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CK enzymes belong to a conserved family of
2020-07-23

CK1 enzymes belong to a conserved family of serine/threonine protein kinases that plays an important and diverse role in vesicular trafficking, DNA repair, Quinupristin-Dalfopristin Complex mesylate progression and cytokinesis in organisms from yeast to humans [15]. In multicellular organisms CK1 e
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The present study is the first time to investigate the
2020-07-23

The present study is the first time to investigate the effect of piperine on intestinal sterol transporters and enzymes in the small intestine. NPC1L1 is a sterol transporter responsible for taking up cholesterol from the lumen to enterocytes (Davis et al., 2004). ACAT2 is an enzyme, which esterifie
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Several large scale clinical studies have set out with the
2020-07-23

Several large-scale clinical studies have set out with the common goal to further understand the cognitive impact of menopause and hormone therapies taken by women (Gleason et al., 2015, Greendale et al., 2011, Karlamangla et al., 2017, Rapp et al., 2003, Shumaker et al., 2003). Only one human study
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Our previous work has demonstrated
2020-07-23

Our previous work has demonstrated that two glutamate residues (Glu-305 and Glu-331 in murine and human TPP II) in the active site are important for exopeptidase activity in mTPP II [17]. At least one of these, Glu-331, seems to form a salt bridge to the N-terminal amino group of the substrate, posi
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Perturbations in cell cycle are
2020-07-22

Perturbations in triclabendazole mg are known to induce apoptosis. Our results show that a fraction of the DT40YB-1b+/− cells, in addition to becoming tetraploids, undergo apoptotic cell death. Similar observations linking polyploidy and apoptosis have been made in the past [23], [30], [31], [32],
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We have previously reported the characterization of A
2020-07-22

We have previously reported the characterization of A-127722, a novel, non-peptide endothelin antagonist that displays very high affinity binding (K=69 pM) with a more than 1000-fold greater affinity for human endothelin ETA than ETB receptor. Although A-127722 is >1000-fold more selective for endot
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igf 1 inhibitor The discovery of proteases that
2020-07-22

The discovery of proteases that are active in organic solvent media has greatly extended their ability in the synthesis of useful products. Microbial proteases which are able be catalyse in non-aqueous solvents present new expectation in enzyme applications. This kind of enzymes gives a major contri
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br Discussion The N terminal domain of DDRs has
2020-07-22

Discussion The N-terminal domain of DDRs has long been recognized as a member of the DS superfamily (Johnson et al., 1993, Karn et al., 1993), and its role in collagen binding is understood in atomic detail (Carafoli et al., 2009, Ichikawa et al., 2007). Our crystal structure shows that the secon
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br Experimental Procedures br Author Contributions br Acknow
2020-07-22

Experimental Procedures Author Contributions Acknowledgments Introduction Germinal centers (GCs) form in secondary lymphoid organs of vertebrates in response to challenge with T-cell-dependent antigens. After extrafollicular and follicular interactions with cognate antigen and T helper c
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br Discussion The regulation of
2020-07-22

Discussion The regulation of intracellular cholesterol levels is a biological process of vital importance for cellular function and integrity, and involves robust transcriptional and post-transcriptional mechanisms that are sensitive to metabolic feedback control. Amongst post-transcriptional mec
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We report here that DAPK signaling pathways
2020-07-22

We report here that DAPK signaling pathways play significant roles in OGD-induced neuronal death. Exposure of the LY 2109761 to OGD led to DAPK activation, which then promoted cell death through BimEL overexpression. Furthermore, DAPK-induced BimEL overexpression was mediated by inactivating ERK1/2
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The optimization of the lead
2020-07-22

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 amyloid definition synthesis moiety with other functional groups led to loss of functional activity agai
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Only a few studies have examined the effect of
2020-07-22

Only a few studies have examined the effect of prostanoids on cardiac fibroblasts. Therefore, this study examines the effect of PGE2 on cardiac fibroblast proliferation and tests the hypothesis that PGE2 causes cardiac fibroblast proliferation via alterations of 54011 receptor regulatory molecules
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br Results and discussion br Conclusion
2020-07-21

Results and discussion Conclusion Novel and selective aziridine-based inhibitors for the Leishmania mexicana protease LmCBP2.8 were discovered. Compounds 7d (Ki = 0.8 μM), 9d (Ki = 1.36 μM), 12d (Ki = 0.77 μM), 14d (Ki = 0.9 μM) and 18 (Ki = 0.441 μM) showed the highest potency and selectivity
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Compounds and were outliers for this equation being the two
2020-07-21

Compounds and were outliers for this equation being the two most reactive compounds. The presence of outliers implies that other factors or specific mechanisms are involved in their chemical hydrolysis. Generally urea derivatives prove to be highly stable in aqueous solutions in vitro. Additional
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