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Intriguingly our laboratory has shown that the
2020-10-13
Intriguingly, our laboratory has shown that the I638F kinase domain mutant, unlike the L63V and G505 mutants, is incapable of receptor autophosphorylation and activation of its downstream effector SHP-2 when exposed to collagen stimulation. These data indicate that I638F is a loss of function mutati
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br DDR role in kidney Thirty eight papers are reported
2020-10-13
DDR1 role in kidney Thirty-eight papers are reported in PubMed upon the keyword search “DDR1 AND kidney”. Careful examination of those papers shows that only 31 are related to DDR1\'s role in glomerulosclerosis and renal fibrosis, 24 of those being research and the rest review articles. Since the
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Our recent discovery M P H
2020-10-13
Our recent discovery (M.P., H.R., A.S.) of a highly selective and in vivo active DDR1 small-molecule inhibitor provides evidence that DDR1 is a druggable pharmaceutical target, and some details of our efforts are provided below. To avoid the repurposing of known kinase inhibitor structural motifs, w
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Interferon IFN induces formation of a
2020-10-13
Interferon (IFN)-γ induces formation of a heterotetrameric, IFN-gamma-activated inhibitor of translation (GAIT) complex in human monocytic Annexin V-Cy3 Apoptosis Kit (Mazumder et al., 2003a, Sampath et al., 2004). The complex binds a bipartite stem-loop element in the 3′UTR of vascular endothelia
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The following are the supplementary data related to
2020-10-13
The following are the supplementary data related to this article. Acknowledgments Introduction Drug-resistant epilepsy (DRE) occurs in approximate 30% of patients who suffer from epilepsy [1]. Temporal lobe epilepsy (TLE) is one of the most common partial seizures and the common cause of DRE
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br Results br Discussion br Experimental Procedures br Ackno
2020-10-13
Results Discussion Experimental Procedures Acknowledgments In the preceding paper, we reported 3-amido-4-anilinoquinolines as highly selective inhibitors of CSF-1R kinase, along with our initial efforts to optimize the series. Examples from the 6,7-dimethoxyquinoline series were very p
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Behaviors were compared between saline and amphetamine pre t
2020-10-13
Behaviors were compared between saline and amphetamine pre-treatment groups at 24h and 2 weeks following the last treatment, or between pre-treatment groups that received vehicle or ASV-30 infusions, using separate two-way ANOVAs. Significant effects were analyzed further using Student–Newman–Keuls
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The use of inhibitors clearly has
2020-10-12
The use of inhibitors clearly has its caveats and the field should come to a consensus on etomoxir concentration to maximally block LC-FAO while minimalizing off-target effects. The current papers convincingly show that 200 μM is too high, but it should be noted that 3 μM does not fully suppress LC-
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A neurotoxic syndrome called Intermediate
2020-10-12
A neurotoxic syndrome called “Intermediate syndrome” has been described after acute cholinergic crisis, which has been interpreted as the result of pre- and postsynaptic disruptions of neuromuscular transmission (Senanayake and Karalliedde, 1987). Other toxic effects with unknown molecular targets h
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In summary we demonstrated the high
2020-10-12
In summary, we demonstrated the high potency of fluxametamide against M. domestica, L. striatellus, and T. urticae GABACls, which leads to high acaricidal/insecticidal effects on these arthropod pests. In contrast to its high potencies against the GABACls of arthropod pests, fluxametamide exhibited
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Currently phosphodiesterase type PDE inhibitors are used wid
2020-10-12
Currently, phosphodiesterase type 5 (PDE-5) inhibitors are used widely as the first- line oral treatment for erectile dysfunction of varying causes. Radical prostatectomy for the treatment of prostate cancer is frequently associated with erectile dysfunction, and this type of erectile dysfunction is
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Within the availability of large
2020-10-12
Within the availability of large number of experimental data, it is easy to develop the relation between the mechanical strength and corrosive resistance of the RHA added cement concrete. The developed correlation is given in the following Eq. (4.8). This equation can be used to predict any of the p
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br Materials and methods br Results br
2020-10-12
Materials and methods Results Discussion Inflammatory signalling and in particular the arachidonic ionomycin cascade have been suggested as targets for disease modification, optimization of the therapeutic response, and even restoration of pharmacosensitivity (Potschka, 2010). Recently, we
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br Substrate Specificity Discrimination and
2020-10-12
Substrate Specificity, Discrimination, and Binding Energy In MK-1775 to catalytic efficiency, which can be gauged in reference to an absolute scale of ‘catalytic perfection’ 10, 11, specificity is a relative concept because it requires comparison between given alternative substrates. In fact, spe
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br Protein protein interactions of LEI L
2020-10-12
Protein-protein interactions of LEI/L-DNase II and the control of cell death Evolutionary tips The serpin inhibitory mechanism is extremely well adapted to evolutionary changes because a single amino Kartogenin substitution in the RSL can led to the inhibition of a totally different protease.
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