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We first confirmed LPS induction
2020-01-25
We first confirmed LPS-induction of markers known to induce NF-κB signaling in Caco2BB cells, as established for numerous other cell types [31]. We initially selected this approach to monitor NF-κB activation instead of directly monitoring p65 as it is technically straightforward and provides both u
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Tolvaptan receptor br Multi subunit RINGs There are RING typ
2020-01-25
Multi-subunit RINGs There are RING-type E3s that exist as multi-subunit assemblies (see Fig. 3B). A striking example is the Cullin RING Ligase (CRL) superfamily [35], which exhibits enormous plasticity in substrate specificity. Each CRL subfamily is characterized by a cullin protein (Cul-1, 2, 3
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Tumor cells exposed to the effect
2020-01-25
Tumor Diclofenac mg exposed to the effect of these compounds were shown to become chemo and radio-sensitive. Based on that, it was possible to anticipate the selectivity requirement for DNA-PK inhibition and the best route for their development. Accordingly, prompted by the clinical significance an
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In this context we initiated a
2020-01-25
In this context, we initiated a program to develop new antiviral chemotypes towards a host factor implicated in SB 216763 replication: the host (human) dihydrofolate reductase (DHFR) [21]. We recently identified this enzyme as the molecular target of 1-aryl-4,6-diamino-1,2-dihydrotriazines, structu
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Our western blotting results showed that phospho DDR
2020-01-25
Our western blotting results showed that phospho-DDR1 levels continued to increase after I/R injury, and the overall activation trend between phospho-DDR1 and MMP-9 was the same. We found that phospho-DDR1 expression started to increase significantly at 12h after I/R injury, which may be related to
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Our previous high throughput screening HTS
2020-01-23
Our previous high-throughput screening (HTS) campaign using automated, robust, and sensitive fluorescence based 2hcl mg 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], [23],
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br Results br Discussion Oxysterols
2020-01-23
Results Discussion Oxysterols and EBI2 have received growing attention in the field of immunology, with works highlighting an important role for EBI2 in immune cell migration. However, these studies are mainly limited to animal models (Chalmin et al., 2015, Hannedouche et al., 2011, Kelly et a
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Advances in the total chemical synthesis
2020-01-23
Advances in the total chemical synthesis of ubiquitin have enabled the efficient synthesis of new and improved ubiquitin-based reagents. Using an optimized linear synthesis, ubiquitin can now be easily obtained in high yield and purity [35]. Using this synthetic methodology, ubiquitin can be functio
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ARQ 621 synthesis The Fontan circulation When first describe
2020-01-22
The Fontan circulation When first described in 1971, the Fontan operation ushered in a new paradigm in the care of children born with the varied forms of complex congenital ARQ 621 synthesis disease (CHD) characterized by a single effective pumping chamber.1., 2. This procedure, which creates a to
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br Acknowledgments Denise Fernandes acknowledges a postdoc f
2020-01-22
Acknowledgments Denise Fernandes acknowledges a postdoc fellowship (SFRH/BPD/34289/2006) from the Portuguese Fundação para a Ciência e Tecnologia (FCT) of the Ministry of Science and Technology of Portugal. This work was supported by the Spanish National Plan for Research (Project Ref. CGL2011-24
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br EphB as a therapeutic target
2020-01-22
EphB4 as a therapeutic target in cancer Eph receptors and ephrins are promising new therapeutic targets in cancer. Various strategies have been employed to evaluate the interference of tumor-promoting effects or the enhancement of tumor suppressive effects. The inhibition of the Eph-ephrin system
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Protein ubiquitination occurs at the lysine residues and is
2020-01-22
Protein ubiquitination occurs at the lysine residues, and is mediated by the sequential reactions of ubiquitin-activating enzyme (E1), conjugating enzyme (E2), and ligase (E3). The first step in this process comprises the ATP-dependent activation of ubiquitin by E1 to form a ubiquitin–E1 conjugate.
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It was demonstrated that ET signaling is the primary axon
2020-01-22
It was demonstrated that ET-1 signaling is the primary axon guidance mechanism that accounts for sympathetic innervation of the sinoatrial node and myocardium in the developing mouse heart [11]. In this article, we will review the findings relating to the basic profiles; i.e. molecular features of
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br Funding br Disclosure of interest br Acknowledgments br I
2020-01-22
Funding Disclosure of interest Acknowledgments Introduction Pulmonary fibrosis (PF) is a chronic disease characterized by extensive deposits of the extracellular matrix (ECM) that can impair the architecture and function of the lungs (Cavazza et al., 2010). Imbalance between the prolifer
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Moreover Hypericum perforatum L was also included in the
2020-01-22
Moreover, Hypericum perforatum L. was also included in the initial screening, showing only a weak percentage of inhibition on both enzymes. In fact, it was not selected among the most active plants. The phytochemical profiles of these three Hypericum species were already reported to be significantly
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