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GSTs have been originally named ligandins because
2022-06-23
GSTs have been originally named ‘ligandins’ because of their capacity to bind large ligand molecules (of molecular weight >400 Da) (Oakley et al., 1999). At least three separate Adaptaquin have been reported for xenobiotics within the H-site; only one is for CDNB (Ralat and Colman, 2004). Usually,
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Calcium mobilization FLIPR assay CHO K
2022-06-23
Calcium mobilization (FLIPR) assay: CHO-K1 cells expressing an NFAT-β-lactamase reporter and the promiscuous Gα-subunit Gqi5 were stably transfected with either empty vector (pCDNA3.1, Invitrogen) or vector expressing HA-GPR81, GPR109A or GPR109B. Cells were seeded at 10,000cells/well in 384-well cu
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Obestatin synthetized mainly in the gastrointestinal tract p
2022-06-23
Obestatin, synthetized mainly in the gastrointestinal tract, participates in the regulation of metabolic functioning at both central and peripheral levels (food intake, pancreatic activity or/and adipocytes proliferation) (Granata et al., 2008; Li et al., 2011). It is involved in the complex gut-bra
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Among the compounds prepared at this stage the
2022-06-23
Among the compounds prepared at this stage, the cyclopropylmethylenoxy analogue attracted our most attention since it demonstrated particularly good in vitro potency at GlyT1 (16nM), no activity at the GlyT2 isoform up to the highest concentration tested (30μM), good physical properties with modera
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br Acknowledgments This research was
2022-06-23
Acknowledgments This research was supported by a grant from the Korea Health Technology R&D Project through the Korean Health Industry Development Institute (KHIDI), funded by the Ministry of Health & Welfare, Republic of Korea (grant number: HI17C0616). Dr. Jun-Mo Yang was supported by the Natio
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Glucagon regulates the transition from hepatic glucose utili
2022-06-23
Glucagon regulates the transition from hepatic glucose utilisation in the absorptive state to glucagon production in the post-absorptive state by acute stimulation of glycogenolysis and inhibition of glycolysis [1]. An important component of this response is the phosphorylation of liver PFK2/FBPase2
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The regulation of the stem cell
2022-06-23
The regulation of the stem cell compartment in CML is dynamic, in particular, during disease progression to a blast crisis and might involve a complex cross-regulation of Hh, Wnt, Notch, and hox signaling pathways (). Significant upregulation of Ptch1 and cyclin D1, upon other proteins, marks the bl
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br Contributions br Acknowledgements This research was
2022-06-22
Contributions Acknowledgements This research was supported by Natural Sciences and Engineering Research Council (NSERC) Discovery grant No. 341538 and Ontario Graduate Scholarships to HM and VS. Introduction Sexual size dimorphism describes size difference between male and female individua
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Ghrelin receptors in non mammals are reportedly more
2022-06-22
Ghrelin receptors in non-mammals are reportedly more “complicated/complex and diverse” than in mammals, having additional paralogs and splice variants (Kaiya et al., 2014). Several teleost fish GHS-Rs have been identified; however, functional characterization has been conducted in only a few (see, K
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For the two KO models CX and CX
2022-06-22
For the two KO models (CX30 and CX43), fluorescence recovery is almost always best fitted with a 2-component exponential (Fig. 6A and D). Statistical analysis of the parameters (Table 1) shows that in both cases the two time scales and the fraction of recovery associated with the fast intracellular
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In conclusion starting from the
2022-06-22
In conclusion, starting from the weakly potent GSM , exploration of various spacer groups between the triazole ring and the aromatic DiscoveryProbe™ Inhibitor Library led to the discovery of a new series of potent gamma secretase modulators, with an improved drug-like profile—compared with the orig
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br Gamma secretase trafficking GS activity for APP can be
2022-06-22
Gamma-secretase trafficking GS activity for APP can be influenced by sub-cellular trafficking, as APP cleavage differs depending on its localization. APP is synthesized in the ER and transported to the trans-Golgi network (Annaert et al., 1999, Pasternak et al., 2003, Ray et al., 1999a, Rechards
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More recently Serna Marquez and colleagues
2022-06-22
More recently, Serna-Marquez and colleagues investigated LA-induced migration and invasion of MDA-MB-231 breast cancer cells. In this study, LA was shown to induce AKT-2 phosphorylation and cell invasion and migration in MDA cells. LA-induced cell migration was inhibited by siRNA that selectively ta
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br Notch Similar to the Wnt
2022-06-22
Notch Similar to the Wnt and Hedgehog pathways as discussed earlier, Notch is an evolutionarily conserved primordial developmental pathway which affects patterning, and has an important role to play in cancer biology ranging from angiogenesis to cancer stem ampa receptors to tumor immunity [88].
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A nitric oxide donor glyceryl trinitrite and the substrate f
2022-06-22
A nitric oxide donor, glyceryl-trinitrite, and the substrate for nitric oxide, l-arginine, have been used to treat preterm labor. However, these studies are preliminary. The beneficial effect of nitric oxide donors needs to be confirmed by more controlled studies. The probable pitfall of using nitri
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