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Because of the commercial availability of
2022-05-13
Because of the commercial availability of some acetamide phenol starting materials, a few acetamide final products (such as and , ) were directly synthesized via a Mitsunobu reaction with chloropyrimidine piperidinyl cyclopropyl alcohol . The 3-pyridinyl analogue was synthesized by a nucleophilic ar
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br TGR Agonists br FXR
2022-05-13
TGR5 Agonists FXR/TGR5 Dual Agonists In 2010, a FXR/TGR5 dual agonist, 51 (INT-767), was reported [57]. Using an AlphaScreen coactivator recruitment assay, the potency of 51 at FXR was 30nM. In NCI-H716 cells, 51 stimulated intracellular cAMP secretion with an EC50 of 0.63μM. Its TGR5 potency
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Next to their indirect effect on ASBT expression
2022-05-13
Next to their indirect effect on ASBT expression, microbiota are also directly involved in BA homeostasis and FXR-FGF15/19 signaling. Different species of intestinal microbiota have the ability to biotransform BAs mainly by deconjugation and subsequent de-hydroxylation, the latter resulting in more
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Level of CD and other
2022-05-13
Level of CD4 and other blood parameters in patients before and after intervention are presented in Table 2. The mean of the CD4+ level before treatment in the intervention and placebo groups was 161.5 ± 291.1 and 159.9 ± 337.4, respectively (P = 0.232), which increased after treatment in both groups
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br Materials and methods br
2022-05-13
Materials and methods Results Discussion The redox domain that spans the region between amino NNC 55-0396 positions 35 and 127 of the major human AP endonuclease, APE1, regulates the sequence-specific DNA binding of various transcription factors [[52], [85]]. The existent crystal structures
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br Conclusion br Conflict of interest statement br
2022-05-13
Conclusion Conflict of interest statement Acknowledgements This work was supported by the National Science Foundation (MCB-1817417 to S.D.) and National Institutes of Health (R01-GM72711 to A.C.D.). We thank members of the Delaney laboratory for careful reading of the manuscript and helpful
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br Materials and methods br Results
2022-05-13
Materials and methods Results Discussion Quercetin is a relatively abundant bioactive flavonoid with a wide variety of documented physiological effects, which has gained popularity as a nutritional supplement [40]. There is increasing interest in quercetin's anticancer properties (for recen
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To support maximal growth and
2022-05-13
To support maximal growth and metabolic function of major organs, glucose and Cholic acid are essential. We assessed the plasma levels of glucose and amino acids in LBW and NBW piglets at birth and at day 7 postpartum. Blood glucose levels were influenced by birthweight and age. In this study, the
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Until now various reports have demonstrated the therapeutic
2022-05-13
Until now, various reports have demonstrated the therapeutic potential of enzyme-resistant forms of GIP in experimental diabetic animal models , , . In essence, structural modifications performed at the Tyr residue in GIP generate analogues that are completely resistant to the actions of DPP-IV and
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Fatty acids are also known to
2022-05-12
Fatty acids are also known to activate G-protein coupled receptors (GPCRs). LCFAs activate the GPCRs for free fatty Nalidixic acid (FFA)1 and FFA4 (Briscoe et al., 2003; Hirasawa et al., 2005), whereas SCFAs activate FFA2 and FFA3 receptors, which are expressed in bovine neutrophils (Alarcon et al.
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We focus here on the historical discoveries that
2022-05-12
We focus here on the historical discoveries that led to the development of the concept of ferroptosis. Ferroptosis is defined as an iron-dependent form of regulated cell death, which occurs through the lethal accumulation of lipid-based reactive oxygen species (ROS) when glutathione (GSH)-dependent
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br Ethics statements br Introduction Hepatocellular carcinom
2022-05-12
Ethics statements Introduction Hepatocellular carcinoma (HCC) is the fifth most common malignant tumor and the third leading cause of cancer-related mortality worldwide, with rapidly-increasing incidence in recent years [1,2]. Mounting evidence shows that viral hepatitis, toxin exposure, non-a
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832 582 4016 receptor Depletion of PI P e g by knockout
2022-05-12
Depletion of PI(4,5)P2, e.g. by knockout of PIPKIγ, also profoundly inhibits SV endocytosis (Di Paolo et al., 2004). Conversely, loss of the PI(4,5)P2-metabolizing PI-phosphatase synaptojanin or its recruitor endophilin stalls SV recycling at the level of clathrin-coated vesicles (Bai et al., 2010,
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BMS-626529 receptor Septic shock a condition where
2022-05-12
Septic shock, a condition where endothelium-derived substances most likely play an important role, is often accompanied by cardiac dysfunction, pulmonary hypertension, systemic hypotension and impaired oxygen utilisation with systemic acidosis (Vincent, 1998). Experimental endotoxaemia shows a simil
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br Results and discussion Computer
2022-05-12
Results and discussion Computer modelling studies suggested that the endocyclic oxygens in furocoumarin derivatives, such as Cathepsin S inhibitor synthesis 3a (Fig. 1), could also coordinate metal ions in the HIV-1 IN enzyme active site and inhibit the integration of viral DNA. The coumarin moi
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