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Currently much effort has been made to design and synthesize
2020-06-24

Currently, much effort has been made to design and synthesize ThDP analogs (such as ThTDP, ThTTDP, and triazole-ThDP in Fig. 2)8, 9, 10, 11, 12 as PDHc E1 inhibitors. These ThDP analog inhibitors, such as ThTDP and ThTTDP, can block the ThDP binding site, and exhibit significantly stronger binding a
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Inhibition of DHODH is reflected by an antiproliferative
2020-06-24

Inhibition of DHODH is reflected by an antiproliferative effect on peripheral blood mononuclear apoptosis (PBMCs), which can be measured by the inhibitory effect on their phytohemagglutinin (PHA) stimulated growth. The test was performed as described in the reference. Data for few selected compound
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Consistent with previous simulations on the DFG Asp out in
2020-06-24

Consistent with previous simulations on the DFG-Asp-out/-in interconversion of Abl kinase, we only observe the DFG flip with protonated Asp747 (Shan et al., 2009). We showed previously that the pKa for the DFG-Asp in Abl is elevated at 6.5. Further “constant pH” simulations whereby protonation even
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With a favorable spectrum of
2020-06-24

With a favorable spectrum of CRTh2 dependent in vitro and in vivo efficacy demonstrated, the off-target activity of compound 18 was investigated, first against a panel of prostanoid receptors and related eicosanoid targets (Table 8), where no significant activities at 10μM concentration were found i
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Park et al expanded their
2020-06-24

Park et al. [34] expanded their own model as hydrogen- bonding lattice fluid EOS (NLF-HB) [35] for calculating the activity coefficients of aqueous amino BG45 solution. Further, Pazuki et al. [36] extended the perturbed hard chain theory which has been proposed by Beret and Prausnitz [37] for modeli
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Nanocomposite films with a GNP DNA
2020-06-23

Nanocomposite films with a GNP-DNA filler concentration of 20 wt%, 30 wt%, and 40 wt% were investigated by electrical impedance spectroscopy before and after UV-C irradiation (Fig. 2). EIS data were fitted to a RC-circuit model and surface resistivity values were calculated from the fitted resistanc
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Possibly there are similarities among euphorb plant species
2020-06-23

Possibly there are similarities among euphorb plant species but extraction of the 5-ht3 present in the microsomal fraction is needed for testing their preferences for substrates. Although R. communis, E. lathyris and E. lagascae belong to the same family, the DGAT activity of their microsomal prepa
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Bmp products such as Fig are persistent pollutants that
2020-06-23

Bmp7 products, such as 7–9 (Fig. 2), are persistent pollutants that accumulate in the marine environment and can potentially be transferred to the human population via our trophic connections to the oceans (Wan et al., 2009). In addition to potentially addressing the mechanistic curiosities describe
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In summary these results are consistent with
2020-06-23

In summary, these results are consistent with our hypothesis that chemical nitrosation of BMAA to N-BMAA results in the formation of an alkylating agent. Furthermore, we have shown that N-BMAA is more toxic than BMAA itself. Previously, methylazoxymethanol (MAM), which is also present in the cycad n
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In addition to the ESIs identified
2020-06-23

In addition to the ESIs identified that target both EPAC1 and EPAC2, ESI-05 and ESI-07 were identified as compounds that selectively antagonise EPAC2, displaying almost no inhibition of EPAC1 at concentrations up to 100μM [99]. Both compounds were effective inhibitors EPAC2 GEF activity towards Rap1
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In this review we first introduce
2020-06-23

In this review, we first introduce the in vivo metabolism profile of VD3, and the mediation of Cyp3a gene transcription by PXR and CAR in humans, mice and rats. We then focus on the species-specific VDR-dependent regulation of human (CYP3A4, CYP3A5 and CYP3A7), mouse (mainly CYP3A11 and CYP3A13), an
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These evidence prompted us to
2020-06-23

These evidence prompted us to investigate the effectiveness of CT-133, a newly discovered, well-tolerated, selective and potent CRTH2 antagonist, as a treatment of ALI. CT-133 has shown a potential response in treating chronic obstructive pulmonary disease (COPD), allergic rhinitis and bicuculline
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TR provides requirements for qualification of commercial PLC
2020-06-23

TR-107330 (1996) provides requirements for qualification of commercial PLC. It uses the criteria of NUREG/CR-6421. EPRI TR-104159 (1995) includes experience about dedicating COTS SW for PLC-based digital systems such as DAFAS (Diverse Auxiliary Feedwater Actuation System) and Emergency Diesel Bus Lo
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Assessment of DNA damage by comet
2020-06-23

Assessment of DNA damage by comet assay and ChEs activity has been widely used as a biomarker of genotoxicity and exposure to pesticide respectively, to measure the risk related to pesticides in the exposed population [15]. Very few studies have explored the association between DNA damage and worker
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br Funding This work was supported by a research
2020-06-22

Funding This work was supported by a research grant of the Deutsche Forschungsgemeinschaft (SCHN477-9-2 to R.S.S), the Manfred-Stolte-Stiftung (to R.S.S.) and by a research grant from the German Cancer Aid (Deutsche Krebshilfe, No. 106696/TP 5 to T.F.). Introduction Death-associated protein k
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