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In summary we have developed
2022-01-12

In summary, we have developed an efficient synthetic route to the required urea-isostere containing hydroxamic acid-based inhibitor . The target molecule, , was found to retain the inhibitory potency of the corresponding carbo-analog against glyoxalase-I while possessing resistance to cleavage by γ
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EAAT glutamate uptake is driven by the co transport of
2022-01-11

EAAT glutamate uptake is driven by the co-transport of three sodium ions and one proton, as well as the counter-transport of one potassium ion (Fig. 1B). This complex stoichiometry frees up enough energy to permit Oxaprozin synthesis of glutamate into the cell against a steep concentration gradient
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br Results and discussion A
2022-01-11

Results and discussion A diverse set of compounds were synthesized to improve the PK and physicochemical properties of 2. Compounds' agonist effects on hGPR40 were assessed by calcium mobilization assay using hGPR40-HEK293 cell line which stably expressed human GPR40. Preliminary explorations fo
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br Genetic rescue of GluR A
2022-01-11

Genetic rescue of GluR-A-dependent spatial working memory Spatial working memory performance in GluR-A−/− mice can be restored by the forebrain-specific Novobiocin Sodium of GluR-A subunits labeled with green-fluorescent protein (GFP) on an otherwise GluR-A knockout background (Schmitt et al., 2
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br Acknowledgments This study was supported by a Conquer Can
2022-01-11

Acknowledgments This study was supported by a Conquer Cancer Foundation (American Society for Clinical Oncology) Drug Development Research Professorship Grant (AAA). Introduction Gastric cancer (GC) is one of difficult cancers to treat in terms of its poor prognosis and limited applicability
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The glycolytic activator phosphofructo kinase fructose bisph
2022-01-11

The glycolytic activator 6-phosphofructo-2-kinase/fructose 2,6-bisphosphatase 3 (PFKFB3) is well-known as a downstream substrate of hypoxia-inducible factor 1α (HIF-1α) signaling pathway [5,6]. Tumor hypoxia has long been associated with increased malignancy, poor prognosis and drug resistance. HIF-
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The haspin gene is also
2022-01-11

The haspin gene is also unusual because it lacks introns. This is more remarkable when one compares the mammalian genes to those of likely haspin orthologs that are present in the genomic sequences of other species. Such genes in Drosophilamelagonaster, Arabidopsisthaliana and Caenorhabditiselegans
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Although historically the two ROCK isoforms have
2022-01-11

Although historically, the two ROCK isoforms have been viewed as redundant, recent observations show that the two isoforms of ROCK might have different functions (Newell-Litwa et al., 2015). Knockdown of ROCK1 was found to result in cell rounding and a decrease in cell size while cells with knockdow
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Compounds and were tested for pharmacodynamic effects in a m
2022-01-11

Compounds , and were tested for pharmacodynamic effects in a mouse oral glucose tolerance test (oGTT) in wild-type and GPR120 deficient mice, and each compound demonstrated GPR120 mechanism-based effects. Data for compound is shown in , indicating mechanism-based reduction in glucose excursion a
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Nicotinamide Next to their indirect effect on ASBT expressio
2022-01-11

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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A oligomers increased ubiquitination of GLT in
2022-01-10

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 Conclusion br Conflict of interest br Acknowledgments Thi
2022-01-10

Conclusion Conflict of interest Acknowledgments This work was supported by an NRF grant (2016R1A2B4011196) from the Korea Research Foundation. Introduction Thymic epithelial tumors are rare, but they are the most common primary neoplasm of the thymus and of the anterosuperior mediastinu
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br Introduction Glucose is the
2022-01-10

Introduction Glucose is the major carbon source in most organisms. Cancer Prednisone australia in particular require a steady source of energy to maintain growth and proliferation, and preferentially use glycolysis for their energy supply even under aerobic conditions. Glucose uptake in mammals
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Following an endoproteolytic cleavage of C secretase
2022-01-10

Following an endoproteolytic cleavage of C99, γ-secretase trims the remaining fragment Aβ49 or Aβ48 in successive, mostly three-residue steps. Aβ49 typically gives rise to Aβ46, Aβ43, and Aβ40; whereas Aβ48 usually yields Aβ45 and Aβ42 [59]. The physical basis for this characteristic cleavage patter
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FBPase deficiency is a very rare inborn error of fructose
2022-01-10

FBPase deficiency is a very rare inborn error of fructose LY3023414 of autosomal recessive inheritance. This disorder usually occurs in the first year of life through ketotic hypoglycemia and lactic acidosis triggered by catabolic episodes such as prolonged fasting or febrile infections (Steinmann
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