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br Conclusions The results of this work showed
2021-12-30

Conclusions The results of this work showed that β-glucosidase could be efficiently immobilized onto hydroxyapatite nanoparticles in a single adsorption step. The enzyme adsorption was accomplished by coordination bonds between remaining Ca2+ sites of HA and COO− of amino acids. The immobilizatio
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Viroptic br Regulation of GCK by intrinsic conformational dy
2021-12-30

Regulation of GCK by intrinsic conformational dynamics GCK is a 465-residue, 52-kDa enzyme comprised of two domains, hereafter referred to as the large domain and the small domain, that are separated by a flexible hinge region. As with other proteins that adopt the hexokinase fold, substrates bin
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Cortisol targets many organs and tissues and has
2021-12-30

Cortisol targets many organs and tissues and has certain effects on metabolism, including promoting glycolysis. It can cross the blood b ng barrier and act centrally to regulate HPA axis activity by activating negative feedback mechanisms effectively, cortisol inhibits its own production (Fairchild,
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Importantly the levels of the pro inflammatory
2021-12-30

Importantly, the levels of the pro-inflammatory cytokines TNF-α and IL-1β and Nf-κB, a key transcription factor in chronic inflammatory responses that is activated by pro-inflammatory cytokines, were also reduced by the drugs, confirming our previous results that demonstrated anti-inflammatory effec
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Furthermore our results are the
2021-12-29

Furthermore, our results are the first to demonstrate that the stimulating effect of GALP on AVP release in rats is independent of galanin receptors. The same stimulatory GALP influence on AVP secretion has been also observed in the presence of galantide, an antagonist of Gal receptors in the incuba
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br General features of FGFRs and inhibitors br Conclusion Gi
2021-12-29

General features of FGFRs and inhibitors Conclusion Given the critical role of FGFRs in the progression of tumors, the co-crystal structures of these kinases in complex with inhibitors are determined in order to clarify the mechanism of actions and explore new efficient inhibitors. This manusc
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Canonical and non canonical Wnt
2021-12-29

Canonical and non-canonical Wnt signaling pathways play essential roles in various cellular activities, including cell fate determination, proliferation, migration and gene expression [57]. The canonical Wnt pathway (β-catenin dependent pathway), is activated by the binding of Wnt ligands, leading t
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ADAM has two alternative splicing forms a membrane anchored
2021-12-29

ADAM12 has two alternative splicing forms, a membrane-anchored long form (ADAM12-L) and a secreted short form (ADAM12-S). Both the long and short forms have metalloproteinase, disintegrin, cysteine-rich, and epidermal growth factor-like domains and can shed pro-heparin binding-epidermal growth facto
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Compounds and were evaluated for their pharmacokinetic
2021-12-29

Compounds and were evaluated for their pharmacokinetic properties in rats and the results are summarized in . Following intravenous (IV) administration, both compounds displayed low clearance (CL), short half-lives (t) and low volumes of distribution (V). When dosed orally as a solution, exposure
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It is apparent from the data
2021-12-29

It is apparent from the data in that none of the ligands exhibits significant toxicity as determined by the viability of human embryonic kidney (HEK 293) cells at a concentration of 100 μM. It is also apparent from the data in and that a number of the ligands inhibit the HIV-1 IN enzyme. However,
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The primary physiological role of the HO system
2021-12-29

The primary physiological role of the HO system is the protection of Peficitinb from oxidative stress. These cytoprotective effects are attributable both to the degradation of the pro-oxidant heme and to the positive contribution of the metabolites produced during this degradation, namely CO, BV, an
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GSK621 The inhibition of HDAC increases the level of
2021-12-29

The inhibition of HDAC increases the level of histone acetylation and consequently turns the chromatin to be loose and active, allowing multiple transcription factors to access to promoters of diverse genes including tumor suppressor genes []. As compound possessed potent HDAC inhibitory activity an
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In summary P P macrocyclization proved to
2021-12-29

In summary, P2-P4 macrocyclization proved to be an effective strategy to drive activity in this series of HCV NS3 protease inhibitors while microsomal stability was enhanced by the introduction of steric bulk along the tether. This modification augmented the previously-described tactic of improving
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The diseases of ocular surface and
2021-12-29

The diseases of ocular surface and the cornea are very common in ophthalmological practice and as a result there is a continuous, need for novel therapeutic options. Here, we demonstrated a corneal distribution of GPR35, a potential molecular target for new drugs (; ). The search for the expression
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Some years ago it has been described that
2021-12-29

Some years ago, it has been described that CD45RA+ CD62L+ naïve CD4+ T autophagy inhibitor can be further differentiated into two distinct subpopulations by analysing their surface expression of CD31(Kimmig et al., 2002a; Kohler and Thiel, 2009; Kohler et al., 2005b). CD31+ thymicnaive CD4+ T cells
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