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Identification of the drug to be used as
2021-01-09
Identification of the drug to be used as first-step antihypertensive treatment has always been, and remains, a matter of debate. The decision wihich drug (or drug combination) to choose as first-line therapy depend on many variables such as coexisting metabolic disorders, obesity, presence of subcli
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Two GPCR subtypes of interest in
2021-01-09
Two GPCR subtypes of interest in the myocardium are the endothelin receptor (ETR) and the α1-adrenergic receptor (α1-AR). Upon ligand binding, these receptors canonically activate the Gαq protein leading to activation of phospholipase C, hydrolysis of phosphatidylinositol 4,5-bisphosphate into diacy
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A growing number of other
2021-01-09
A growing number of other post-translational modifications are implicated in regulation of the ubiquitin system, including substrate modification by hydroxylation, glycosylation, acetylation, methylation, modification by poly(ADP-ribose) (PAR), and attachment of ubiquitin-like modifiers. The HIF1-α
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br Acknowledgments br The design of polyaromatic
2021-01-09
Acknowledgments The design of polyaromatic molecules able to bind to DNA is of significant importance for the development of anticancer and fluorescent imaging agents. Among them, 1,8-naphthalimide derivatives have received significant attention and have been extensively investigated for their
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G DH has gained interest because of
2021-01-09
G3DH has gained interest because of its broad substrate specificity and site-selective oxidation properties [9,10]. The conversion product, 3-ketoglycoside, possesses potential as a starting material for the chemical industry such as in polymer and surfactants because the keto group becomes a specif
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Phos-tag Acrylamide We had earlier reported that collagen f
2021-01-08
We had earlier reported that collagen fibers with intact native banded structure were occasionally observed in the kinase-deficient, membrane-anchored DDR2 ECD (DDR2/-KD) samples; however, in our DDR1/ECD and DDR2/ECD samples, observation of native banded structure of collagen was far more infrequen
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It is common for plants that are deficient in
2021-01-08
It is common for plants that are deficient in P to invest in their roots in order to maximise P uptake from the soil. Here, plants grown in soil amended with OA had a higher root biomass:shoot pentylenetetrazol ratio compared with plants in the INORG-P treatment. Additionally, greater allocation of
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There may be an interplay of EP
2021-01-08
There may be an interplay of EP2, EP3, EP4 alone, or in combination, with EP1 for the onset of TCDD-induced neonatal hydronephrosis. EP2 and EP4 have been reported to increase AQP2 phosphorylation and membrane trafficking (Li et al., 2009; Olesen et al., 2011). The EP2 and EP4 mRNA concentrations w
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Accordingly we prepared three compounds and
2021-01-08
Accordingly, we prepared three compounds (, , and ) as shown in . Condensation of commercially available GS-7340 with glycine methyl ester gave amide . A Friedel–Crafts reaction between compound and 4-methyl valeryl chloride in the presence of aluminum chloride mainly produced undesired compound
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br Methods br Results br Discussion With this study
2021-01-08
Methods Results Discussion With this study, we provided evidence that acriflavine can interfere with EMT and UPR, two well-described pathways associated with cancer aggressiveness. And, because drug resistance is also clearly associated with the mesenchymal state [36], blocking of the epith
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Together the protein engineering approaches
2021-01-08
Together, the protein engineering approaches employed by Teyra et al., (2019) demonstrate the effectiveness of affinity maturation for improving the affinity of UbVs, but this comes at a cost in terms of specificity. Indeed, the most effective UbV was the dimeric construct generated from UbVs isolat
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Our data indicate that the ability of these promiscuous
2021-01-08
Our data indicate that the ability of these promiscuous kinases to bind chemically diverse inhibitors is defined by the hydrophobic pocket formed by the activation loop, which is only accessible in the DFG-Asp-out conformation. Inhibitors do not artificially induce the DFG-Asp-out conformation as wa
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Eukaryotic cell cycle machinery is thought to appropriately
2021-01-08
Eukaryotic cell cycle machinery is thought to appropriately modulate cell proliferation and cell expansion in various developmental stages and environmental conditions. The core feature of cell-cycle control is the fluctuation of CDK activity, which is regulated by three interactive and conserved me
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Currently multiple clinical trials of CSF CSF R
2021-01-08
Currently, multiple clinical trials of CSF-1/CSF-1R-targeting agents in combination with standard treatment modalities and immunotherapies are underway (Table 1). In particular, results for combinations with checkpoint blockade inhibitors and other immunotherapeutic approaches are eagerly awaited.
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hUcn II influence on MAP is mediated by the activation
2021-01-08
hUcn II influence on MAP is mediated by the activation of CRF2 receptors. In vitro binding studies established that hUcn II is a selective ligand for CRF2 receptors with a slightly higher affinities for CRF2β compared with CRF2α and low or no affinity for CRF1 receptor [13], [19], [24]. Recent in vi
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