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In the preclinical evaluation of CRF receptor antagonists
2021-05-31
In the preclinical evaluation of CRF1 receptor antagonists, effects were mainly focused on the regulation of hyperactivated HPA axis and the modulation of anxiety or depressive-like behaviors in CRF challenge [16], [17], [18] or stress models [16], [19], [20]. However, it remains to be concluded whe
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The availabilities of serotonin and dopamine are modulated b
2021-05-28
The availabilities of serotonin and dopamine are modulated by the serotonin transporter and catechol-O-methyltransferase enzyme. The serotonin transporter (5-HTT) is a key protein that reuptakes serotonin from the synaptic cleft back into synaptic boutons (Coleman et al., 2016; Talvenheimo et al., 1
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Future advances in the in vivo
2021-05-28
Future advances in the in vivo molecular imaging of enzyme activity will greatly benefit from the progress towards the quantitative detection of enzymes. Quantitative imaging requires knowledge of both the location and concentration of a specific enzyme, which is dependent on the simultaneous measur
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Regardless of its effect on
2021-05-28
Regardless of its effect on EBV infection, the chemokine system has been found to be regulated in both nasopharyngeal cancer and Hodgkin lymphoma. As such, Hodgkin and Reed–Sternberg (HRS) cells from Hodgkin lymphoma and nasopharyngeal carcinoma cells have been shown to express CXCL8 and CCL17. Furt
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DGK is classified into the type II DGK subfamily As
2021-05-28
DGKη is classified into the type II DGK subfamily [12], [13], [14], [15]. As described above, DGKη has the splice variants η1 and η2 [10]. DGKs η1 and η2 possess in common a pleckstrin homology domain at the N-terminus and a catalytic domain that is divided into two subdomains (catalytic subdomain-a
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br Results and discussion br Conclusions An optimization
2021-05-28
Results and discussion Conclusions An optimization study of the dipeptidyl enoates was performed by chemical structure modifications (Fig. 5). Compound FGA50 displaying R configuration at C-3 was more active than its epimer FGA40. Two modifications of the chemical structure of FGA50 were done:
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Previous studies revealed the expression of the CCR receptor
2021-05-28
Previous studies revealed the expression of the CCR3 receptor in neurons and its neuroprotective function using mice lacking CCR3 expression (Wainwright et al., 2009). The regulation of CCR3 receptor expression in the microglia and astrocytes was shown in neurological disorders and has been demonstr
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GSK 2830371 DDX belongs to the DEAD
2021-05-28
DDX3 belongs to the DEAD-box family of proteins, ATP-dependent RNA helicases characterized by the presence of a highly conserved helicase core domain [13]. This catalytic core is composed of two RecA-like domains containing motifs involved in ATP binding/hydrolysis, RNA binding and helicase activity
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Introduction Neuropathic pain occurs in approximately one
2021-05-27
Introduction Neuropathic pain occurs in approximately one-third of patients with diabetes and is refractory to currently available analgesic drugs (Abbott et al., 2011). This painful diabetic neuropathy (PDN) is associated with elevated levels of methylglyoxal (MG; a reactive glucose metabolite) an
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Anaesthetized mice of one eNOS KO strain
2021-05-27
Anaesthetized mice of one eNOS-KO strain showed a paradoxical decrease in blood pressure (BP) in response to i.p. administration of the NOS-inhibitor L-NA suggesting a role for non-endothelial isoforms of NOS in maintaining BP [1]. Alternatively, diminution in the activity of the renin-angiotensin
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cevimeline br Funding This work was partly supported by the
2021-05-27
Funding This work was partly supported by the grant ‘Maria Grazia Cuccoli’ from Fondazione Cassa di Risparmio di Bologna. Declarations of interest Acknowledgements Introduction The main strategy of oncolytic viral therapy is based on the fact that naturally occurring or engineered virus
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br Experimental Procedures br Author Contributions br Acknow
2021-05-27
Experimental Procedures Author Contributions Acknowledgments Introduction In addition to the HLA region numerous other loci have shown association with type 1 diabetes risk [1], and susceptibility farnesyl diphosphate synthase have been identified in many of these regions [2]. How these
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Cyanine 5-dCTP mg Proteases as multifunctional enzymes play
2021-05-26
Proteases, as multifunctional enzymes, play key roles in controlling a wide variety of cellular and extracellular processes in plants and animals, including protein degradation and processing, germination, complement activation, inflammation, responses to environmental stimuli, senescence and so on.
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The requisite extended benzyl alcohols
2021-05-26
The requisite extended benzyl alcohols –, , and and final potential DFG-out binding hybrid inhibitors – and – were prepared as shown in , . Benzaldehyde was alkylated with -methoxybenzyl chloride and then reduced with sodium borohydride to give benzyl alcohol . Pyridine derivative was prepared by
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In a cell based functional assay the antagonist
2021-05-26
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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