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Multi subunit RING type E
2019-08-02
Multi-subunit RING-type E3 ligases are exemplified by the CULLIN-RING-ligase (CRL) and the anaphase-promoting complex/cyclosome (APC/C) [19]. CRLs constitute the biggest family of other multi-component E3 ligases. These consist of a cullin scaffold protein (CULLIN 1, 2, 3, 4A, 4B, 5, 7), a substrate
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The intracellular redox situation of MC T E cells
2019-08-02
The intracellular redox situation of MC3T3-E1 hyPerFUsion™ high-fidelity DNA polymerase after exposure with fluoride has been investigated and results revealed that the generation of ROS increased at a concentration-dependent manner, which indicated that NaF induced oxidative stress damage in MC3T3
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br Regulation of DGK activity Activation of
2019-08-02
Regulation of DGK activity Activation of the DGKs is complex and unique for each DGK isotype. In most cases, DGKs must translocate to a membrane compartment to access DAG. However, translocation does not necessarily activate the enzyme [57]. In addition, DGK activity can be modified by other cofa
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We have previously reported DAPK inhibitors discovered throu
2019-08-02
We have previously reported DAPK inhibitors discovered through our structure-based virtual screening (SBVS) research program. In this paper, we describe the general protocol of our in silico approach, and the strategy used to develop hit compounds. In addition, the studies conducted on the structure
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br A major physiological action of ET is to
2019-08-01
A major physiological action of ET-1 is to function as one of the most powerful vasoconstrictors of human blood vessels. As such, ET-1 plays a major role in regulating vascular function in all organ systems, including the kidney (Fig. 1). As in other vessels, ET-1 is thought to be released from en
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As retinol was not inducing any
2019-08-01
As retinol was not inducing any of the isoforms of CYP450 responsible for the bioactivation of paracetamol, we decided to examine retinol\'s effect on renal and hepatic glutathione to determine whether retinol was potentiating hepatotoxicity through a mechanism of glutathione depletion. Studies, uti
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br Materials and methods br Results br
2019-08-01
Materials and methods Results Discussion Studies have suggested that the Hh signaling pathway, which plays as an essential autocrine viability factor for MFBs [10], [11], is a potential therapeutic target for liver fibrosis. Previously reported works have proven the effectiveness of the Hh
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Due to the high attractiveness of E and E
2019-08-01
Due to the high attractiveness of E2 and E3 ligases as drug targets, a number of drug discovery assays have been published, based on detection by fluorescence (Dudgeon et al., 2010, Krist et al., 2016, Zhang et al., 2004), Mometasone furoate (Davydov et al., 2004, Huang et al., 2005, Kenten et al.,
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Vitamin B12 br Results and discussion br Conclusion We have
2019-08-01
Results and discussion Conclusion We have constructed a series of potent and greatly selective DPP-4 inhibitors with pyrazolo[1,5-a]pyrimidin-7(4H)-one core surrogates. The modification of the core led us to b2 which has IC50 of 80 nM and > 1000 fold selectivity over DPP-8 and DPP-9. We utiliz
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Expression of MGMT in human
2019-08-01
Expression of MGMT in human SAR131675 can be switched off by enzymatic methylation of a cytosine residue in the MGMT promoter sequence. In this regard, both MGMT and the mismatch repair function MLH1 belong to a subset of DNA repair genes that are subjected to epigenetic control. In consequence, ab
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ApicomplexansApicomplexans are unicellular and spore forming
2019-08-01
ApicomplexansApicomplexans are unicellular and spore-forming obligate intracellular parasites that occupy diverse host niches (Mogi and Kita 2010). They have remodeled mitochondrial carbon and energy metabolism through reductive evolution. The development of novel drugs is now a very serious challen
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The phenotypes of KD Ddr transgenic mice were
2019-08-01
The phenotypes of KD-Ddr2 transgenic mice were less severe than expected from the results of miDdr2-transfected ATDC5 cells, which indicated that DDR2 might play important roles in endochondral ossification but neither critical nor essential roles in determining total body and skeleton size. The gr
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On the basis of the published articles it is
2019-08-01
On the basis of the published articles, it is known that chemokines are produced by leukocytes and tissue cells, constitutively or after induction. Chemokines are responsible for the recruitment of leukocytes to maintain proper functioning of the immune system [14]. They exist in the central nervous
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Several studies have already shown that mPR activation can s
2019-08-01
Several studies have already shown that mPR activation can significantly reduce intracellular cAMP levels in different kind of cells, such as GT1-7 neuronal cells [32], MDA-MB-468 breast cancer cells [55] and primary vascular endothelial cells [56]. The experiments performed with PTXa and 8-Br-cAMP
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br Results br Discussion br Materials and Methods
2019-08-01
Results Discussion Materials and Methods Acknowledgment This work was funded by the Collaborative Research Centre (SFB) 807 of the German Research Foundation (DFG) and supported by the state of Hessen (Center for Biomolecular Magnetic Resonance) and the German Research Foundation (DO545/
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