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The transcription factor Nrf is a master regulator of
2021-12-29

The transcription factor Nrf2 is a master regulator of cytoprotective responses to endogenous and exogenous stresses caused by reactive oxygen species (ROS) and electrophiles [6]. Nrf2 promoter polymorphisms are significantly associated with the development of gastric mucosal inflammation, either in
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Among the GSK inhibitors available in market lithium is prob
2021-12-29

Among the GSK-3 inhibitors available in market, lithium is probably the only example and the oldest one. Some molecules, both natural and synthetic, such as maleimide derivatives, staurosporine (from the bacterium Streptomyces storosporeus), indole derivatives such as indirubin (used since long in t
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br Materials and methods br Results Human adipocytes differe
2021-12-29

Materials and methods Results Human adipocytes, differentiated from fibroblastic preadipocytes in culture, were incubated with IL-33 for either 3 or 24 h to examine acute and prolonged responses to the cytokine. Low, medium and high concentrations of IL-33 were employed. IL-33 had no significa
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Notably we observed that GPR activation induced by PA
2021-12-29

Notably, we observed that GPR35 activation induced by PA, an in vivo GPR35 agonist [6], significantly decreased DAI, colon weight, and histological score, while increasing colon length in mice with DSS-induced colitis. Furthermore, fibronectin and integrin α5 were co-localized with GPR35 on the colo
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The mechanisms of action of MMF and DMF are not
2021-12-29

The mechanisms of action of MMF and DMF are not well understood, but a growing body of evidence has demonstrated that DMF may act on both the neurodegenerative and inflammatory response of MS patients. The majority of the data related to the mechanism of action of DMF/MMF demonstrates the associatio
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br Discussion Naloxone and CTAP were able to alter
2021-12-29

Discussion Naloxone and CTAP were able to alter the febrile response induced by gp120. This effect was particularly evident during the initial hours following gp120 administration (90–210min). We also investigated the potential role of the delta-2 opioid receptor in gp120-induced fever. The delta
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Trypanosomatid GLO enzymes are monomeric and contain
2021-12-29

Trypanosomatid GLO2 enzymes are monomeric and contain a zinc–iron binuclear metal center (Irsch and Krauth-Siegel, 2004, Silva et al., 2008), similar to all other glyoxalases II. As mentioned, in T. brucei there are two GLO2 genes but only one encodes an enzyme with glyoxalase II activity (Irsch and
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br Materials and methods br Results br
2021-12-29

Materials and methods Results Discussion DNA repair pathways have evolved for a long time to act independently of one another. However, over the past decade several overlaps and crosstalks between these pathways were identified, showing that the DNA repair system is more complex than previo
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We noticed that the spontaneous openings of
2021-12-29

We noticed that the spontaneous openings of the D97R α1 GlyR appeared to be quite similar to those elicited by a maximally-effective glycine concentration on wildtype GlyR; both generated similar open and shut dwell-time histograms, both exhibited openings grouped into clusters with Popen values gre
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The GlyR is pentameric with each subunit
2021-12-29

The GlyR is pentameric, with each subunit consisting of an extracellular ligand binding domain (LBD), four transmembrane (TM) segments, and a large intracellular loop between TM3 and TM4. Binding of neurotransmitter produces conformational changes that are rapidly transmitted to the membrane-spannin
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Many studies support that Gli transcription factors are
2021-12-29

Many studies support that Gli transcription factors are not solely regulated by Hh/smo signaling but are also influenced by crosstalk with other pathways, such as RAS, PI3K/AKT, transforming growth factor-b/SMAD, PKC, or extracellular signal-regulated kinase pathways which are downstream and indepen
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The highest metabolic stability observed for compound
2021-12-28

The highest metabolic stability observed for compound 4k (EC50=0.41μM corresponding to 218ng/mL) among the four selected frontrunner candidates was the principal decisive point in nominating this compounds for pharmacokinetic characterization in mice at the dosage of 10mg/kg (administered intravenou
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In this study we present
2021-12-28

In this study, we present the first data on the kinetic properties of the hexokinase of T. equiperdum, which we compare with similar data available for pleomorphic T. brucei (Seed and Baquero, 1965, Nwagwu and Opperdoes, 1982, Hara et al., 1997, Morris et al., 2006, Chambers et al., 2008b, Chambers
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In addition to lifestyle factors genetic factors
2021-12-28

In addition to lifestyle factors, genetic factors may also influence the efficacy of antineoplastic drugs in breast cancer patients.16, 17 The HER2 gene contains several single nucleotide polymorphisms (SNPs). Two of the most investigated HER2 SNPs are Ile655Val (rs1136201) and Ala1170Pro (rs1058808
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These inhibitors possess a cap group
2021-12-28

These inhibitors possess a cap group build from cyclization of several amino-acid or non-amino-acid residues, four or more, with one residue bearing an alkyl arm terminated by ZBGs of various types: thiols, ketones or epoxides. In the case of romidepsin 30 (Fig. 7), the thiol group is initially in a
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