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Initial studies generally focused on the co administration o
2021-12-06
Initial studies generally focused on the co-administration of glutamate with transport inhibitors and clearly revealed the ability of the blockers to exacerbate excitotoxic injury in both in vitro and in vivo models (McBean & Roberts, 1985, Robinson et al., 1993a). In addition to demonstrating the c
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In this study for the first
2021-12-06
In this study, for the first time: 1) the electrochemical glutamate oxidase-based biosensor was optimized for the determination of low micromolar glutamate concentrations; 2) the algorithm of the analysis of exocytotic and transporter–mediated glutamate release was developed; 3) the comparative anal
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About epilepsy no specific seizure type has been identified
2021-12-06
About epilepsy, no specific seizure type has been identified because GLUT1-DS is associated with a wide range of epilepsies: patients develop seizures in infancy and early childhood, which are, frequently, do not respond to anticonvulsant medication. In infants, seizures are described as brief, subt
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Here we studied GLUT targeted nanomedicines as a new strateg
2021-12-06
Here, we studied GLUT1-targeted nanomedicines as a new strategy directed to overcome vascular barrier, enhancing delivery and efficacy in solid tumors. These nanomedicines were prepared by controlled installation of glucose on polymeric micelles incorporating the antitumor agent cisplatin, which is
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The focused set of additional
2021-12-06
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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CHR2797 receptor Nicastrin is heavily glycosylated contribut
2021-12-06
Nicastrin is heavily glycosylated, contributing 40–70KDa to the molecular weight of human γ-secretase. Among the 16 predicted N-linked glycosylation sites in the ECD, 11 have been unambiguously identified. The glycans appear to mostly stabilize the local structure, thus contributing to the folding a
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levosimendan Despite their undisputed importance however FPR
2021-12-04
Despite their undisputed importance, however, FPR receptors are not in the limelight of GPCR-related research (for review [12] and references therein). We, therefore, draw attention to this GPCR receptor family, in order to re-initiate FPR-related research, particularly in the light of biased agonis
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The objective of this study is to design and synthesize
2021-12-04
The objective of this study is to design and synthesize drug-like molecules with agonistic activity on both receptors; PPARγ and FFAR1. These agents would act as insulin sensitizers and insulin secretagogues through their action on PPARγ and FFAR1, respectively. The design of drugs with dual mode of
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To evaluate the role of increased FPPS expression in
2021-12-04
To evaluate the role of increased FPPS expression in paclitaxel-treated cells, we investigated the effects of FPPS on GSK2334470 progression. DNA content analysis showed that the number of cells accumulating in the G/M phase increased in a dose-dependent manner in paclitaxel-treated cells (A and B),
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br Acknowledgement The authors would like to
2021-12-04
Acknowledgement The authors would like to thank the University of Johannesburg and the National Research Foundation for the financial support. Mr. D Harris and Dr. R Meyer from Shimadzu South Africa are thanked for their technical support. Prof Ian Dubery is thanked for access to the LC-MS instru
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br Conclusion br Introduction Gastric adenocarcinoma
2021-12-04
Conclusion Introduction Gastric adenocarcinoma (GA) is the fifth most commonly diagnosed malignancy and the third most common cause of death due to cancer worldwide. It is a highly aggressive cancer and 5-year survival rate (5YSR) is usually toward anabolic pathways to synthesize their requir
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Recent work by Que et al
2021-12-04
Recent work by Que et al with mouse models implicates GSNOR in the cause of asthma. GSNOR is expressed in multiple cell types in the lung, including airway epithelial cells and infiltrating leukocytes. After exposure to ovalbumin, GSNOR activity increased in airway lining fluid, perhaps reflecting i
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br Introduction Adipose tissue AT in addition to its functio
2021-12-04
Introduction Adipose tissue (AT), in addition to its function as HyperScribe Poly (A) Tailing Kit storage, is an important endocrine organ and it secretes adipokines (Ahima, 2006). Adipose tissue is related to different physiological processes such as energy metabolism, insulin sensitivity, and
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br Animal models of NASH
2021-12-04
Animal models of NASH The human NAS system (see above) is largely reproducible in NAFLD mouse models [37] and, therefore, has been increasingly applied in the preclinical assessment of liver histological responses to test compounds. In general, the NAS system is well suited for this purpose, alth
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doxercalciferol In conclusion atorvastatin but not pravastat
2021-12-03
In conclusion, atorvastatin but not pravastatin impaired glucose utilization in C2C12 cells and glucose tolerance in HFD mice, which may be partly due to the inhibition of GLUT4 translocation in muscle cells. The decrease in the cholesterol level induced by atorvastatin may partly account for the in
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