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Our previous high throughput screening HTS campaign
2021-05-19

Our previous high-throughput screening (HTS) campaign using automated, robust, and sensitive fluorescence based ampk pathway 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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From an industrial perspective the low turnover
2021-05-19

From an industrial perspective, the low turnover numbers and limited substrate scope of α-KG halogenases still represents a significant challenge. However, in light of the fact that currently no chemical processes are available for the selective halogenation of aliphatic carbon centers in complex mo
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The importance of AAE in enhancing the
2021-05-19

The importance of AAE3 in enhancing the survival of plants and yeast when confronted with certain environmental stresses has been documented in recent reports. In response to biotic stress such as oxalate-secreting micro-organisms, AAE3 was found to reduce the inhibitory growth effects of the secret
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Early diagnosis of CVS and
2021-05-19

Early diagnosis of CVS and DCI is a key issue in the management of SAH patients. In this regard, CT Perfusion (CTP) is the most accurate and sensitive method for noninvasive imaging assessment of cerebral ischemia with a great value for prediction and early diagnosis of CVS and DCI. CTP is a relativ
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br Roles of DDR in epithelial cell differentiation br
2021-05-19

Roles of DDR1 in epithelial cell differentiation Roles of DDR1 in cell migration, and invasion Dichotomous functions of DDR1 in disease progression Conclusions and perspectives The switch in cc-5013 from DDR1 to DDR2 during EMT is another important issue. The DDRs may exert distinct or r
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Nimodipine is an L type calcium channel antagonist that
2021-05-19

Nimodipine is an L-type calcium channel antagonist that reduces excessive calcium influx during pathological conditions, contributing to its neuroprotective properties (Zornow and Prough, 1996; Kobayashi and Mori, 1998). Autophagy can be induced by increased [Ca2+] (Rami et al., 2008). Nimodipine si
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Although the reasons why viral RNA does
2021-05-19

Although the reasons why viral RNA does not bind to and activate PKR in WNV-infected cells are not known, some of the known characteristics of flavivirus infections provide possible clues. The viral L-Glutamine protein forms dimers that associate with ER membranes and viral RNA (Lindenbach et al., 2
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How does an increase in E affinity for the
2021-05-19

How does an increase in E2 affinity for the RING domain favor higher activity and polyubiquitination by the E2? Binding of the RING domain to the E2 positions the donor Ub in the E2~Ub conjugate in a closed complex [16], [17], [18] that increases the reactivity of the thioester [60]. A higher affini
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Acknowledgments We acknowledge the Danish
2021-05-18

Acknowledgments We acknowledge the Danish Council for Independent Research (Grant no. 11-105250) and the Carlsberg Foundation (Grant no. 2011-01-0567) for funding this work. Introduction DNA is vital as a biological target to design diagnostic agents as well as therapeutic drugs. The recognitio
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Previous studies from our lab
2021-05-18

Previous studies from our lab looked at the effect of interfering with crossover helix interactions in TS-DHFR. One study utilized peptide mimetics of the crossover helix to inhibit wild-type TS-DHFR noncompetitively, and with an IC of 230 μM. A second study used a virtual screening approach to iden
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The second DDR binding partner identified
2021-05-18

The second DDR1-binding partner identified here, Shp-2, which was not found in the two-hybrid screen but using a bioinformatics approach, is also a mediator of cell migration. Since Shp-2 has two SH2 domains, as well as phosphotyrosine phosphatase enzymatic activity and two C-terminal tyrosines targ
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br Introduction The allergic response is a
2021-05-18

Introduction The allergic response is a complex process involving the interaction of several mediators; among these, cysteinyl leukotrienes (CysLTs) represent one of the most important actors in the pathogenesis of airway allergic diseases such as allergic rhinitis and asthma [1]. Pharmacological
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In our model CSF R blockade with
2021-05-18

In our model, CSF-1R blockade with PLX647 mainly targeted the more abundant MDSCs instead of macrophages, suggesting that the role of CSF-1 may be tumor model-dependent. Different tumor models, genetic backgrounds, or treatments may induce different growth factors or cytokines in the tumor microenvi
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It should also be noted that remarkable individual differenc
2021-05-18

It should also be noted that remarkable individual differences in extinguished fear bradycardia (i.e., CS+E vs. CS−E) during initial Day 2 recall test were observed, particularly within Met carriers. Exploratory analyses revealed that these individual differences were partly driven by the level of r
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br Materials and methods br Results
2021-05-18

Materials and methods Results and discussion Iron (II)/2-oxoglutarate (2-OG)-dependent oxygenases [28], [29] catalyze oxidative reactions of a range of metabolic processes including the hydroxylation of l-proline and l-lysine residues during the post-translational modification of collagen. Mor
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