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Ghrelin contains an n octanoylation at
2021-09-24
Ghrelin contains an n-octanoylation at its Ser3 residue (Kojima et al., 1999). While des-acyl ghrelin is found in high concentrations in the blood, only the lipidated form is active at GHSR (Bednarek et al., 2000). We previously showed that ghrelin interacts with the membrane via its lipid modificat
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Hyperactivation of Notch pathway can
2021-09-24
Hyperactivation of Notch1 pathway can give rise to transformation into T-ALL in murine models. In more than 50% of acute T-cell lymphoblastic leukemias oncogenic activating mutations of Notch1 have been detected and inactivation of Notch1 signaling impairs leukemia cell proliferation and promotes ap
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In vitro studies have described the kinetic parameters of th
2021-09-24
In vitro studies have described the kinetic parameters of the KDM4A catalytic site (cKDM4A) (Figure 1C) (23); the kcat/KM (kcat as the catalytic constant and KM as the Michaelis constant) values represent how fast the enzyme reacts with the substrate once it encounters the substrate, where the value
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Histamine H and H receptors are considered as low affinity
2021-09-24
Histamine H1 and H2 receptors are considered as low affinity receptors (pKi of 4.2 and 4.3 respectively), whereas histamine H3 and H4 receptors as a high affinity receptors (pKi of 8 and 8.2 respectively) (Schreeb et al., 2013). Therefore it might well be that other histamine receptors might be invo
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Previously we reported that the inhibition of PKC and
2021-09-23
Previously, we reported that the inhibition of PKC-ζ and PKC-ε activity in hypertrophic adipocytes had deleterious effects on EPA-induced GPR120-mediated VEGF-A production [12]. However, the activation of PKC-θ, -ζ and -λ can also enhance the phosphorylation of IKK and p65, and facilitate the transl
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br Introduction Inflammatory bowel diseases IBDs
2021-09-23
Introduction Inflammatory bowel diseases (IBDs) including Crohn's disease and ulcerative colitis (Baumgart and Sandborn, 2012; Beaugerie et al., 2006) are typically characterized by chronic, progressive, and relapsing inflammation of the intestine. Although the exact pathogenesis of IBD is unknow
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The differential tissue and ligand dependent signaling descr
2021-09-23
The differential tissue- and ligand-dependent signaling described here has important implications for the therapeutic potential of synthetic GPR109A agonists for the treatment of atherosclerosis. The failure of MK-0354, a biased, partial GPR109A agonist, to activate signaling pathways upstream of va
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br Animal models of NASH The human NAS system
2021-09-23
Animal models of NASH The human NAS system (see above) is largely reproducible in NAFLD mouse models [37] and, therefore, has been increasingly applied in the preclinical assessment of liver histological responses to test compounds. In general, the NAS system is well suited for this purpose, alth
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Several investigators including ourselves have
2021-09-23
Several investigators including ourselves have previously shown, that allogeneic HLA-DPB1 class II-alleles are powerful leukemia rejection PHA-665752 australia for CD4 T-cell therapy following allogeneic hematopoietic stem cell transplantation (Herr et al., 2017, Rutten et al., 2008, Stevanovic et
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Selective pharmacological inhibition of tonic currents indic
2021-09-23
Selective pharmacological inhibition of tonic currents indicated that the effects of gp120 are predominantly mediated by α5-containing GABAARs. The other dominant subtype that contributes to tonic current in the hippocampus, the δ-containing GABAAR, was unaffected by gp120 treatment. Additionally, i
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GT cells were treated in
2021-09-23
GT1-7 VX-661 sale were treated in two ways; specifically, they were either dosed or transfected with VP, reflecting the extracellular and intracellular actions of VP, respectively. A dose of 200 pg/ml VP in culture supernatants was effective in stimulating GnRH in the supernatant and cell extracts;
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Ironically another series of studies examining the role of
2021-09-23
Ironically, another series of studies examining the role of EAATs in CNS injury and disease suggest that under some pathological conditions, the operation of the EAATs is not protective, but actually contributes to the excitotoxic process (Rossi et al., 2000). The transporters do so by serving as th
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br Inclusion exclusion criteria br Quality assessment All
2021-09-23
Inclusion/exclusion criteria Quality assessment All studies included in the qualitative synthesis were evaluated using the Quality Assessment Tool for Quantitative Studies (QATQS), which allows to determine their methodological quality. QATQS assesses 8 sections: selection bias, study design,
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The LBD experiences a large scale conformational transition
2021-09-23
The LBD experiences a large-scale conformational transition between open and closed states upon agonist binding within the cleft separating the two lobes of the domain. The upper lobe (Lobe 1, also called D1) is connected to the ATD, and the lower lobe (Lobe 2, also called D2) is connected to the TM
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mimosine In summary our findings provide the evidence and
2021-09-23
In summary, our findings provide the evidence and the mechanistic understanding of the protective effects of GIP receptor agonist, D-Ala2GIP, in the MPTP-induced neurotoxicity in mice. The observed protective effects are potentially due to reduced oxidative stress and attenuation of dopamine loss in
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