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C527 mg High throughput screening HTS of
2021-07-27
High throughput screening (HTS) of the AstraZeneca C527 mg 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 was s
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Testosterone is inactivated through hydroxylation and conjug
2021-07-26
Testosterone is inactivated through hydroxylation and conjugation pathways [3], [4]. 6β-Hydroxylation is the main pathway among testosterone hydroxylation processes in the liver microsome. Testosterone 6β-hydroxylation is mainly catalyzed by cytochrome P450 3A (CYP3A) [5], [6], which is expressed in
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Data from our in vitro studies using BEAS
2021-07-26
Data from our in vitro studies using BEAS-2B cells showed a biphasic response of cells to NNK. The initial phase of decrease in CRM1 expression in NNK-exposed cells was observed in our previous study. In this study, we further showed that p-p53 (Thr55) expression was also decreased during this initi
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Distribution of DGTS in basidiomycete fungi has been demonst
2021-07-26
Distribution of DGTS in basidiomycete fungi has been demonstrated to be heterogeneous. In certain fungal taxons, such as Agaricales, Polyporales and Russulales, there are species that synthesize and species that do not synthesize DGTS that belong to the same order or even family (Dembitsky, 1996, Va
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The COMT gene maps to chromosome q
2021-07-26
The COMT gene maps to chromosome 22q11.2 (Grossman et al., 1992) and has two protein isoforms. The differences between S-COMT and longer MB-COMT are in the N-termini, which use alternative translation initiation sites and promoters. These two isoforms display different affinity and capacity for COMT
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Our study has several limitations As this study was performe
2021-07-26
Our study has several limitations. As this study was performed at a single institution, it had a limited sample size and was not powered to detect specific differences in assay performance by organ group or waitlist status. In the two CMV seropositive subjects with potential passive antibodies, the
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Cx platin could improve the
2021-07-26
Cx-platin could improve the level of cellular uptake and DNA platination, hence triggering distinct DNA damage repair pathways. The data (Fig. 3B, C and D) demonstrated that Cx-platin could increase the foci number of γH2AX in cancer cells, preventing the efficient DSBs repair. This gives a good exp
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br Results br Discussion br Conclusions br Acknowledgments
2021-07-26
Results Discussion Conclusions Acknowledgments The basic studies were funded in part by a grant of the Clinical Research, Endocrinology and Metabolism Merck Research Laboratories, Medical School Grant Committee for Ezetimibe, Rahway, NJ, USA. Introduction Elevated cholesterol, partic
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We hypothesize that both IGF dependent
2021-07-26
We hypothesize that both IGF-1-dependent kinase activation and locally synthesized neuroestrogens interactively regulate estrogen receptor activity in neuronal taxifolin in the absence of exogenously applied estradiol. The Neuro-2A cell line was chosen as the model system for these studies because
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Halopemide In this study we also conducted an analysis compa
2021-07-26
In this study, we also conducted an analysis comparing the expression profiling of Hh genes among the sarcomas investigated. In these tumors, the IHH gene showed a higher expression level than PTCH1 gene in RMS and SS samples (pHalopemide in human RMS cell lines as well as mouse NIH-3T3 fibroblasts
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The optimization of the lead compound was
2021-07-26
The optimization of the lead compound () was initiated and the initial key SAR and the results of the structural modifications of lead compound are summarized in . Replacement of the carboxylic α-Cyperone sale moiety with other functional groups led to loss of functional activity against EP4 recep
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PRRSV is a single stranded positive
2021-07-26
PRRSV is a single-stranded, positive-sense enveloped RNA virus in the family Arteriviridae of the order Nidovirales (Meng et al., 1994, 1996). The PRRSV pd98059 is approximately 15 kb in length and contains eleven known open reading frames (ORFs) (Snijder et al., 2013). The 3′ end of the genome enc
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In this study Oncomine GEO and TCGA databases were
2021-07-26
In this study, Oncomine, GEO and TCGA databases were used to analyze the expression of UBE2S gene in HCC and normal liver tissues to determine the relationship between UBE2S expression and prognosis of hepatocellular carcinoma. The potential function of UBE2S in HCC was analyzed by screening UBE2S
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In contrast to the methylation
2021-07-26
In contrast to the methylation that is catalyzed exclusively by DNMTs, there have been suggested several pathways that could induce demethylation (Watt & Molloy, 1988). However, the existence and influencing of enzymes that promote active demethylation remains elusive. Studies aiming to gain more in
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Thus DGK active sites remain ill defined
2021-07-26
Thus, DGK-active sites remain ill-defined and, combined with the lack of crystal structures for mammalian DGKs, have limited our understanding of substrate and inhibitor binding. As a result, current DGK inhibitors consist of compounds with poor specificity within the DGK superfamily (de Chaffoy de
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