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Several in vivo human studies have produced conflicting resu
2021-05-12

Several in vivo human studies have produced conflicting results for evaluating the inhibition of OCs on the metabolism of CYP3A substrates. Balogh et al. [12] demonstrated an approximately 25% inhibition of CYP3A activities in vivo after the administration of an OC containing 30μg of ethinylestradio
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A variety of fused membered
2021-05-12

A variety of fused 6–5-membered ring chemotypes have arisen such as 7-azaindole acetic acids, benzimidazolyl acetic acids, spiro-indolinone acetic acids, and indolizine acetic acids, however, to the best of our knowledge, fused 5,5-membered ring systems have not been reported. Prostaglandin D (PG
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Based on both the observational and theoretical data generat
2021-05-12

Based on both the observational and theoretical data generated in this study, it appears that the mechanism(s) underlying lower IFM CPT1 activity is complex. Modeling enzyme activity versus alterations in catalytic efficiency (Fig. 3A) suggests that the observed age-associated changes in Km and Vmax
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Introduction Hepatocarcinoma is a common and aggressive form
2021-05-11

Introduction Hepatocarcinoma is a common and aggressive form of cancer (Trad et al., 2017). Due to a high rate of postoperative recurrence and metastasis, the prognosis for HCC remains dismal (Wang et al., 2017a, 2017b). Subclinical metastasis is the major cause responsible for tumor recurrence and
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Although the analysis described above goes far to
2021-05-11

Although the analysis described above goes far to explain the mechanism of ibotenic acid perturbations through CHK1 inhibition, it raises important questions about the mechanism by which WT RAS isoforms promote CHK1 S280 phosphorylation. Previous reports have shown that both the MAPK-RSK and PI3K-AK
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MNs can be obtained from iPSCs
2021-05-11

MNs can be obtained from iPSCs, using signaling molecules such as retinoic ZD 7288 (RA) and Sonic hedgehog (Shh) (Table S1).4, 5, 12, 23, 24, 25, 26, 27, 28, 29 These methods rely on developmental principles and require changing the combinations of signaling molecules at multiple steps, which is wh
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Another clinical study indicated the daily consumption of gr
2021-05-11

Another clinical study indicated the daily consumption of green tea with low concentrations of theanine and catechin would improve cognitive function (Ide et al., 2014). Further, in a double blind randomized clinical study involving 102 patients, the Hypericum extract was examined in terms of effica
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PET CT static images of F
2021-05-11

PET/CT static images of F-CJ-042794 acquired at 1h p.i. from LNCaP tumour-bearing mice with/without co-injection of non-radioactive CJ-042794 (50μg) are shown in . The LNCaP tumours were clearly visualized in PET images with a moderate tumour-to-background contrast. High radioactivity accumulation w
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The Acat gene was identified by
2021-05-11

The Acat1 gene was identified by functional complementation of a Chinese hamster ovary cell mutant lacking ACAT activity [12]. Unlike most other genes, human Acat1 is located in two different chromosomes, Alosetron 1 and 7, with each site containing a distinct promoter: chromosome 1 contains exons
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br Cytochrome P monooxygenases Cytochrome P monooxygenases P
2021-05-11

Cytochrome P450 monooxygenases Cytochrome P450 monooxygenases (P450s) belong to one of Nature’s most versatile group of enzymes for C–H functionalization and are able to perform challenging regioselective and stereoselective activations of remote, unactivated C(sp3)–H bonds, for which there are o
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To investigate the role of DPP
2021-05-11

To investigate the role of DPP-4 inhibition in inflammation-induced bone resorption, we evaluated the effect of a DPP-4 inhibitor on LPS-induced osteoclast formation and bone-resorption in vivo. Our results showed that the DPP-4 inhibitor inhibited LPS-induced osteoclast formation and bone resorptio
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The kinase activity of DNA
2021-05-11

The kinase activity of DNA-PKcs is essential for NHEJ, but the exact role of the enzymatic activity of DNA-PKcs plays in NHEJ is not fully understood [57]. In vitro, DNA-PKcs can phosphorylate each of the canonical NHEJ factors including Ku70/80 [58], [59], XRCC4 [60], [61], colony stimulating facto
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Nanocomposite films with a GNP
2021-05-11

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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We have reported previously that aminoacrylate derivatives o
2021-05-11

We have reported previously that β-aminoacrylate derivatives of the general structure () are inhibitors of DHODH. In particular, tricyclic derivatives and displayed sub-micromolar IC values against DHODH, and in the case of there was a 1000-fold greater potency compared to the human enzyme (DHOD
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[Ala107]-MBP (104-118) Predictions of enzyme topology for DG
2021-05-11

Predictions of enzyme topology for DGAT2 are more difficult since the DGAT2 polypeptide sequences are more diverse across species than those of DGAT1. The length and function of the hydrophilic N-terminus preceding the first hydrophobic segment varies with species – for example, segments in fungi ar
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