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HSOR belonging to the aldoketo reductase superfamily is a
2021-11-29

3α-HSOR, belonging to the aldoketo reductase superfamily, is a rate-limiting enzyme for the synthesis of 3α-reduced steroids, such as allopregnanolone and tetrahydrodeoxycorticosterone. 3α-HSOR was extensively expressed in the spinal dorsal horn and was upregulated following peripheral nerve injury,
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The widespread involvement of HH GLI in
2021-11-26

The widespread involvement of HH/GLI in human malignancies has initiated a remarkable effort to identify selective HPIs. As shown in Table 2.1, most of these small molecule inhibitors target the essential effector protein SMO, which should lead to pathway abrogation by eventually decreasing the GLIA
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br Conclusions We concluded that the
2021-11-26

Conclusions We concluded that the inhibitory effects of propofol on fMMYALF-induced neutrophil activation are mediated by competition with FPR1, which inhibits receptor-mediated downstream signaling and inflammatory responses such as oxidative burst, elastase release, and chemotactic migration (F
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2-Phenyl-2-(1-piperidinyl)propane Moreover studies on subcel
2021-11-26

Moreover, studies on subcellular localization of FBPase in carp heart and smooth muscle revealed nuclear localization of the enzyme. Previously, we have unequivocally demonstrated the presence of FBPase in the nuclei of mammalian cardiomyocytes (Gizak and Dzugaj, 2003) and myocytes (Gizak et al., 20
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The suboptimal trypsin selectivity profile
2021-11-26

The suboptimal trypsin selectivity profile of DPC423 prompted us to investigate additional P moieties for potency and selectivity. Glycinamide P () showed low nanomolar binding affinity against fXa which suggested that this P moiety sits deeper into the S pocket of fXa. To further elaborate on this
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Recent findings of us suggest that
2021-11-26

Recent findings of us suggest that compounds that inhibit both FAAH and TRPV1 may be more efficacious in pain relief than those targeting only one such protein. As continuation of our efforts to identify new molecules able to target simultaneously both FAAH and TRPV1 receptors, we hypothesized that
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Enhancer of zeste homolog EZH which functions as a methyltra
2021-11-26

Enhancer of zeste homolog 2 (EZH2), which functions as a methyltransferase, is a critical subunit of polycomb repressive complex 2 (PRC2), which has been demonstrated to be involved in the development of the jak inhibitors [23]. Aberrant expression of EZH2 has been found to be associated with a var
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Previous studies have shown that inhibition of
2021-11-26

Previous studies have shown that inhibition of voltage-gated Na+ Z-WEHD-FMK has a reduced effect on GABAergic boutons compared with other neurotransmitter phenotypes,46, 47 and voltage-gated Na+ channel subtypes are differentially expressed in hippocampus. In addition, SV exocytosis evoked by eleva
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br Results br Discussion Impaired BBB
2021-11-26

Results Discussion Impaired BBB functions evoke vasogenic edema, which elevates intracranial pressure and leads to a life-threatening condition (Sperk, 1994, Unterberg et al., 2004, Simard et al., 2007). In addition, vasogenic edema formation results in the worsen consequence contributing to p
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The biochemical cell culture activities and properties
2021-11-26

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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Describing histone acetylation machinery in rivulus will
2021-11-26

Describing histone acetylation machinery in rivulus will provide a basis for understanding the role of epigenetic mechanisms in mediating phenotypic variation, by guiding both phenotypic flexibility in adults and developmental plasticity in young. Together with its biological characteristics, rivulu
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The repurposing of well characterized and well tolerated
2021-11-26

The repurposing of well-characterized and well-tolerated drugs in order to treat illnesses for which they were not originally intended has emerged as an attractive alternative to a long and costly process of drug development. Repositioning antihistaminergic ligands seems a promising idea given that
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Taken together this study provides the proof
2021-11-26

Taken together, this study provides the proof of concept that our novel heterologous human/rat HER2-specific T cell vaccine HuRt-TEXO, which is capable of stimulating both humoral and CTL responses leading to potent antitumor immunity through the circumvention of HER2 tolerance in double transgenic
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Finally worth of mention are few papers that report
2021-11-26

Finally, worth of mention are few papers that report on the discovery of HO-2 selective inhibitors. In 2013, starting from the screening of a calcitonin gene related peptide library, the above-mentioned Canadian research group identified Clemizole (Table 6) as a new hit compound for the development
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To identify factors associated with being
2021-11-26

To identify factors associated with being HCV-unaware, univariable and multivariable logistic model were used, odds ratios, 95% confidence intervals and p-values were reported. We included in the multivariable model factors associated with unawareness of HCV infection in univariable analysis with a
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