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Previous in vitro studies have demonstrated that
2020-12-10

Previous in vitro studies have demonstrated that DNA-PK-deficient cell line (MO59J) is approximately 30-fold more sensitive to radiation than DNA-PK-proficient cell line (MO59K) [31]. Moreover, specific DNA-PK inhibitors SU11752 and wortmannin have been shown to sensitize GBM SR 49059 (MO59K) to ra
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Expression of MGMT in human
2020-12-10

Expression of MGMT in human ω-Agatoxin TK 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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br DAG kinase activity is confined to specific cell
2020-12-10

DAG kinase activity is confined to specific cell compartments A number of reports demonstrating agonist-dependent translocation of DGKs to distinct membrane compartments suggest that DGK activity is restricted to localized DAG pools generated after activation of receptors. Perhaps the best eviden
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MTX and MTXPGs block the activity of the key
2020-12-10

MTX and MTXPGs block the activity of the key enzyme DHFR (Fig. 1), which converts folates to their active forms – dihydrofolate (DHF) and tetrahydrofolate (THF). MTXPGs also potently inhibit thymidylate synthase (TS). Furthermore, during dTMP synthesis, TS utilizes the cofactor 5,10-methylene THF, w
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Given the excellent in vitro
2020-12-10

Given the excellent in vitro pharmacology profiles of methyl ester 28 and primary amide 29 efforts were reengaged on neutral analogs of these leads, with a focus on non-amide replacements for the carboxylic Epiandrosterone functionality of 1. Acetonitrile 49 was found to have a good balance of DGAT
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Since these first results KSTD activity
2020-12-10

— Since these first results, Δ1-KSTD activity has been identified in many other microorganisms, albeit sometimes with different substrate preferences. For instance, Comamonas testosteroni ATCC 11996 (formerly Pseudomonas testosteroni) is active on several steroid substrates, but it cannot use 11β-h
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Although PQQ has nutritional importance and pharmacological
2020-12-10

Although PQQ has nutritional importance and pharmacological effects in higher organisms, including humans [15], until recently, there was no clear evidence for the use of PQQ as a co-factor in a eukaryotic enzyme. This review presents a novel eukaryotic PQQ-dependent quinohemoprotein recently discov
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In addition to an action via P Y
2020-12-10

In addition to an action via P2Y receptors, extracellular UDP activates GPCRs for cysteinyl leukotrienes (CysLT1, CysLT2; Mellor et al., 2001, 2003). GPR17 has been reported to function as a receptor for cysteinyl leukotrienes and uracil nucleotides (Boda et al., 2011; Fumagalli et al., 2011; but se
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Like professional accounting organizations many
2020-12-10

Like professional accounting organizations, many accounting educators have also embraced the potential recruitment value of advanced placement. For example, high school and college educators collaborated to create the Accounting Pilot and Bridge Project (APBP), in order to jump start the profession'
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br Study br Study meta analyses br Discussion Ten
2020-12-09

Study 1 Study 2: meta-analyses Discussion Ten studies have examined the associations of 5-HTTLPR and COMT Val158Met with alexithymia. However, the findings were mixed. In this study, we found that neither the 5-HTTLPR nor COMT Val158Met is associated with alexithymia. The previous findings
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Estradiol the predominant circulating estrogen in humans it
2020-12-09

Estradiol, the predominant circulating estrogen in humans, it is mainly secreted by the granulosa cells of the ovarian follicles, and the corpora lutea, by the mechanisms indicated above. On the other hand, estretrol is synthesized exclusively during pregnancy by the fetal liver and reaches maternal
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The mechanism by which OC use leads
2020-12-09

The mechanism by which OC use leads to impaired glucose tolerance is yet to be fully clarified. Decreased insulin sensitivity appears to be mainly accounted for by estrogenic component and this effect may be modified by progestogenic component [14], [15]. Estrogenic effect on glucose tolerance has b
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A possible explanation for these
2020-12-09

A possible explanation for these observations has been provided by a recent study showing that EWS-FLI-1 increases the Skp2-mediated 26S proteasome degradation, decreasing p27 protein stability and preventing cell senescence [42]. Mechanism of action of EWS-FLI-1 Molecular analysis has revealed
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br Structure of USP Schematic representation of
2020-12-09

Structure of USP7 Schematic representation of the USP7 domain architecture is shown in Fig. 3B. USP7 is a 135 kDa protein that consists of seven domains, including the N-terminal TRAF-like (Tumor necrosis factor Receptor–Associated Factor) domain, followed by the catalytic core domain and the fiv
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br Halogenases Enzymatic C H activation leading to halogenat
2020-12-09

Halogenases Enzymatic C–H activation leading to halogenation is another emerging area in biocatalysis [55,56]. Incorporation of halogen atoms during medicinal chemistry eff ;orts is a well-established practice, presenting an effective means to control the molecule’s bioactivity and physicochemical
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