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Among the compounds prepared at this
2021-11-12
Among the compounds prepared at this stage, the cyclopropylmethylenoxy analogue attracted our most attention since it demonstrated particularly good in vitro potency at GlyT1 (16nM), no activity at the GlyT2 isoform up to the highest concentration tested (30μM), good physical properties with modera
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PFI-2 Pediatric cancers are fundamentally different from adu
2021-11-12
Pediatric cancers are fundamentally different from adult tumors and usually display a lower mutational burden and a faster growth rate. About 30% of all childhood malignancies are solid tumors and, in a majority of cases, respond well to chemotherapy. However, in particular in neuroblastoma the succ
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This study was approved by our
2021-11-12
This study was approved by our institutional ethics committee, and informed consent was obtained from each participant or legal guardian. We performed whole-genome SNP genotyping in the one unaffected and two affected siblings by using the Illumina Human 610 Genotyping BeadChip panel, which interrog
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The effect of GCK NES mutations on enzyme kinetics
2021-11-12
The effect of GCK-NES mutations on enzyme kinetics and protein stability might account for the hyperglycaemia that characterizes MODY2 patients, since reduced GCK activity would increase the threshold for glucose stimulated insulin release in beta-cells [31,37,49]. However, a more in depth functiona
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Ketamine has recently been found to exert rapid and
2021-11-12
Ketamine has recently been found to exert rapid and sustained antidepressant effect. Single dose ketamine can have an efficacy of up to 1 week [20]. Furthermore, ketamine is an effective drug against refractory depression [21,22]. The antidepressant mechanism of ketamine is still unclear. Whether CO
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N6-Methyl-dATP Immunohistochemistry analysis shown ghrelin a
2021-11-12
Immunohistochemistry analysis shown ghrelin and GHSR-1a immunostaining was located in the epithelial cells of N6-Methyl-dATP and ducts throughout the lactation, strong immunoreactive cells were detected in L30, L60 and L120 stage. The distribution of ghrelin has been shown in many tissues, includin
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Due to the versatility of the ghrelin system and its
2021-11-12
Due to the versatility of the ghrelin system and its multiple functions, dysregulation in some of the components of the ghrelin system, such as ghrelin, GOAT, and GHSR, might lead to pathogenesis of many endocrine-related diseases, including obesity, short stature, cancer, inflammatory, and cardiova
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FFAs concentration response curves for increasing intracellu
2021-11-12
FFAs concentration–response curves for increasing intracellular calcium and receptor phosphorylation showed a difference of ≈1 order of magnitude indicating a relatively large receptor reserve, which is expected for a transfected model, and that high receptor occupancy is necessary to induce recepto
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We then explored the possible mechanisms by
2021-11-12
We then explored the possible mechanisms by which integrin α5β1 was involved in the PHEV proliferation process. Normally, the virus activates integrin and induces its downstream protein activation to promote its own invasion and proliferation. Human papillomavirus type 16 (HPV16) binds to heparan su
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br Interference in coagulation assays Conversely
2021-11-12
Interference in coagulation assays Conversely to heparin, or heparin like D609 synthesis (LMWH, Fondaparinux, Sodium Danaparoid), which are catalytic inhibitors requiring the presence of AT for their activity, as depicted on Fig. 2, DiXaIs are directly targeted to Factor Xa, and are reversible [
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There has been conflicting evidence on the possible receptor
2021-11-12
There has been conflicting evidence on the possible receptor mechanisms that mediate the neuro-immuno-modulatory effects of FAAH substrates. Evidence from in vitro studies indicates that AEA-mediated modulation of TLR4-induced neuroinflammation may be mediated by CB1/CB2 receptor dependent (Correa e
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The biochemical cell culture activities and
2021-11-12
The biochemical, cell culture activities and properties of bicyclic carboxamides are compiled in , with the prototype of the series, 4-fluorobenzyl carboxamide , displaying an antiviral profile comparable to the spirocyclic carboxamide . The introduction of a small hydrophobic methyl () and chlori
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Fig C presents the secondary structure arrangement of the
2021-11-12
Fig. 1(C) presents the secondary structure arrangement of the PAS-A and PAS-B domains in both HIF-2α and ARNT. The common scaffold of the PAS domains is a β sheet with numerous flanking α helixes. The PAS-A domains of both HIF-2α and ARNT have A’α, Aβ, Bβ, Cα, Dα, Eα, Fα, Gβ, Hβ, and Iβ from the N t
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Metal organic frameworks MOFs have emerged
2021-11-12
Metal–organic frameworks (MOFs) have emerged over the past two decades with the potentials to act as promising materials in gas storage, chemical separation, catalyst, magnetism, sensing, and drug delivery etc (Du et al., 2013, Zhou and Kitagawa, 2014). Additionally, the secondary interactions, such
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Recently it has been found that treatment of
2021-11-12
Recently, it has been found that treatment of human phagocytic PyBOP receptor or microvascular endothelial cells with NO donors inhibited the O2− generating capacity of NADPH oxidase [[8], [9], [10], [11]], which may involve down-regulation or S‑nitrosylation of the p47phox subunit (a cytosolic sub
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