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Multi subunit RING type E
2020-09-25
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 authors identified inhibitors of SUMOylation
2020-09-25
The authors identified inhibitors of SUMOylation using two assays to monitor the conjugation of SUMO1 to RanGAP1 by E1 and E2 enzymes: a fluorescence resonance energy transfer (FRET) primary screen that evaluated over 250,000 compounds and a chemiluminescence secondary screen. A counter screen was u
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We initially identified four putative Egr binding
2020-09-25
We initially identified four putative Egr1 GDC-0623 (−39/−36, −105/−102, −107/−104, and −227/−224) on the DBH proximal promoter. The deletion and mutagenesis experiments indicate that the motif at −227/−224 is required for Egr1-elicited reduction in DBH promoter activity. It remains to be determined
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At this stage it is still difficult to
2020-09-25
At this stage it is still difficult to assign specific domains to some of the regions observed in these structures, although some attempts have already been made (Brewerton et al., 2004). Clearly, higher resolution data is needed. In the future, even if an atomic structure of DNA-PKcs is determined,
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Miltefosine DNMT is the dominating enzyme responsible for ma
2020-09-25
DNMT1is the dominating enzyme responsible for maintenance of the DNA methylation pattern and the primary enzyme responsible for copying methylation patterns following DNA replication (Moore et al., 2013). DNMT1 maintains the mitotic inheritance of the original methylation pattern in a cell lineage d
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Next the BE obtained for the different complexes were
2020-09-25
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 current study provides evidence for a
2020-09-25
The current study provides evidence for a previously unknown role for DHODH as a growth/survival factor in KRAS mutant tumors. While many aspects of the link between DHODH inhibition and survival of KRAS mutant cells remain to be established, de novo pyrimidine biosynthesis appears to be a crucial p
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For the SAR optimization of the right hand side
2020-09-24
For the SAR optimization of the right hand side, it was decided to explore the inclusion of the key carboxylic T7 High Yield Fluorescein RNA moiety present in the original DGAT-1 inhibitors from . Analogs were constructed by the synthetic routes outlined in , . In , the methylene-oxy linker was int
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The purposes of this study are to investigate
2020-09-24
The purposes of this study are to investigate the molecular function of DDR2, especially in cellular proliferation in prechondrocytes, and to examine the relationship between the proliferation and differentiation of prechondrocytes through both in vitro and in vivo analysis. Materials and methods
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The discoidin domain receptors DDR and DDR are
2020-09-24
The discoidin domain receptors, DDR1 and DDR2, are receptor tyrosine kinases (RTKs) that are stimulated by collagen in the extracellular matrix (ECM). Unlike most other RTKs, they form ligand-independent stable dimers that are non-covalently linked. This ECM activation induces receptor phosphorylati
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br Conclusions This study showed that
2020-09-24
Conclusions This study showed that in EOC cells, tyrosine kinase receptor DDR1 was expressed mainly in EOC transferases with an Epithelial phenotype. The repressed expression of DDR1 in EOC cells with Mesenchymal phenotype could be due to the higher CpG methylation levels observed at the promoter
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Azaperone Some mechanistic experiments performed in
2020-09-24
Some mechanistic experiments performed in the early 2000s by Ongusaha et al. [78], suggest that DDR1 induction protects Azaperone from apoptosis in a p53-dependent manner, and that impairment of DDR1 expression or function leads to a pronounced increase of DNA damage-induced apoptosis. This evidenc
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Patients with a tumor of
2020-09-24
Patients with a tumor of 4 cm or greater were more likely to have lymph node or tumor metastasis (Fisher’s test p = 0.0001 and 0.0003, respectively). In this smaller patient group a significant correlation between higher DAPK-1 mRNA cetylpyridinium in tumor and normal tissue in tumor-free patients c
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Several evidences showed that seizures increase brain extrac
2020-09-24
Several evidences showed that seizures increase brain extracellular glutamate, which binds to N-methyl-d-aspartate (NMDA) receptor, then up-regulated cyclooxygenase-2 (COX-2) expression in brain capillaries to increase BBB P-gp expression [11,13,29,30]. A recent study demonstrated a different signal
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Nicotine is the main psychoactive component of tobacco
2020-09-24
Nicotine is the main psychoactive component of tobacco that causes addiction. Besides the regulation of the stress responses, CRF has been implicated in nicotine addiction based on several lines of evidence (Bruijnzeel and Gold, 2005, Sarnyai et al., 2001). First, acute administration of nicotine, l
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