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Interestingly the rabbit cornea exhibited a more than
2022-04-18
Interestingly, the rabbit cornea exhibited a more than two-fold higher level of total GST activity compared with that of the porcine cornea, whereas their levels of GSTO1‐1 and GSTP1‐1 activity were similar (Fig. 4). Because members of the GST Alpha, Mu, Pi and Omega SGC707 primarily utilize CDNB a
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All experiments in this study were performed at pD for
2022-04-18
All experiments in this study were performed at pD 6.1 for reasons described above. This leaves a question about the implications of stereochemistry in vivo. At physiological pH the GSTP1-1 catalyzed rate of EASG formation is only 1.1-fold higher than the non-enzymatic rate [26]. However, when human
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GPR agonistic activity was evaluated for the human
2022-04-18
GPR119 agonistic activity was evaluated for the human GPR119 receptor in a cell-based cAMP assay. The results expressed the potency as EC values and the inherent activity (IA) as percentages which were compared to the test compound with oleoylethanolamide (OEA), an endogenous ligand of GPR119 (defin
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Based on these findings we set out
2022-04-18
Based on these findings, we set out to identify GPR109A agonists capable of biasing the receptor's signaling towards the functional anti-lipolytic and presumed therapeutic response, and away from the flushing side-effect pathways. Indeed, using recombinantly expressed GPR109A, two classes of compoun
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br TGR agonists current developments and
2022-04-18
TGR5 agonists: current developments and future landscape The amphipathic nature of bile acids is crucial in aiding the digestion and Teriflunomide of vitamins and fats. With the emerging roles of bile acids in the regulation of energy and glucose homeostasis through TGR5, the pharmaceutical indu
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GT cells were treated in two ways
2022-04-18
GT1-7 IL-4, murine recombinant 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 c
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A oligomers increased ubiquitination of
2022-04-18
Aβ1-42 oligomers increased ubiquitination of GLT-1 in astrocytes. Previous studies found that astrocytic GLT-1 is internalized from the cell surface by ubiquitination of lysines located in the cytoplasmic C-terminus of the transporter (Gonzalez-Gonzalez et al., 2008, Martinez-Villarreal et al., 2012
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br Acknowledgements br Introduction Aminoacyl tRNA synthetas
2022-04-18
Acknowledgements Introduction Aminoacyl-tRNA synthetases catalyze the formation of an ester bond between an amino Floxuridine mg and the 3′ end of a tRNA in a two-step reaction. First, the amino acid is activated and an enzyme-bound adenylate intermediate is formed. Then, the amino acid is tra
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Here we studied the effects
2022-04-18
Here we studied the effects of BZ flurazepam (FZ) at high doses in acute and chronic settings of tolerance and dependence in GluR-A−/− mice (Zamanillo et al., 1999). We used measurements in which the phenomenon of “learning while intoxicated” should play only a minor role in order to find out the si
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Moreover to evaluate the properties of immobilized glucosida
2022-04-18
Moreover, to evaluate the properties of immobilized β-glucosidase further, the anti-protease test was also carried out. The result showed that the residual activity of the β-glucosidase@ZIF-8 was higher than that of the nano-SiO2@β-glucosidase and free β-glucosidase. Because free β-glucosidase and t
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Meleagrin australia The manner in which various residue side
2022-04-18
The manner in which various residue side chains are oriented in the active site of HsHxKIV was a driving factor for why glucosamine analogues could not bind, as we previously proposed [16]. These compounds would have difficulty managing access into the active site based on residue P153 in addition t
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Analogous to all GPCRs the GLP R transduces signals from
2022-04-18
Analogous to all GPCRs, the GLP-1R transduces signals from the outside of the cell to the inside by allosterically converting a ligand-binding event to activation of intracellular effectors. The GLP-1R couples to several intracellular effectors and this pleiotropic coupling is physiologically releva
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Ac-DEVD-AFC In patients with type diabetes glucagon receptor
2022-04-18
In patients with type 2 diabetes glucagon receptor antagonism led lowered fasting glucose however not postprandial glucose levels [9], which may reflect that glucagon may not be of particular importance for the diabetic hyperglycemia upon a meal. Current glucagon receptor antagonists have however be
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In mammals the primary cilium is
2022-04-18
In mammals, the primary cilium is considered a hub for signal transduction. The cilium has previous been associated with transduction of several pathways including Wnt (Corbit et al., 2008, McDermott et al., 2010, Tran et al., 2014), PDGF (Clement et al., 2013, Schneider et al., 2010, Schneider et a
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Importantly the levels of the
2022-04-18
Importantly, the levels of the pro-inflammatory cytokines TNF-α and IL-1β and Nf-κB, a key transcription factor in chronic inflammatory responses that is activated by pro-inflammatory cytokines, were also reduced by the drugs, confirming our previous results that demonstrated anti-inflammatory effec
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