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Compounds were screened for their activity against the hERG
2020-12-23
Compounds were screened for their activity against the hERG channel, with the 2,3-Cl compounds more active here than the 2,4-F compounds. The homopiperazine examples (, , , ) showed increased hERG activity relative to the corresponding piperazines. The cell data for the 6,7-dimethoxyquinoline compo
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Flexible alignment of isopropylphenylaminobenzimidazole with
2020-12-23
Flexible alignment of 7-isopropylphenylaminobenzimidazole 16 with the lead topotecan 1 was performed using MOE. It was found that the aryl group of compound 16, exemplified as a yellow circle in Figure 2, overlapped well with the corresponding alkyl chain of compound 1 as well as the other key func
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In these tables the AAD for most
2020-12-23
In these tables, the AAD for most of the alcohols in 2B and 3B schemes is less than 1%. It should also be said that for ethanol, AAD in 2B scheme is (0.36%) and for 3B scheme it is (0.02%), which indicates superior prediction of 3B scheme compared to 2B in CPA ƒ-theory model. Table 8a, Table 9 show
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During recent years two primary types of models
2020-12-23
During recent years, two primary types of models have been applied for calculating various thermodynamic properties of amino 961 solutions, i.e. excess Gibbs energy (gE) models used numerously to describe the solubility of amino acid solutions, and equations of state (EOS) models appropriate to obt
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System Analysis and Modeling In this
2020-12-23
System Analysis and Modeling - In this work, a three-level hierarchical modeling – composed by combinatorial and state-space models – is used: (1) First, failure rates () of TMS servers subsystem units are estimated through continuous Markov chains; (2) Then, the single server HU 308 mg failure rate
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The vascular endothelium is a highly dynamic multifunctional
2020-12-23
The vascular endothelium is a highly dynamic multifunctional organ that is critically involved in the regulation of vessel integrity, vascular growth and remodeling, tissue growth and metabolism, immune responses, cell adhesion, angiogenesis, hemostasis and vascular permeability [23]. Therefore, the
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Several studies suggest that the beneficial metabolic effect
2020-12-23
Several studies suggest that the beneficial metabolic effects of adiponectin in humans are primarily mediated by its HMW isoform. Increases in the ratio of HMW to total adiponectin, but not the total adiponectin level, correlated well with improved N-acetyl D-galactosamine sale sensitivity during tr
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In BBR was reported to increase LDL receptor LDLR
2020-12-22
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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Theoretically the expression profile of GluCl variants was
2020-12-22
Theoretically, the expression profile of GluCl variants was related to their physiological roles. It was reported that all the three variants (GluCl A, GluCl B, GluCl C) were highly expressed in head tissue of L. striatellus and M. domestica, and the expression level of GluCl A was significantly hig
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4-P-PDOT br Introduction Diacylglycerol kinase DGK is a lipi
2020-12-22
Introduction Diacylglycerol kinase (DGK) is a lipid-metabolizing enzyme that phosphorylates diacylglycerol (DG) to produce phosphatidic 4-P-PDOT (PA) [[1], [2], [3], [4]]. DG and PA act as lipid second messengers in a wide variety of biological processes. Ten DGK isozymes (α, β, γ, δ, η, κ, ε, ζ
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Some pyrimidine analogs are substrate based inhibitors that
2020-12-22
Some pyrimidine analogs are substrate-based inhibitors that bind to the dihydroorotate binding site, but most reported inhibitors of DHODH bind to the site occupied by the ubiquinone co-factor., , , , , , , , , , , , , , , , , X-ray crystallographic studies of inhibitor complexes with DHODH and DHO
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The presence of external NAD P H dehydrogenases NDE
2020-12-22
The presence of external NAD(P)H dehydrogenases (NDE) on the outer surface of the inner mitochondrial membrane enables the mitochondria to oxidize cytosolic NAD(P)H (Moller 2001). A porin (a voltage-dependent anion-selective channel, VDAC) that is abundant in the outer mitochondrial membrane permits
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br Progestogens and venous thromboembolism clinical data
2020-12-22
Progestogens and venous thromboembolism: clinical data Progestogens and haemostatis: biological studies For many years, the effect of HT on haemostatis has been largely investigated in observational studies as well as in high evidence level studies among users of oral and transdermal estrogens
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Adding MPA or NETA we found no impact on
2020-12-22
Adding MPA or NETA we found no impact on the estradiol-induced downregulation of serum-stimulated endothelin synthesis in vitro [40]. Progesterone was also able to inhibit the angiotensin II-induced increase in endothelin production [41]. Several clinical studies on the effect of oral or transderma
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br Conclusions ERK and its phosphorylation plays an
2020-12-22
Conclusions ERK 1/2 and its phosphorylation plays an essential role in the hippocampus and can be triggered by both ROS accumulation and excessive Ca2+. DBP exposure can also affect the production of ROS and Ca2+ in the hippocampus. The question therefore arises as to whether the cell injury or a
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