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br Rho protein networks in malignancy It has
2022-03-29
Rho protein networks in malignancy It has long been recognized that Rho activity and expression are frequently elevated in tumors (Fritz et al., 1999, Orgaz et al., 2014). In this chapter we will introduce the most prominent Rho proteins, their regulators and effectors and provide an overview of
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PBI is an agonist of
2022-03-29
PBI-4050 is an agonist of GPR40 and acts as an antagonist or inverse agonist of GPR84. It cannot be excluded that other targets besides GPR40 and GPR84 could be implicated in the mechanism of action of PBI-4050 and could be explored in future studies. However, the present study, and in particular th
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Further our study provides the first evidence
2022-03-29
Further, our study provides the first evidence that zaprinast and kynurenic SB 225002 administration not only prevented the development of thermal and mechanical hypersensitivity but also enhanced morphine antinociceptive properties. Morphine is considered to be one of the most effective analgesic
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br Acknowledgments br Introduction Manipulating target prote
2022-03-29
Acknowledgments Introduction Manipulating target protein expression via either induction or suppression of gene expression is a powerful technology that has been widely used in the recent past in the field of neurobiology, both to study the pathophysiological significance of a target gene and
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The dopamine substrate currents IDA IControl were
2022-03-29
The dopamine substrate currents (IDA – IControl) were determined at different holding potentials (IV curves) in transfected HT22 cells (Fig. 5A). The plot for HT22 cells transfected with DAT exhibited the typical behavior of dopamine transporter currents (Ingram et al., 2002; Sonders et al., 1997),
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Nuclear export of GK has
2022-03-29
Nuclear export of GK has been reported to be dependent on a GK nuclear export signal (NES), mapped to residues 300–310 (Shiota et al., 1999). The assignment of a nuclear export signal common to both the liver and pancreatic GK isoform sequence suggests a possible reversible translocation of GK acros
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br Conclusions We have shown
2022-03-29
Conclusions We have shown that despite the development of severe insulin intolerance and marked alterations in whole body substrate oxidation that Gcgr−/− mice are protected against olanzapine-induced hyperglycemia. Our data provides evidence that this protective effect is likely due in large par
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The MeO CFO phen yl group was
2022-03-29
The 1-MeO-4-CFO-phen-2-yl group was then selected for the C-3 position when we investigated the aryl substituents at the C-6 position of indazole. As shown in , C-6 position seems to be more tolerant than the C-3 position, as all the aryl groups examined exhibited potent hGCGR activity. Interestingl
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In the absence of HH ligand HH signaling is
2022-03-29
In the absence of HH ligand, HH signaling is actively maintained in a repressed state by the activity of the HH receptor Patched (PTCH). PTCH is a 12-transmembrane domain protein whose intracellular localization is concentrated at the ido1 inhibitor of the primary cilium, a single antenna-like stru
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Our own search towards aryl imidazole derived
2022-03-29
Our own search towards aryl-imidazole derived GSMs led to the discovery of the benzimidazole derivative (). It is one of the most potent GSMs to date, suffering however from sub-optimal drug-like properties. More recently, we have described the design and synthesis of bicyclic triazolo-derivatives,
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br Conclusion In the present study
2022-03-29
Conclusion In the present study, we found that the majority of commercially available antibodies and antibody-based tools against galanin and its receptors that we tested do not meet validation requirements. Therefore, critical validation of these tools by the user is essential before being used
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br Materials Aspergillus oryzae GS U mg solid
2022-03-29
Materials Aspergillus oryzae βGS (8.4 U mg−1 solid) was obtained from Sigma-Aldrich Chemicals Co. (USA). o-Nitrophenyl β-d-galactopyranoside (ONPG), sodium carbonate, zinc chloride, manganese chloride, calcium chloride and potassium chloride were procured from Sisco Research Laboratories (SRL), M
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Interestingly transgenic mice that constitutively express ac
2022-03-29
Interestingly, transgenic mice that constitutively express active FXR in the intestine (iVP16FXR) are protected from chemically-induced and genetically-induced cholestasis. This protective effect is attributed to the induction of intestinal FGF15 and repression of hepatic Cyp7a1 expression, downregu
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br Acknowledgments br Introduction Non steroidal
2022-03-29
Acknowledgments Introduction Non-steroidal anti-inflammatory drugs (NSAIDs) are a common treatment for a number of disease states involving an inflammatory reaction. This group of drugs mediate their anti-inflammatory effects mainly by inhibition of cyclooxygenase (COX), an enzyme of prime imp
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The lower number of samples
2022-03-28
The lower number of samples tested for the comparison between cobas 4800 HIV-1 and RealTime HIV-1, especially at or below 50 copies/mL (Table 6), could limit our ability to discern a difference in the ability of the various assays to identify patients with virological failure. However, the 95% CI ar
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