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Besides by substrate and product KSTDs may also be
2020-03-06
Besides by substrate and product, Δ1-KSTDs may also be inhibited by other steroids. N. simplex ATCC 6946 Δ1-KSTD was strongly inhibited non-competitively by dicortinone (60), a steroidal dimer, and by bis-1-dehydrodicortinone, with values of 0.7 and 0.75 μM, respectively. This enzyme was also inhib
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TBCA mg br Results and discussion Compounds
2020-03-06
Results and discussion Compounds were tested for their binding affinity to human CRTH2 in a radioligand binding assay (3H-PGD2) using CHO cells stably transfected with human CRTH2. In addition, these compounds were assessed for their functional activity in PGD2 driven Ca2+ flux in KB8 cells expre
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In this study we investigated the role phenyl
2020-03-06
In this study we investigated the role 17-phenyl tinor (pt)-PGE2 on endothelial barrier function and the underlying molecular mechanism in HMVEC-Ls as well as in a murine model of LPS-induced acute pulmonary inflammation. We found that 17-pt-PGE2 concentration-dependently enhanced endothelial barrie
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Our present results support a major role of EP
2020-03-06
Our present results support a major role of EP1 receptors in peripheral heat sensitization and a smaller contribution to central heat sensitization but no contribution to mechanical sensitization. While the contribution of peripheral EP1 receptors to heat hyperalgesia is in good agreement with the a
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Introduction Enzymes have higher selectivity
2020-03-06
Introduction Enzymes have higher selectivity, specificity and efficiency than chemical catalysts. Due to their properties and their green chemistry, biocatalysts are widely used in food, textile and pharmaceutical industry [1], [2]. A high efficient biocatalyst for industrial applications must be s
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In contrast a single instillation of BLM results
2020-03-06
In contrast, a single instillation of BLM results in a progression of inflammatory events that culminates in marked remodeling of the lung interstitium. This process takes 2–3 weeks, with the fibrotic lesions becoming most pronounced within the first month [9]. Consequently, the BLM model offers the
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br Introduction O Methylguanine DNA methyltransferase
2020-03-06
Introduction O6-Methylguanine-DNA methyltransferase (MGMT) is a DNA-repair enzyme that specifically transfers alkyl adducts from the O6 position of guanine to the cysteine residue (Cys145) in its active site. In cancer cells, this ability of MGMT disrupts the cytotoxic actions of alkylating antic
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Covalent inhibitors are well suited for targeting the
2020-03-06
Covalent inhibitors are well suited for targeting the E1 glutathione reductase of Ubl modifications. Because the E1 enzymes in Ubl modifications, such as the SUMO E1 and Atg7, have a slow turnover rate (Boggio et al., 2004), prolonged inhibition can be achieved without requiring compounds to be stab
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br Materials and methods br Results br Conclusion
2020-03-06
Materials and methods Results Conclusion Conflict of interest Acknowledgements This work was supported by the National Key Research and Development Program of China (2018YFD0400302) and General Program of National Natural Science Foundation of China (31471602). Introduction A sign
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The absence of the LIG gene in yeasts has prevented
2020-03-06
The absence of the LIG3 gene in yeasts has prevented the use of genetically tractable lower eukaryotes, such as Saccharomyces cerevisiae and Schizosaccharomyces pombe, as models to gain insights into the cellular functions of and interplay between the DNA ligases encoded by the LIG1, LIG3 and LIG4 g
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br Results br Discussion MSCs derived from
2020-03-06
Results Discussion MSCs derived from the bone marrow and adipose tissue have been shown to promote the growth and metastatic ability of breast cancer and other human malignancies, but the mechanisms are incompletely understood (Barcellos-Hoff et al., 2013, Cuiffo et al., 2014, Del Pozo Martin
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The immune control of CMV replication in vivo is primarily
2020-03-06
The immune control of CMV replication in vivo is primarily driven by the T-cell-mediated response, a characteristic that has been proposed as a tool to individualize and therefore to optimize antiviral treatment [6], [7], and it has been associated with spontaneous clearance of CMV viraemia in patie
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The present study sought to determine if chlorodifluoroaceto
2020-03-06
The present study sought to determine if chlorodifluoroacetophenones, such as 3 and 4, were amenable to a radiolabelling methodology to generate potential 18F imaging agents with high cholinesterase affinity. A number of procedures have been reported for the synthesis of trifluoromethyl ketones, inc
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Otherwise ES cells express high
2020-03-06
Otherwise, ES CRT 0066101 express high level of histone lysine specific demethylase 1 (LSD1) expression. In this context, it is proposed that LSD1 inhibition may block the function of EWS-ETS proteins [70]. Furthermore, checkpoint kinase 1 (CHK1), a modulator of cell survival under the condition of
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Kif15-IN-2 The effects of the endocrine
2020-03-05
The effects of the endocrine active agents on hepatic ERα were varied. Both nonylphenol and genistein caused an increase in hepatic ERα in female rats, whereas EE2 did not. It is doubtful that the small changes in hepatic ERα induced by genistein and nonylphenol in female rats are sufficient to alte
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