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Collectively the results presented here provide new insights
2020-09-22
Collectively, the results presented here provide new insights into ligand binding, clustering, spatial distribution, and phosphorylation of DDR1b and DDR2 in response to soluble collagen I. As depicted in the cartoon of Scheme 1, we postulate a model in which the spatial distribution and assembly of
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In conclusion DDR ECD was shown
2020-09-22
In conclusion, DDR1 ECD was shown to be sufficient for collagen mediated DDR1 oligomerization, and the oligomerized form binds to collagen with increased affinity. In full length receptors expressed on live cells, DDR1 oligomerization occurred on the cell surface in agreement with the role of DDR1 E
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br Conclusion The preclinical data reported
2020-09-22
Conclusion The preclinical data reported in this study shows that LAS191859 is a potent and safe CRTh2 antagonist, with a long receptor residence time that provides a sustained in vivo efficacy. This property is reflected in the prolonged duration of action of LAS191859 in in vitro and in vivo fu
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br Nuclear export and the functions of CRM
2020-09-22
Nuclear export and the functions of CRM1 The nuclear envelope provides a compartmentalized intracellular environment for DNA replication, the synthesis of RNA, and production of ribosomes, and, as such, it can regulate cellular biological processes including apoptosis and proliferation. Nucleocyt
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SCH772984 br Conclusions br Acknowledgments This work was su
2020-09-22
Conclusions Acknowledgments This work was supported by a grant from NIH from the National Institutes on Arthritis and Musculoskeletal and Skin Diseases [AR056092]. Introduction Prior exposure to stressors has been consistently associated with the manifestation and/or exacerbation of psychi
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In a cell based functional assay the antagonist
2020-09-22
In a cell-based functional assay, the antagonist properties of were assessed by measuring inhibition of CRF-stimulated cyclic adenosine monophosphate (cAMP) production in human Y-79 retinoblastoma cells. produced a concentration-dependent inhibition of CRF (1nM)-induced cAMP production with an IC
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It is generally thought that the nature
2020-09-22
It is generally thought that the nature of a memorial and the meaning attributed to it SGI1776 by a tourist determines, at least in part, the behaviour that is socially appropriate (Mayo, 1988). Duncan (1995) argues however, that certain places are structured in such a way that they facilitate ritu
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br Tests and measurements We used
2020-09-22
Tests and measurements We used a set of FPGA cores for all tests and measurements. Firstly, the control circuit for the Controlled Current Limiter illustrates the proposed TMR method. The circuit contains a D-Register to enable or disable the power to the protected device, a counter, which is use
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br Materials and methods br Results br Discussion
2020-09-22
Materials and methods Results Discussion For many years, oral PDE5-Is have been prescribed as an on-demand regimen for treating ED. Several studies have reported on the efficacy and safety of such a regimen, with an overall efficacy rate of 60–70% [21]. However, many patients complain of a
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br Materials and methods br
2020-09-22
Materials and methods Results Discussion In this study, we confirmed the activation of Akt by udenafil in 3T3-L1 cells. To elucidate the underlying mechanism of udenafil, we focused on the mitochondria. Our findings demonstrated that udenafil improved mitochondrial function and expression o
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Determination of relative potency EC by
2020-09-22
Determination of relative potency (EC50) by dose response assays in vitro is subject to the same sources of variability as determination of affinity, since the EC50 and Hill slope of the dose response curve are highly dependent on the binding of ligand to a competing receptor that may be present, an
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The cpm corresponding to bound substrate in
2020-09-21
The cpm corresponding to bound substrate in the sample well can be expressed as the difference between the total cpm in the sample well (3Hswtotal; 14Cswtotal) and the cpm for the unbound substrate in the sample well, as illustrated by Eq. (2): By combining Eqs. (1), (2), cpm for the bound substrat
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Molecular imaging that provides a
2020-09-21
Molecular imaging that provides a non-invasive means to visualize and measure a biological process of interest at the molecular and cellular level in living subjects has emerged as a promising approach for in vivo detection of enzyme activity in recent decades [6]. In orexins to anatomical imaging,
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br Analytical improvements Since our review of Oxysterol Met
2020-09-21
Analytical improvements Since our review of “Oxysterol Metabolomes” in 2011 [7], there have been a number of improvements in analytical methods for the analysis of oxysterols and related compounds. McDonald and colleagues in Dallas have refined their LC-MS methods which are now applicable for ana
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Historically covalent drugs have had great
2020-09-21
Historically, covalent drugs have had great success (e.g., aspirin and penicillin), and covalent drugs have become a focus in anticancer and antiviral drug discovery (Kalgutkar and Dalvie, 2012, Singh et al., 2011). These compounds contain low reactivity warheads that allow covalent adducts to form
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