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The significance of the difference in the
2020-11-25

The significance of the difference in the DDR2 binding specificity towards fibrillar and non-fibrillar collagens is not understood, but may imply differences in biological responses when chondrocytes bind to different collagens in the growth plate. Investigations by Labrador et al. (2001) have shown
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In addition to EGFR other receptor tyrosine kinases RTKs als
2020-11-25

In addition to EGFR, other receptor tyrosine kinases (RTKs) also play roles in the tumor progression under hypoxia, especially hepatocyte growth factor receptor (cMet) (Le et al., 2012). Our data suggested that unlike EGFR, hypoxia had no apparent effect on cMet tlr signaling (data not shown), sugg
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br Conflict of interests br Introduction Ubiquitylation is
2020-11-25

Conflict of interests Introduction Ubiquitylation is a post-translational modification which impacts almost every biological process in the cell. Dysregulation of the ubiquitylation pathway is associated with several diseases, including cancer, neurodegenerative disorders, and immunological dy
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PD 123319 ditrifluoroacetate br Results br Discussion Taking
2020-11-25

Results Discussion Taking advantage of the highly specific protein–protein interactions among cognate PD 123319 ditrifluoroacetate that mediate SUMO conjugation to substrates, we have developed a novel strategy for achieving inhibition of SUMO conjugation in vivo based on disruption of SUMO E
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Approximately of the etamicastat dose was recovered in
2020-11-25

Approximately 50% of the etamicastat dose was recovered in urine, 30% in the form of etamicastat and 20% in the form of BIA 5-961. These data agree with those from a study with [14C]-labeled etamicastat in healthy subjects, which showed that approximately 95% of the administered radioactivity had be
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Two parameters were extracted from these experiments
2020-11-25

Two parameters were extracted from these experiments to compare the interactions of the three compounds with ct-DNA. The association constant K for the binding of the naphthalimide derivatives to ct-DNA was calculated by fitting the evolution of the fluorescence spectra with a 1:1 binding model usin
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Expression of MGMT in human cells can
2020-11-25

Expression of MGMT in human SBI-0206965 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,
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MK-4827 hydrochloride Targeting both PARP and DHODH for anti
2020-11-25

Targeting both PARP-1 and DHODH for anti-cancer therapy would certainly be beneficial as these enzymes share a common role in the DNA replication and repair mechanisms which are involved in the hyper-proliferation of cancer cells. Since benzimidazole-containing compounds have been reported to show g
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There was a good alignment profile between compound IC M
2020-11-25

There was a good alignment profile between compound 26 (IC50 0.06μM) and MTX (IC50 0.08μM) explaining its activity pattern (Fig. 5a). Fig. 5b clearly indicates a different alignment profiles where carbonyl groups are not on the same side between 25 (IC50>100.0μM) and MTX which is in consistency with
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Our observation that FAK is downregulated in
2020-11-25

Our observation that FAK is downregulated in vascular smooth muscle Fruquintinib on fibrillar collagen confirms observations reported for other cell types [14]. However, unlike the results reported previously [14], our work suggests that matrix rigidity per se does not determine FAK downregulation.
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In previous works Gotor Vila et al c differences in
2020-11-24

In previous works (Gotor-Vila et al., 2017c), differences in solubility between the two carriers used during formulation were evidenced. Summarizing, maltodextrin (BA3 product) resulted in a much more soluble product since this polysaccharide is typically composed of an amount of reducing sugars bet
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The small molecule d mannuronic acid M patented DE has
2020-11-24

The small molecule β-d-mannuronic NIBR189 (M2000), patented (DE-102016113018.4), has been tested as an anti-inflammatory and a novel immunosuppressive agent in various experimental models such as animal models of immune complex glomerulonephritis, nephrotic syndrome, multiple sclerosis and rheumatoi
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br Involvement of p MAPK pathway The NF
2020-11-24

Involvement of p38 MAPK pathway The NF-κB signal transduction cascade is a major stress response signaling pathway for the COX-2 gene expression. In mice and humans, the COX-2 promoter has the most successful film for many transcription factors, including NF-κB in the 5′ region of the COX-2 gene
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Interestingly from our consensus SBVC protocol only
2020-11-24

Interestingly, from our consensus SBVC protocol only few compounds (less than 150) have been scored with a full ‘ consensus’. That means that these compounds appear in the top 5% of the database when ranked by every scoring function independently. After visual inspection, we have realized that two a
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br Materials and methods br
2020-11-24

Materials and methods Results Discussion Adiponectin is one of the most studied adipocytokines. Its release from adipocytes is down-regulated in obesity and other adverse metabolic conditions leading to decreased serum concentrations (Turer and Scherer, 2012). Several factors and conditions
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