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Also important in binding of E to the
2021-07-13

Also important in binding of E2 to the ER is the hydroxyl on the D ring, which has a stabilizing contact with His-524 in ERα (Fig. 7) and with His-475 in ERβ (Fig. S1) [8,9,36,37]. The spatial relationship of the functional groups on the A and D rings on E2 has been used to develop chemicals contai
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It is now well accepted that increased
2021-07-13

It is now well accepted that increased local estrogen levels are associated with both the onset and growth of breast cancer. Tissue concentrations of estradiol (E2) in breast cancer are 10 times higher than that found in plasma [12]. Breast cancer tissues also contain increased activity and express
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After activation AKT phosphorylates target proteins involved
2021-07-13

After activation, AKT phosphorylates target proteins involved in cell growth, metabolism and survival (Manning and Cantley, 2007). For example, AKT phosphorylates the pro-apoptotic protein BAD, preventing it from binding to and inactivating Bcl-xL in mitochondria (Datta et al., 1997). In turn, Bcl-x
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Here we describe preparation of three stable conjugates that
2021-07-12

Here, we describe preparation of three stable conjugates that are linked by either oxyester, disulfide, or isopeptide bonds (Fig. 10.1). Each of these conjugates depends upon the prior purification of E2 and ubiquitin proteins that have been engineered to favor specific linkages. For the oxyester- a
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Immunofluorescence assays were performed to localize the enz
2021-07-12

Immunofluorescence assays were performed to localize the enzyme during growth and differentiation to further characterize Giardia E1. As stated before, the assays showed that the 6780 generated recognized specific E1 forms (E1-114, E1-90 and E1-67 with anti-gNTE1; and E1-47 with anti-gE1CT); the pa
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Given the fact that most criticism on genetic
2021-07-12

Given the fact that most criticism on genetic association studies is the lack of replicability (Hirschhorn, Lohmueller, Byrne, & Hirschhorn, 2002), the aim of the present study is to investigate the influence of the DBH polymorphism rs1611115 (C-970T) on RD in two independent samples of healthy par
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Expression of MGMT in human cells can be switched off
2021-07-12

Expression of MGMT in human nk1 antagonist can be switched off by enzymatic methylation of a cytosine residue in the MGMT promoter sequence. In this regard, both MGMT and the mismatch repair function MLH1 belong to a subset of DNA repair genes that are subjected to epigenetic control. In consequenc
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High throughput screening HTS of the
2021-07-12

High throughput screening (HTS) of the AstraZeneca MK-4827 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 sel
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In the PTEN loss mouse
2021-07-12

In the PTEN loss mouse model, deletion of ATG7 gene not only caused an autophagy-deficient phenotype, but also postponed the progression of inoculated prostate tumor [22]. On the basis of these experimental facts, these ATG7 and PTEN related genes were then compared with the 3020 BCR-associated gene
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In the present study we combined
2021-07-12

In the present study, we combined activity-based protein profiling, biochemical and genetic approaches to identify the PLCPs involved in the sphingolipid pathway leading to plant PCD. By using Arabidopsis SU 5402 and leaves, we demonstrate that this sub-class of plant proteases is activated in respo
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In summary our findings show that LPS can
2021-07-12

In summary, our findings show that LPS can activate CysLT2R on microglial tipiracil australia to induce microglial inflammation and microglia-dependent neuronal death. Furthermore, pharmacological inhibition or knocking down of CysLT2R expression protects neurons against neurotoxicity via suppressi
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DDI is one of the main problems with serious clinical
2021-07-12

DDI is one of the main problems with serious clinical consequences in clinical settings. Several reports have highlighted the role of modulation of drug-metabolizing enzymes, especially CYP450 s, as a major mechanism involved in clinical DDIs [3,4,7]. The present study aimed to investigate the effec
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Mitophagy is a selective autophagic process
2021-07-12

Mitophagy is a selective autophagic process which leads to the degradation of damaged mitochondria in response to metabolic or environmental stress conditions. In this study, we found that LFS-01 treatment significantly enhances p62 in a time-dependent manner. We found that the upregulation of p62 i
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Findings from the present study indicate that CRF
2021-07-12

Findings from the present study indicate that CRF1 receptors are especially important in fear acquisition. CP154,526 given before acquisition training, at least partly, reinstated the fear-potentiated startle response and blocked the development of contextual conditioned fear in SERT−/− rats. CP154,
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Nevertheless of the different types of
2021-07-12

Nevertheless, of the different types of scoring systems so far proposed, each of these [14], [29], [30] considered some aspects that could describe the fibrotic evolution, though none provided a quantitative assessment. Calvaruso et al. [8] showed that CPA had a better histological correlation with
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