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In this paper we focused on Ewing
2021-07-22
In this paper, we focused on Ewing sarcoma (ES), a rapidly growing, highly malignant bone tumor developing metastases in the vast majority of patients unless multiagent chemotherapy is applied [16]. ES is the second most frequent bone tumor in childhood and adolescence, and is characterized by the p
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In summary we have identified a series of amides
2021-07-22
In summary, we have identified a series of amides as ERRγ agonists with suitable potency for further development. Our SAR studies of this chemotype identified SR19881 as the most potent full agonist of ERRγ with an EC=0.39 μM in a binding assay and an EC=4.7 μM in a cell-based assay. SR19881 was als
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It has been reported that Eph
2021-07-22
It has been reported that Eph/Ephrin are involved in the regulation of the tumor angiogenesis [10], [11], [12]. The distinct and specific involvement of RGDS peptide australia and veins in tumor angiogenesis is unclear. EphrinB2 is expressed in arteries and its receptor EphB4 is expressed in veins;
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Given the molecular pharmacology and in vitro
2021-07-22
Given the molecular pharmacology and in vitro metabolism data, we proceeded to evaluate the in vivo pharmacokinetics of . Mice (=3) were subsequently administered a subcutaneous dose (5mg/kg) with intermittent plasma collections to measure systemic levels of (). Compound achieved a maximum plasma
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br Conclusions There is significant interest in understandin
2021-07-22
Conclusions There is significant interest in understanding the contribution of biological mechanisms to the non-linear/bilinear dose–response curves for DNA-reactive agents. Model monofunctional alkylating agents have datasets amenable to PoD determination for genotoxic effects in both in vitro a
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Effect of a C C double
2021-07-21
Effect of a C4-C5 double bond — The presence of a double bond at the substrate’s C4-C5 position affects the reactivity of Δ1-KSTDs to varying extent, depending on the enzyme. Most 3-ketosteroids that are converted by Δ1- KSTDs have this double bond. For some Δ1-KSTDs this double bond is even require
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Our previous studies have demonstrated that the
2021-07-21
Our previous studies have demonstrated that the DDR2 discoidin domain fully contains the binding site(s) for the fibrillar collagens I and II (Leitinger, 2003, Leitinger et al., 2004). The binding site for collagen I was mapped to three spatially adjacent surface loops within the DDR2 discoidin doma
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Angiotensin (1-7) In summary in the present study we
2021-07-21
In summary, in the present study we found that CysLT1 receptor attenuates while CysLT2 receptor facilitates OGD-induced PC12 cell death as confirmed by receptor over-expression and antagonism. However, we cannot explain why their roles are distinct and why the cell size is increased in the CysLT2 re
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br Materials and methods br
2021-07-21
Materials and methods Results Discussion Recently it has been found that prostaglandins play an important role in modulating the host immune system [1,3,22,23], and some parasites produce these eicosanoid mediators to survive into their hosts [6,[10], [11], [12],24,25]. The discovery that p
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Recent studies showed that the activity of
2021-07-21
Recent studies showed that the activity of CK2 was significantly reduced in ischemic stroke model rats, and cerebral I/R injury significantly decreased the expression of CK2α (Lee et al., 2004; Kim et al., 2012; Zhou et al., 2016). In addition, the dysregulation of CK2 is involved in ERS/UPR in non-
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Oxidative stress is associated with
2021-07-21
Oxidative stress is associated with elevated levels of intracellular reactive oxygen species (ROS) generation which then causes DNA damage and the death of cells (Miyata et al., 2017). Generation of ROS affects main signaling pathways in cells associated with tumorigenesis: mitogen activated protein
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br Materials and methods br Results and discussion br
2021-07-20
Materials and methods Results and discussion Conclusions Data about the ability of non-conventional ligands to operate class-A GPCRs have been accumulating. Specifically, increasing evidence indicates that oxysterols, oxidized derivatives of cholesterol, are involved in many activities that
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Inflammation is critical in the pathobiology of atherosclero
2021-07-20
Inflammation is critical in the pathobiology of atherosclerosis. The inflammatory mediators impacted by FBXO3 described herein i.e. NF-κB, IL-1β, and TNF-α, and IL-8 have purported causal roles in atherosclerosis. For example, NF-κB activation is increased in mononuclear cells in human plaques [29]
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Haj Yahya et al applied
2021-07-20
Haj-Yahya et al. [52] applied native chemical ligation for the construction of diubiquitin probes. They attached a cysteine residue to the lysine side chain of the proximal ubiquitin and ligated the distal module using the C-terminal thioester of ubiquitin. Elimination of the sulfur depends on resu
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br Discussion The biochemical separation of exonuclease acti
2021-07-20
Discussion The biochemical separation of exonuclease activity from DNA-PK dependent endonuclease activity reported in this manuscript is consistent with genetic separation of Artemis enzymatic activity. Mutations in the protein which result in disruption of endonuclease activity have no effect on
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