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To further verify the effect of BBR on
2021-05-10
To further verify the effect of BBR on ACAT2 protein expression, we have conducted an in vitro permeability assay using Caco-2 monolayer. This assay has long been used to predict the in vivo glutathione reductase and bioavailability of a compound. It was observed that the amount of cholesterol este
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In a study performed simultaneously by
2021-05-10
In a study performed simultaneously by another group, EWS-FLI-1 introduction into unsorted murine bone marrow-derived AM251 resulted in tumors with various phenotypes including one that is consistent with that of Ewing sarcoma [68]. The tumors expressed markers associated with Ewing sarcoma and dis
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Estrogen receptor related receptor ERR
2021-05-10
Estrogen receptor-related receptor γ (ERRγ), like other members of the ERR subfamily, is a constitutively active orphan nuclear receptor, though unlike ERRα and β, it is more selectively expressed in metabolically active and highly vascularized tissues such as heart, kidney, brain, and skeletal musc
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The effect of ET activity on the
2021-05-10
The effect of ET-1 activity on the development of experimental pulmonary fibrosis has also been examined by other investigators. One study found that repeated administration of Bosentan, an ERA used to treat pulmonary arterial hypertension (PAH), significantly decreased bleomycin-induced pulmonary f
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br Materials and methods br Results
2021-05-10
Materials and methods Results + discussion Conclusions We have demonstrated the systematic optimization of the functional folding of a CF synthesized GPCR. The approach addresses central issues relevant for many membrane proteins such as disulfide bridge formation, proper hydrophobic enviro
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Previous studies have indicated that hSSB may be phosphoryla
2021-05-10
Previous studies have indicated that hSSB1 may be phosphorylated at threonine residue 117 (T117) [13] and acetylated at lysine residue 94 (K94) [15], both of which promote hSSB1 function in response to ionising radiation exposure. Mass spectrometry screens of proteins immunoprecipitated with phospho
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We then undertook computational studies
2021-05-10
We then undertook computational studies that suggest the cyanobacterial ALDH (and planctomyces ALDH) represent the evolutionary ancestor of human and other eukaryotic ALDH1/2 given that cfALDH contains signature residues matching both the human proteins throughout the surface of the protein and the
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br Additional CDKs with a role in cancer
2021-05-10
Additional CDKs with a role in cancer Small molecule CDK inhibitors The majority of protein kinase inhibitors developed to date are type I inhibitors: they bind at the ATP–binding site, are ATP-competitive and target the kinase in its active state; with the activation loop DFG motif in the ‘in
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The changes in the chemokine receptors CCR
2021-05-10
The changes in the chemokine receptors CCR-5 and CXCR-4 in women and men with PTSD are completely different. In the group of women with PTSD alone the level of this 6015 receptor increased six times, whereas, in women with APD and PTSD, the level of the receptor CCR-5 was eight times higher than in
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Pralatrexate mg Recent studies investigating the effects of
2021-05-10
Recent studies investigating the effects of mesenchymal stem cell (MSC) therapy in rodent models including chronic renal failure and glomerulonephritis have demonstrated that MSC therapy can result in beneficial effects [57], [58]. In cats, autologous intra-renal injections of either adipose tissue-
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Dopamine activity in the PFC and striatum
2021-05-08
Dopamine activity in the PFC and striatum may be antagonistic, meaning that lower levels of dopamine in the striatum tend to correspond to higher levels of dopamine in the PFC and vice versa (Cools and D'Esposito, 2011; Tunbridge et al., 2006). Human PET studies have reported that dopaminergic PFC f
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Ligand independent activation of neuronal nuclear estrogen r
2021-05-08
Ligand-independent activation of neuronal nuclear estrogen receptors may also continue to occur in absence of ovarian estrogens. AF-1 requires intracellular kinase cascade-dependent phosphorylation of specific residues in the A/B domain of nuclear estrogen receptors (Le Goff et al., 1994; Kato et al
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Endothelial dysfunction has been associated with
2021-05-08
Endothelial dysfunction has been associated with most of the established cardiovascular risk factors, such as hypercholesterolemia, hypertension, smoking, diabetes mellitus, a positive history of premature CAD and elevated ampk pathway homocysteine 4, 26, 27. Endothelial dysfunction is present in t
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Another important consideration with respect
2021-05-08
Another important consideration with respect to drug conditioning suggested by the present findings is the observation of an attenuated PRIMA-1 australia on the second extinction trial. Seemingly, if ERK measurements were made following a partial reduction in the conditioned response the ERK respon
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Further modifications on the position of
2021-05-08
Further modifications on the 8-position of compound led to compound 4 (8-pCPT-2′--Me-cAMP, a.k.a. 007, ), which is a potent (half-maximal activation of EPAC1 at 2.2µM) and selective (about 100-fold EPAC/PKA selectivity) EPAC agonist. Since the discovery of compound , it has been widely used as a po
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