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br Regulation of Glu transporters The pivotal role of
2021-09-08

Regulation of Glu transporters The pivotal role of Glu transporters in the fine tuning and turnover of this excitatory amino ion channels calls for a detailed characterization of its regulation. Several general mechanisms that modify Glu uptake activity have been described. These include transcr
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Further explorations at the ortho and
2021-09-08

Further explorations at the ortho- and meta-positions of the phenyl in the tail proceeded on the basis of the preliminary results. First, we investigated the fluorine group at the meta- (13p) and ortho-positions (13q) of the phenyl group, with both compounds being slightly less potent than 13o. Surp
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A number of anti diabetic drugs are available that inhibit
2021-09-08

A number of anti-diabetic drugs are available that inhibit α-glucosidase activity, including acarbose, voglibose and miglitol [6,7]. These inhibitors, however, also exhibit undesirable side effects, such as adverse gastrointestinal symptoms and liver toxicity [8,9]. For diabetics, it would therefore
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Ketamine has recently been found to exert rapid and
2021-09-08

Ketamine has recently been found to exert rapid and sustained antidepressant effect. Single dose ketamine can have an efficacy of up to 1 week [20]. Furthermore, ketamine is an effective drug against refractory depression [21,22]. The antidepressant mechanism of ketamine is still unclear. Whether CO
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br Introduction Glucagon is a peptide hormone that acts
2021-09-08

Introduction Glucagon is a peptide hormone that acts to increase blood glucose levels. The secretion of glucagon from the alpha ML-291 of the islets of Langerhans in the pancreas is increased during fasting and prevents hypoglycemia. Glucagon increases glycogenolysis and gluconeogenesis and there
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Due to the versatility of the ghrelin system and
2021-09-08

Due to the versatility of the ghrelin system and its multiple functions, dysregulation in some of the components of the ghrelin system, such as ghrelin, GOAT, and GHSR, might lead to pathogenesis of many endocrine-related diseases, including obesity, short stature, cancer, inflammatory, and cardiova
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The focused set of additional pyrazole analogs allowed
2021-09-08

The focused set of additional pyrazole analogs allowed the identification of three additional moderately potent γ-secretase modulators, , and which were subsequently screened in a kinetic solubility assay. Unfortunately, neither the architectural changes in analog nor the integration of trifluoro
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PK profiles of were evaluated and found to be
2021-09-08

PK profiles of were evaluated and found to be improved compared to compound presumably due to interruption of β-oxidation. Low clearance and high plasma exposure were considered to be suitable profiles as an oral agent (). We first examined in vitro insulinotropic effects of compound from MIN6 c
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We conclude that a combination of GD specific CAR
2021-09-07

We conclude that a combination of GD2-specific CAR T cell therapy with pharmacological EZH2 inhibition deserves investigation as a new therapeutic strategy in EwS and potentially other cancers with heterogeneous GD2 expression, including osteosarcoma, various soft tissue sarcomas, melanoma, lung can
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br Acknowledgements This work was financially supported by t
2021-09-07

Acknowledgements This work was financially supported by the National Natural Science Foundation of China (Grant No. 81803033) and the “Double First-Class” University project (CPU2018GF02). Introduction Atrial fibrillation (AF) is the most common progressive cardiac rhythm disorder. Studies ha
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The following are the supplementary data related to
2021-09-07

The following are the supplementary data related to this article. Introduction Target therapies have achieved significant gains in the fight against cancer, however, they are still a long way from providing generally curative treatments for the majority of cancers. Targeted agents can be used wi
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In summary we have designed
2021-09-07

In summary, we have designed and explored synthetic routes towards novel acylsulfamoyl benzoxaborole-based HCV NS3 protease inhibitors. Interestingly, the resulting, unoptimized P1–P3 and P2–P4 macrocyclic inhibitors were equipotent in an enzyme assay and somewhat less potent in replicon assays, com
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Our results show furthermore that higher concentrations of b
2021-09-07

Our results show furthermore, that higher concentrations of butyric Quercetin dihydrate mg additionally affect GSTP1 mRNA stability leading to a strongly reduced half-life. Concentration-dependent effects of butyric acid on RNA stability and cell signaling pathways involved in the regulation of GST
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The urinary levels of OHP among the exposed workers were
2021-09-07

The urinary levels of 1-OHP among the exposed workers were higher than those reported for a Brazilian group of charcoal workers (0.07 μmol mol creatinine) exposed to wood smoke (Kato et al., 2004), and for nonsmoking bus drivers (0.19 μmol mol creatinine) and nonsmoking mail carriers (0.11 μmol mol
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br Introduction Depressive disorder is a
2021-09-07

Introduction Depressive disorder is a syndrome characterized by a group of heterogeneous symptoms that affect more than 350 million people worldwide, 4% of world population (WHO, 2012). The WHO estimates depression will be the leading global cause of disability in 2020, with tremendous economic c
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