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Three kinase inhibitors dasatinib type I imatinib type
2021-07-19
Three kinase inhibitors dasatinib (type I), imatinib (type II) and nilotinib (type II), identified initially as inhibitors of tyrosine kinase BCR-ABL, were found to target DDRs in a chemical proteomic profiling study (Bantscheff et al., 2007, Hantschel et al., 2008). These tyrosine kinase inhibitors
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Enzymatic assay The usual in vitro test
2021-07-17
Enzymatic assay. The usual in vitro test for the measure of the activity of DbH involves ascorbate as a cosubstrate (e.g., 5mM) and tyramine as a substrate (e.g., 10mM). When using N-aryl-N′-hydroxyguanidines instead of ascorbate, the hydroxylase activity of DbH was measured by HPLC as the amounts o
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Piceatannol It is currently believed that acute morphine adm
2021-07-17
It is currently believed that acute morphine administration can impair learning and memory (Friswell et al., 2008). Chronic morphine treatment can also impair access to and retention of spatial memory (Spain and Newsom, 1991, Zheng et al., 2002). Using the Morris water maze experiment, we have previ
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In this context we initiated a program
2021-07-17
In this context, we initiated a program to develop new antiviral chemotypes towards a host factor implicated in AH 6809 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, structura
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Molecular modelling studies were performed on the hDHFR
2021-07-17
Molecular modelling studies were performed on the hDHFR inhibitors identified (1, 11, 13, 14, 16, 25 and 32) to explore the structural basis of the interaction between the mentioned compounds and the human enzyme. The docking studies were performed using the X-ray crystallographic structure of the h
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br Conclusion Our objective is
2021-07-17
Conclusion Our objective is to promote cell activity on biomaterials, especially for use in regenerative medicine, by grafting THPs containing collagen-binding sites onto inert substrates. We have previously reported a methodology to derivatize EDC/NHS crosslinked films with photoreactive THPs. T
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The three dimensional crystal structure
2021-07-17
The three-dimensional crystal structure of Ca2+ loaded CaM reveals a dumbbell-shaped molecule with two roughly globular lobes, the N- and C-terminal lobes linked by a long solvent-exposed helix, which has been shown by NMR to be non-helical in its central part and flexible in solution [13]. Each glo
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br Deregulation of CDK Many neurotoxic or stress
2021-07-17
Deregulation of CDK5 Many neurotoxic or stress conditions like ischemic cotransporter damage, oxidative stress, mitochondrial dysfunctions, excitotoxicity, Aβ exposure lead to disruption of the tight regulation of Cdk5 (De Strooper et al., 2010). Calpain-mediated cleavage of p35 to p25 is activa
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Free Fatty Acid Quantification Colorimetric/Fluorometric Kit
2021-07-17
Conclusions Taken together, a distinct contrast is observed between ERK1/2 phosphorylation in hypothalamic and extra-hypothalamic Free Fatty Acid Quantification Colorimetric/Fluorometric Kit regions. The hypothalamus is the only brain region where ERK1/2 phosphorylation was increased 15minutes af
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One significant finding in this
2021-07-17
One significant finding in this study was the overexpression of a protein identified as LysM domain/BON superfamily protein [29], [30]. This protein was highly overexpressed in the meropenem-treated condition. InterProScan analysis revealed that the LysM domain/BON superfamily protein consisted of t
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In recent years neuroimaging studies have increasingly
2021-07-17
In recent years, neuroimaging studies have increasingly demonstrated acute effects of THC on ibuprofen solubility mg function, the vast majority of them involving a cognitive challenge (Bossong et al., 2014b). For example, without affecting performance accuracy, THC caused reductions in activity du
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In order to validate the ATP competitive mode of inhibition
2021-07-17
In order to validate the ATP competitive mode of inhibition, compound 12 was selected as a representative inhibitor of this series, and the IC50 values were determined at eight different concentrations of compound 12 ranging from 0.001 to 100 μM, and repeated four times using different ATP concentra
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Data from immunohistochemical detection of CIC revealed that
2021-07-17
Data from immunohistochemical detection of CIC-3 revealed that the immunostaining of CIC-3 can be present both in hepatocarcinoma and its matched normal controls though; CIC-3 was, on the whole, significantly elevated in hepatocarcinoma relative to its paired normal control. In consideration of the
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Another potential source of variable affinities is inherent
2021-07-17
Another potential source of variable affinities is inherent in the method of RBA determination. While several reports simply use relative IC50 values as RBAs [11], [12], [13], [14], [15], these are only an approximate measure of relative affinity since IC50 varies due to experimental and biological
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It seems plausible that this ESC driven effect relies
2021-07-16
It seems plausible that this ESC-driven effect relies on a paracrine signaling. Numerous studies showed that the Fgf4 (fibroblast growth factor 4)/MAPK (mitogen-activated protein kinase) pathway is involved in PE differentiation in mouse ARRY-614 (Chazaud et al., 2006), (Frankenberg et al., 2011),
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