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The frequency of GSTM and GSTT null genotypes vary in
2021-11-22
The frequency of GSTM1 and GSTT1 null genotypes vary in different populations. For example, Hiragi et al. (2007) reported a frequency of 17–35% for the GSTM1 null genotype and 22–44% for the GSTT1 null genotype in Brazilians of African descent (Hiragi et al., 2007). Chen, Liu, and Relling (1996) rep
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GPR belongs to the G
2021-11-22
GPR84 belongs to the G protein-coupled receptor family, and it was first identified from human peripheral blood neutrophils [,]. GPR84 is now considered to be a member of receptor for medium chain fatty xanthine oxidase (MCFA) with carbon chain lengths of 9–14 []. GPR84 is mainly expressed in bone
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In summary we have designed and optimized a
2021-11-22
In summary, we have designed and optimized a new series of 1,4-dioxycyclohexane GPR119 agonists. SAR studies led to the discovery of the preferred molecule that has potent and efficacious GPR119 activity across species. This lead compound exhibited an excellent ADME and safety profile, and demonstra
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The expression of heat shock proteins HSPs can
2021-11-22
The expression of heat-shock proteins (HSPs) can be upregulated by viral infection, nutritional deficiency, TNF-α and oxidative stress in Agarose GPG/ME mg [44], [45] HSPs are classified in six families (including the HSP10, HSP40, HSP60, HSP70, HSP90 and HSP100 families). HSP90 [46] for example pr
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In glioma or glial derived primary brain tumors as in
2021-11-22
In glioma, or glial-derived primary 6-Hydroxydopamine hydrobromide tumors, as in other cancers, glutathione is an important survival mechanism. Glioma cells are dependent upon SXC-mediated cystine uptake for viability, as they require intracellular cystine/cysteine for GSH synthesis (Ogunrinu and S
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The structure and activity of GLUT has been most
2021-11-22
The structure and activity of GLUT1 has been most intensively studied in erythrocytes, in which this transporter makes up 10–20% of membrane protein content. Carruthers has shown that, while GLUT1 can exist and transport glucose as monomers, dimers and tetramers, in erythrocytes GLUT1 exists predomi
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In the present studies we found that genistein
2021-11-22
In the present studies, we found that genistein did not antagonize fMLF-induced Ca2+ mobilization in FPR1-HL60 3,4-DAA and human neutrophils. Thus, the previously reported inhibitory effect of genistein on fMLF-stimulated degranulation, aggregation, and reactive oxygen species (ROS) production in h
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br Heme and the HO
2021-11-20
Heme and the HO system Heme, a complex of iron and protoporphyrin IX, has versatile functions, which are critical for the survival of all aerobic organisms including mammalians and bacteria [9]. The central iron in heme facilitates six ligand binding sites [10], four of which are occupied by nitr
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Ceftazidime In an effort to further improve the intrinsic
2021-11-20
In an effort to further improve the intrinsic potency, we evaluated the effect of the C4-substituent of the triazole (). Replacement of the phenyl group with a cyclohexyl or with a 2-pyridyl substituent led to losses in potency. Increasing the size of the substituent to a bi-phenyl or naphthyl grou
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The Y H D A variant was
2021-11-20
The Y56H/D168A variant was resistant to all tested PIs, and the inhibitor binding mode determined the molecular mechanism of resistance. Prior to the development of grazoprevir, PIs typically contained large heterocyclic P2 moieties that strongly interacted with S2-subsite residues (Ali et al., 2013
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br Activation of soluble guanylate cyclase
2021-11-20
Activation of soluble guanylate cyclase The molecular steps involved in sGC activation have evolved significantly over the last several years. The key studies are outlined below, but here we provide an overall summary. The activation mechanism of sGC was initially proposed to be relatively simple
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Introduction Non alcoholic hepatic steatosis is characterize
2021-11-20
Introduction Non-alcoholic hepatic steatosis is characterized by the presence of steatosis in hepatocytes [1], which leads to the development of fatty liver [2]. It is strongly associated with obesity, insulin resistance, and type II diabetes [3]. They are major risk factors of non-alcoholic hepati
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Acknowledgment br Main Text From birth to adulthood
2021-11-20
Acknowledgment Main Text From birth to adulthood, humans progressively acquire and maintain a complex microbial ecosystem at various body sites and cavities. Early on, these microorganisms establish a complex relationship with the host, resulting in the modulation of several biological functions
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br Experimental Procedures Information on the
2021-11-19
Experimental Procedures Information on the materials used in this study and the details of how the in vivo and in vitro assays were performed are provided in Supplemental Information. Acknowledgments This research was supported by the National Research Foundation of Korea (NRF) grant funded b
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br Hydroxyfarnesyl diphosphate was synthesised in three step
2021-11-19
12-Hydroxyfarnesyl diphosphate (6) was synthesised in three steps starting from commercially available (E,E)-farnesol (10) (Scheme 5). Chlorination of 10 gave farnesyl chloride (11) in a quantitative yield, which was carried forward without purification. The following step was a selenium dioxide-c
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