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Here we describe preparation of three stable conjugates that
2020-11-04

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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The expression of cytokine inducible genes is mediated by
2020-11-04

The expression of cytokine-inducible genes is mediated by a number of components within the cell. It has been shown that Jak2 and the Ras/Raf/MAP kinase signaling cascades are required for the expression of DUB-1[9], [29]. However, the enhancer domain of DUB-1 lacks a consensus sequence for Stat bin
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dna alkylation Furthermore the determination of downstream t
2020-11-04

Furthermore, the determination of downstream target genes induced by CdCl2 is noteworthy and can help to define its underlying carcinogenesis mechanism. Therefore, we evaluated c-fos and c-jun expression which are stimulated by estrogen through ERK/MAPK pathway. These are not only proto-oncogenes wh
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Also important in binding of
2020-11-04

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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Our previous high throughput screening HTS
2020-11-04

Our previous high-throughput screening (HTS) campaign using automated, robust, and sensitive fluorescence based GSK461364 sale assay [10], [11] led to the identification of several EPAC specific inhibitors (ESIs), and was subsequently followed by extensive hit-to-lead optimizations [20], [21], [22]
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Molecular imaging that provides a non invasive
2020-11-04

Molecular imaging that provides a non-invasive means to visualize and measure a biological process of interest at the molecular and cellular level in living subjects has emerged as a promising approach for in vivo detection of enzyme activity in recent decades [6]. In X-NeuNAc synthesis to anatomic
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Initially we ascertained that if the
2020-11-04

Initially, we ascertained that if the dose of elastase was sufficient to cause pulmonary emphysema, then pulmonary emphysema could be maintained throughout the study. We found that elastase at 3U was sufficient to cause emphysema that remained over 35 days. In this experimental design of lung diseas
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All known vertebrate TRIMs are categorized in distinct
2020-11-04

All known vertebrate TRIMs are categorized in 11 distinct subclasses depending on the types of domains present at their carboxyl-terminals (Fig. 3) [29], [35]. Beyond conserved N-terminal domains, it is the C-terminal that provides specificity of interactions with other proteins. The subclass IV for
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br Acknowledgements These studies were supported by a resear
2020-11-03

Acknowledgements These studies were supported by a research grant from the NIH (R01 AR065594) to C. Putterman. Introduction Macrophages integrate and adapt to their locally encountered cytokine and chemokine milieu. In tumors characterized by an unresolving inflammation, the tumor cell-killin
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Introduction The first reference to a possible
2020-11-03

Introduction The first reference to a possible involvement of orexins in the effects of drugs of abuse appeared in 2003 and showed that orexigenic peptide neurons respond to the chronic administration of morphine followed by abrupt withdrawal symptoms caused by opioid receptor antagonists (Georgesc
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SPR was used to measure biomolecular
2020-11-03

SPR was used to measure biomolecular kinetic interactions between TERRA G-quadruplex and ligand in the present study. SPR is a widely used method, but cannot tell which specific type of interaction happened. Compounds with similar structures probably have similar mechanism of interaction, while comp
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Although the analysis described above
2020-11-03

Although the analysis described above goes far to explain the mechanism of vasopressin receptor antagonist 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 M
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br Methods br Discussion In a recent
2020-11-03

Methods Discussion In a recent survey among 2625 high risk patients on atorvastatin, 10.5% of patients achieved an LDL-target of and Phos-tag level for improvement of acceptance and adherence to effective lipid lowering therapy are warranted to maximize the benefits of standard treatment opti
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A study profiling chemokine expression in LCLs revealed high
2020-11-03

A study profiling chemokine expression in LCLs revealed high expression levels of CCR6, CCR7, and CCR10 and low expression of CXCR4 and CXCR5 in EBV immortalized cells. Accordingly, LCLs showed a markedly increase in migration in response to the ligands of CCR6 (CCL20), CC7 (CCL21), and CCR10 (CCL28
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A role for the E E
2020-11-03

A role for the E2–E3 interface in governing mono- versus polyubiquitination is not mutually exclusive with that of the E2 backside, which has previously been shown to mediate polyubiquitination through its ability to bind to Ub [21], [25], [33]. Brzovic and colleagues first demonstrated the importan
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