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Our data indicate that the
2021-06-16

Our data indicate that the ability of these promiscuous kinases to bind chemically diverse inhibitors is defined by the hydrophobic pocket formed by the activation loop, which is only accessible in the DFG-Asp-out conformation. Inhibitors do not artificially induce the DFG-Asp-out conformation as wa
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Introduction Collagen deposition is a
2021-06-16

Introduction Collagen deposition is a common feature found in cancerous tissues and fibrotic organs/lesions. It is now well accepted that collagen deposition is not just a consequence of disease, but that it can also trigger a vicious cycle. Both chemical and physical signals elicited from collagen
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The following are the supplementary data
2021-06-16

The following are the supplementary data related to this article. Acknowledgments Introduction Drug-resistant epilepsy (DRE) occurs in approximate 30% of patients who suffer from epilepsy [1]. Temporal lobe epilepsy (TLE) is one of the most common partial seizures and the common cause of DRE
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Immunofluorescence Cells were fixed with paraformaldehyde PF
2021-06-16

Immunofluorescence. Cells were fixed with 4% paraformaldehyde (PFA) in PBS and extracted by 0.5% Triton X-100-PBS, or fixed in cold methanol. The cells were immunostained with mouse monoclonal Eltrombopag against α-tubulin (Sigma), γ-tubulin (Sigma), Ran (Upstate), rabbit polyclonal antibodies agai
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Another important mediator in fear learning is the
2021-06-16

Another important mediator in fear learning is the neuropeptide corticotropin-releasing factor (CRF). For example, local repeated administration of CRF into the basolateral amygdala potentiates the acquisition of cue-conditioned fear (Bijlsma et al., 2011) and CRF1 receptor antagonists effectively b
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We further examined our hypothesis
2021-06-16

We further examined our hypothesis that the activation of CRF and CCK systems is responsible for the enhanced anxiety-like behavior induced by immobilization stress using two antagonists to block the expression of CRF1 and CCK2 receptors. It was found that CCK2 receptor antagonist CR2945 or CRF1 ant
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br COTSget based Architectures This section
2021-06-16

COTSget-based Architectures This section describes how our COTSget-based architectures are defined. We use a design inspired by MDE to build a Domain-Specific Language (DSL) of the architecture, as can be seen in the metamodel of Fig. 3. This metamodel defines the abstract syntax of our DSL and i
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The optimization of the lead compound was initiated and
2021-06-15

The optimization of the lead compound () was initiated and the initial key SAR and the results of the structural modifications of lead compound are summarized in . Replacement of the carboxylic angiotensin ii moiety with other functional groups led to loss of functional activity against EP4 recept
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The nitrophenols b d were prepared as
2021-06-15

The nitrophenols 34b–d were prepared as described in Scheme 3b. Nitration of phenols 39b–d with 1equiv of sodium nitrate in the presence of hydrochloric enzastaurin gave an inseparable mixture of 34b–d and 40b–d (1:1). This synthetic problem was successfully avoided as described below. Nitration of
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br Materials and methods br
2021-06-15

Materials and methods Results Discussion Endothelial cells are crucial for both vascular homeostasis and protecting the vasculature against atherogenic insults [3]. OxLDL-mediated injury to endothelial cells is crucial for endothelial dysfunction in the pathogenesis of atherosclerosis and a
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Gliptins have become a part of various
2021-06-15

Gliptins have become a part of various therapeutic regimens to treat type 2 diabetics in recent decades. Gliptins were developed to lower the blood glucose in type 2 diabetes patients and have been shown to be effective [4,5]. More than a dozen gliptins have been developed for the treatment of T2DM,
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DNA bound Ku proteins recruit DNA PKcs and thereby transloca
2021-06-15

DNA-bound Ku proteins recruit DNA-PKcs; and thereby translocate into the duplex by one helical turn, leaving DNA-PKcs near the DNA terminus to assist in tethering the broken ends together [25]. In addition to keeping the DSBs in close proximity, DNA-PKcs may prevent exonucleolytic degradation of the
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Next the BE obtained for the different complexes were evalua
2021-06-15

Next, the BE obtained for the different complexes were evaluated. From the BE obtained from our MD simulations, a very good binder can be differentiated from a very weak binder (−11.85 kcal/mol for MTX vs. −6.74 and −3.61 kcal/mol for compounds 14b and 15c, respectively) but ligands with similar bin
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The results described in the
2021-06-15

The results described in the present study confirm key restrictions on reaction conditions which must considered to maximize reactor productivity. Increased viscosity should be avoided for the amination of ketones by L-AmDH, as a 4-fold increase in viscosity can lower the reaction rate by as much as
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We and others have previously found that supplementation of
2021-06-11

We and others have previously found that supplementation of old rats with ALCAR remediates the age-related decay in mitochondrial bioenergetics in liver (Hagen et al., 1998a, Hagen et al., 1998b), heart (Paradies et al., 1994, Paradies et al., 1999), muscle (Pesce et al., 2010) and Parecoxib Sodium
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