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Mammalian cells have two distinct DNA repair pathways for
2019-09-21
Mammalian CUDC-101 have two distinct DNA repair pathways for DSBs, NHEJ and HR. Our data are consistent with the suggestion that the DNA–PK-mediated NHEJ pathway recognizes DSBs faster than the HR pathway and acts before the activation of the DNA damage S-phase checkpoint. The activation of NHEJ by
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Everolimus treatment showed an increase in the number
2019-09-21
Everolimus treatment showed an increase in the number of plaques and a reduction in plaque size, depending on concentration and treatment time (Fig. 1, Fig. 2). Everolimus-pretreated gap junction adsorbed less virus with more plaque formation in the initial phase of infection (Fig. 3). The ability a
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Roflumilast High throughput screening HTS of the AstraZeneca
2019-09-21
High throughput screening (HTS) of the AstraZeneca Roflumilast collection was conducted and identified oxadiazole amide () originating from a kinase directed screening library (although inactive against a panel of kinases). This compound had moderate potency as a DGAT-1 inhibitor (IC=0.52μM) and w
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We examined the function of immobilised
2019-09-21
We examined the function of immobilised THPs by seeding cells transfected with DDR2-Flag on derivatised crosslinked collagen films, then detecting the phosphorylation of tyrosine 740 (Y740) on the intracellular domain of DDR2 [50]. This regulatory residue is a target for the intracellular tyrosine k
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The in vitro enantioselective metabolism of pesticides
2019-09-21
The in vitro enantioselective metabolism of pesticides has been investigated by employing human liver microsomes, which are a reliable resource to perform MCL enantioselective risk assessment in humans (Carrão et al., 2019; de Albuquerque et al., 2018, 2016; Yao et al., 2016). The enantioselective m
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Acidic substituents showed moderate biochemical activity but
2019-09-21
Acidic substituents () showed moderate biochemical activity, but these compounds showed reduced cellular potency. Additional compounds bearing a carboxylic rat 4 were also prepared and tested (data not shown). All of acidic compounds showed low cellular potency regardless of their biochemical activi
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TCS 5861528 The inhibition of CYP activity by NOR was and
2019-09-20
The inhibition of CYP11β activity by NOR was 11- and 2.5-fold higher than those reported for the antifungal agents ketoconazole (IC50: 4.4μM) and clotrimozole (IC50: 1.0μM) (Fernandes and Porte, 2013). Furthermore, NOR was able to inhibit P450 aromatase activity in carp ovaries, although at a rather
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br Prospect of DDR antagonist DDR a receptor of tyrosine
2019-09-20
Prospect of DDR2 antagonist DDR2, a receptor of tyrosine kinase has been found now to be reported to play a significant role in onset of osteoarthritis at the early stage of diseases progression. The DDR2 are the receptor for extracellular collagen and activated upon the binding of collagen resul
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HCV has evolved mechanisms to evade humoral immune
2019-09-20
HCV has evolved mechanisms to evade humoral immune responses including high functional flexibility and variability of immunogenic portions of its envelope proteins. The highest sequence variability occurs in the first 27 Vicriviroc Malate of the N-terminus of E2, which is referred to as the hypervar
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The aberrant methylation of genes that suppress
2019-09-20
The aberrant methylation of genes that suppress tumorigenesis appears to occur early in tumor development and increase progressively, eventually leading to the malignant phenotype [35]. Genes involved in every step of tumorigenesis can be silenced by this epigenetic mechanism. Hypermethylation of pr
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sirreal Due to cell cell interactions
2019-09-20
Due to cell-cell interactions, high concentrations of LTs can be locally generated in a short period of time during an inflammatory response, thus potentiating LT function. The cellular communication can be mediated between immune cells as well as between immune cells other cell types. Several studi
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CDK S phosphorylation status influences the differential
2019-09-20
CDK5-S47 phosphorylation status influences the differential cellular proliferation versus migration response: Previous work from our laboratory has shown CDK5 to be a critical determinant of the cellular proliferation-migration dichotomy whereby CDK5 activation downstream of stimulated epidermal gro
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Several highly selective COX inhibitors
2019-09-20
Several highly selective COX-2 inhibitors (coxibs) have been reported and marketed [6], including celecoxib [7] and etoricoxib [8] (Fig. 1). Even though these drugs produce less ulceration than conventional NSAIDs, coxibs still produce significant gastric and cardiovascular side effects due to the d
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Kim et al reported for bioactive compounds
2019-09-20
Kim et al. reported for bioactive compounds originating from the endemic species in Korea, the hexane and EtOAc fractions of the MeOH extracts from the roots of Dystaenia takeshimana (Nakai) Kitagawa (Umbelliferae) showed cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX) dual inhibitory activity b
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Though limited to a large cohort of self reported healthy
2019-09-20
Though limited to a large cohort of self-reported healthy individuals, associations between individual hmg-coa reductase inhibitor have been identified which may be clinically significant. Though slight, there is a relationship between the CYP2D6-inferred metabolizer phenotype and the diplotype-pre
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