involved in the enzymatic β-Sitosterol and of many therapeutic agents [29]. The activity of BFCOD has been used to monitor CYP3A activity in humans [30], pigs [31], mice [32], and fish [23]. The predominant isoform expressed in the human liver is CYP3A4 [33]. In pigs, CYP3A29 contributes m
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In agreement with the study on
2019-09-10
In agreement with the study on porcine microsomes (Ekstrand et al., 2015), our results indicated a somewhat higher degree of inhibition of CYP2E1 activity in the male pools compared to females. Nevertheless, the degree of this molar solution calculator inhibition did not reach 50%, indicating that q
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The desire for COTS products and some
2019-09-10
The desire for COTS products––and some potential problems There are also technological reasons in support of the use of OTS products. For example, Dawkins and Riddle (2000) point out that the relatively small safety-related systems market cannot sustain the rate of technological advancement stimula
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A similar pattern was observed for both tissues
2019-09-10
A similar pattern was observed for both tissues of P. harpagos, evidencing the absolute predominance of acetylcholinesterase. As observed, no effects were attributed to Iso-OMPA. The hypothesis that the major cholinesterasic form is AChE was reinforced considering the higher hydrolytic activity, whi
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TMC120 br Methods Ventricular cardiomyocytes from adult male
2019-09-10
Methods Ventricular cardiomyocytes from adult male Wistar rats were isolated using a standard enzymatic digestion [11]. Cells were incubated at 37°C for 4 to 6h with Tyrode solution (in mM: 140 NaCl, 4 KCl, 1.1 MgCl2, 10 HEPES, 10 glucose, 1.8 CaCl2; pH7.4, with NaOH) supplemented or not with 10μ
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In view of the hypotensive effect
2019-09-10
In view of the hypotensive effect of endothelial-specific overexpression of eNOS [17], [19], [28] we correlated skeletal muscle eNOS expression with sBP including data on colony 5 of eNOS-Tg [17] which was used to generate eNOS-Tg/KO (Fig. 4D). We found a highly significant one phase exponential dec
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Emergence of antibiotic resistant strains of Mtb
2019-09-10
Emergence of antibiotic resistant strains of Mtb alongwith the inefficacy of widely used Bacillus Calmette-Guerin (BCG) vaccine in adults are major challenges in the treatment and prevention of TB. Elucidation and characterization of new vaccine and drug candidates are therefore required in order to
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br Introduction Mammalian proteases comprise both the peptid
2019-09-10
Introduction Mammalian proteases comprise both the peptidases or exopeptidases, which act at the N- or C-terminal positions of polypeptides, and proteinases or endopeptidases, which are capable of cleaving peptide bonds in the central regions of polypeptides. The endopeptidases are classified in
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In BBR was reported to increase LDL receptor
2019-09-09
In 2004, BBR was reported to increase LDL receptor (LDLR) gene expression by stabilizing LDLR mRNA [4]. Following this report, the same groups conducted additional studies predominantly in HepG2 cells, with similar effects being observed [8], [11], [12], [4]. In addition to LDLR-mediated LDL cholest
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br Results br Discussion The origin and fate of Tfh
2019-09-09
Results Discussion The origin and fate of Tfh cells has been intensely studied since their first description 14 years ago (Breitfeld et al., 2000, Schaerli et al., 2000). Although mice engineered to report BCL6 (Kitano et al., 2011, Liu et al., 2012) and interleukin-21 (IL-21) (Lüthje et al.,
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Dysfunction of the ubiquitin proteasome system causes abnorm
2019-09-09
Dysfunction of the ubiquitin-proteasome system causes abnormal organelle morphology and impairs sperm formation and maturation steps resulting in male infertility [[7], [8], [9]]; this indicates that ubiquitination is essential for spermatogenesis and sperm function during fertilization. β-catenin i
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We propose two different pathways for the
2019-09-09
We propose two different pathways for the production of this species: either that described by Dooley [24], where the phenol ring is first activated by binding of its oxygen to copper, or one where a copper-peroxo species would directly react with an active site tyrosine residue (Scheme 1B). This se
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Elevation of plasma glucocorticoids as well as a sympathetic
2019-09-09
Elevation of plasma glucocorticoids as well as a sympathetic activation are highly adaptive mechanisms allowing the individual to cope in various situations [39]. Novelty-induced increase in locomotor activity, characterizing the bold fish herein, accompanied by elevated glucocorticoids is a well-es
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br Acknowledgements br Introduction Serum triglyceride conce
2019-09-09
Acknowledgements Introduction Serum triglyceride concentrations increase following ingestion of a fat containing meal resulting in postprandial hyperlipidemia. Peak serum triglyceride levels are observed within 2 to 4h of fat consumption and then gradually return to baseline levels within appr
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