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From the general synthetic route
2020-12-08
From the general synthetic route, we first synthesized a directed set of analogues of general formula , keeping the synthesis simple by using a symmetrical pyrazole (R=R=Me). The SAR of a set of 30 compounds in the GTPγS binding assay turned out to be quite tight: only 4 (13%) compounds showed moder
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br Results br Discussion br Experimental Procedures br Autho
2020-12-08
Results Discussion Experimental Procedures Author Contributions Acknowledgments Introduction Excitatory synaptic transmission within the brain is largely mediated by ionotropic glutamate receptors. At glutamatergic synapses, α-amino-3-hydroxy-5-methylisoxazole-4-proprionic all tran
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An increased CK activity was found in septal neuronal cells
2020-12-08
An increased CK2 activity was found in septal neuronal AM1241 australia dissected from rat embryos after hypoglycemia [36]. These data indicated that CK2 activity is not only regulated by insulin but also by the glucose concentration. One essential step in insulin action is the binding of the hormo
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Ultrasound is an acoustic wave with a frequency kHz
2020-12-07
Ultrasound is an acoustic wave with a frequency >20 kHz that needs a medium to propagate [20]. Accompanied by the spread of an ultrasonic wave, a series of alternating cycles of compression and rarefaction emerge in the liquid medium. During the rarefaction cycle, microbubbles are formed because of
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The expression of DDR receptor has regulated by
2020-12-07
The expression of DDR2 receptor has regulated by numerous types of factors depending upon the cell type. During the osteogenic differentiation, the transcription factorATF4 combined with CCAAT/enhancer binding site in the DDR2 promoter, which is responsible for induction of DDR2 transcription [24].
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Cyclosporine NEORAL Oral Solution Novartis is
2020-12-07
Cyclosporine (NEORAL® Oral Solution, Novartis) is an immunosuppressant widely used in organ transplantation and many other clinical conditions [12]. It undergoes extensive hepatic and intestinal biotransformation mainly via the metabolizing enzyme, CYP3A4 [[12], [13], [14], [15]]. Considering the na
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Mouse Cyp a is a homologous isoform
2020-12-07
Mouse Cyp3a11 is a homologous isoform of the human CYP3A4 gene, and both are highly expressed in the liver (Hart, Cui, Klaassen, & Zhong, 2009). CYP3A4 is the most abundant CYP450 in hepatic microsomes responsible for drug and xenobiotic metabolism (Zanger & Schwab, 2013), and it is the most active
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br Materials and methods br Results br
2020-12-07
Materials and methods Results Discussion In this study, we employed a liquid chromatography mass spectrometry (LC–MS)-based metabolomic approach to profile GEF metabolism and bioactivation in human and mouse liver microsomes. Metabolomic approaches rendered us readily screen out the GEF-rel
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br Methods br Results br
2020-12-07
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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Cellular immune responses such as
2020-12-07
Cellular immune responses, such as phagocytosis and apoptosis, are very important processes to eradicate the invading pathogens and reduce concomitant host damage. And all of these processes are fine-tuned by the ubiquitin system (Li et al., 2016). Phagocytosis is a major mechanism of cellular immun
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E is a classical initiator protein
2020-12-07
E1 is a classical initiator protein and, as such, plays several roles in the initiation and catalysis of viral DNA synthesis. E1 must first recognize a specific segment of the viral glycogen phosphorylase synthesis known as the “origin of DNA replication”, or “ori” for short. For most PV types exam
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As before all calculations are
2020-12-07
As before [3], [4], all calculations are based on thermodynamically first- and second-order hydropathic (amino acid) scales [6], [7], linearly scaled to a common center and a common range for each of the 20 amino acids. These are then converted to a triangular matrix , where is the length of a sli
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ICT is a product of icariin via the
2020-12-07
ICT is a product of icariin via the metabolism of intestinal bacteria with estrogen-like activities [33]. ICT as a bone-protecting agent can enhance osteoblast differentiation while suppressing osteoclastic differentiation in vitro [19], and stimulate osteogenic differentiation and inhibit adipogene
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The inhibition of mRFP Ub
2020-12-07
The inhibition of mRFP-Ub–E1 formation by ginsenosides Re was not in time-dependent in vitro (Fig. 4B). Fifty micrometres ginsenoside Rg1 decreased E1 activity to 0.24- to 0.36-fold over 30min. This finding suggests that ginsenoside Rg1 may irreversibly inhibit mRFP-Ub–E1 formation or a tight-bindin
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br Conflict of Interest br
2020-12-07
Conflict of Interest Acknowledgements Marques F. was supported by the Foundation for Science and Technology (FCT), Portugal, Grant UMINHO/BI/35/2012. This work was supported by FCT by the Project PTDC/AGR-AAM/70418/2006. Introduction β-methylamino-l-alanine (BMAA) exposure has long been as
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