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Unfortunately the approved drugs suffer from failure in
2021-11-06

Unfortunately, the approved drugs suffer from failure in many cases [5,6]. Several mutations occur in the binding site of NS3/4A protease, which affect drug binding and cause drug resistance [13]. It is a big challenge and needs more efforts to be done. This is the reason why research is still conce
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The physiological and pharmacological roles of GPR remain la
2021-11-05

The physiological and pharmacological roles of GPR81 remain largely unclear because of several reasons. The low potency of lactate agonizing GPR81 in the millimolar range, together with its fast metabolic turnover, renders as a challenge in in vivo studies using lactate. Furthermore, there are no po
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br Introduction Few decades after of HIV
2021-11-05

Introduction Few decades after of HIV/AIDS diagnosis, it has been still a health problem and impact will continue in the next decades. In 2015, HIV/AIDS was the 12th cause of death in the world and it's estimated that 1.2 million people was died of HIV/AIDS this year. In the global epidemiologica
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The effects of these steroids
2021-11-05

The effects of these steroids, namely the decrease in the peak and acceleration of desensitization could be observed in IGly activated by 100 μM glycine (concentration close to EC50). However, with an increase in glycine to 500 μM (a concentration close to saturating), the effect of steroids on the
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br Materials and methods br Results br Discussion
2021-11-05

Materials and methods Results Discussion Here, we investigated the inhibitory effects and associated mechanisms of phloroglucinol on α-glucosidase. Our results showed that phloroglucinol reversibly inhibited α-glucosidase in a dose-dependent manner (Fig. 1), with the double-reciprocal plot
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Until now various reports have demonstrated
2021-11-05

Until now, various reports have demonstrated the therapeutic potential of enzyme-resistant forms of GIP in experimental diabetic animal models , , . In essence, structural modifications performed at the Tyr residue in GIP generate analogues that are completely resistant to the actions of DPP-IV and
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nnos As many of the above studies highlight several decades
2021-11-05

As many of the above studies highlight, several decades of research on Cx43 has revealed that many of these functional roles are attributed to the C-terminal domain (CT) of this protein which cannot be explained by the formation and existence of intercellular channels. Recent findings on the existen
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In perimenstrual catamenial epilepsy there is emerging
2021-11-05

In perimenstrual catamenial epilepsy, there is emerging evidence to suggest that P withdrawal plays a key role in seizure exacerbations occurring around the time of menstruation (Backstrom et al., 1984, Bonuccelli et al., 1989, Scharfman and MacLusky, 2006). The mechanisms underlying ovarian cycle-r
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DNAzymes a series of nucleotide sequences with specific cata
2021-11-05

DNAzymes, a series of nucleotide sequences with specific catalytic activity, have been reported frequently applied in detection assays for such as ions and amino acids, due to the advantage in stability, high cost-effectiveness and modification convenience, by comparison with protein enzymes. The DN
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AG-126 In addition to the robust
2021-11-05

In addition to the robust intracellular calcium mobilisation, DHA and TUG-891 also induced MMP-9 granules release and superoxide production, supporting a key role of calcium in bovine neutrophil defense responses (Burgos et al., 2011). Pisani et al. (Pisani et al., 2009) described a reduction of bas
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In this study according to
2021-11-05

In this study, according to the critical pharmacophore T31, Y113 and R140 of FBPase, using the strategy of pharmacophore-based virtual screening, a series of novel scaffold inhibitor targeted the AMP binding site of FBPase were screened, their inhibitory activities against FBPase were further tested
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br Materials and methods br Results br Discussion
2021-11-05

Materials and methods Results Discussion EZH2 is a subunit of the polycomb repressive complex, which trimethylates lysine 27 on histone 3, a repressive marker for gene expression. EZH2 is important for cancer cell proliferation, migration, and invasion, all of which are associated with canc
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casein kinase EZH affects cancer by regulating the expressio
2021-11-05

EZH2 affects cancer by regulating the expression of target genes [22]. EZH2, together with SUZ12 and EED, forms the polycomb repressive complex 2 (PRC2), which catalyzes trimethylation of histone H3 lysine 27 (H3K27me3) [23,24]. PRC2 may recruit other polycomb complexes, DNA methyltransferases, and
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Classical drugs target the viral enzymes reverse transcripta
2021-11-05

Classical drugs target the viral resveratrol reverse transcriptase (RT), protease and integrase (IN) [[4], [5], [6]]. Raltegravir (ISENTRESS/MK-0518) is the prototypical integrase strand transfer inhibitor (INSTI) leading to an extremely strong reduction in viral load [7] and it has been approved fo
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Hypoxia HIF and Inflammation Cellular responses to hypoxia
2021-11-05

Hypoxia, HIF, and Inflammation Cellular responses to hypoxia are essential for life and are now recognized to be dysregulated in a wide range of disease processes. The key players in these pathways are a family of transcription factors, the hypoxia-inducible factors (HIFs; see Glossary), as well as
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