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Introduction Multiple sclerosis MS a neurological autoimmune
2021-12-21
Introduction Multiple sclerosis (MS), a neurological autoimmune disease, is driven by CD4+ aa dutp synthesis of the T helper (TH) cells [1]. There is no curative treatment for MS and the present treatments typically focus on immunomodulation for slowing the progression of the disease. These includ
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To combat the detrimental effects of neuropathological condi
2021-12-21
To combat the detrimental effects of neuropathological conditions, additional therapeutic interventions that either dampen chronic neuroinflammation or attenuate reductions in hippocampal neurogenesis are critically needed. The cannabinoid system has already been shown to rescue impaired neurogenesi
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In addition researchers studying GPR agonists
2021-12-21
In addition, researchers studying GPR119 agonists favor the developing of candidate drugs that are more potent than DPP-4 inhibitors given that the latter are moderate agents in the treatment of DM. Although it glp-1 receptor is unclear why Sanofi-Aventis chose to terminate collaboration with Metab
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Glycine regulates several brain functions and glycine
2021-12-21
Glycine regulates several brain functions and glycine transporters significantly contribute in such processes. In previous work we reported calpain sensitive regions in N-terminal domains of GlyT1a and GlyT1b (Baliova and Jursky, 2005). Here we show that distal part of glycine transporter GlyT1C-ter
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The ester moiety is a promising
2021-12-21
The ester moiety is a promising structural motif at the C-3 position for the development of drug-like molecules. However, the labile C-3 ester bond impels these derivate to be susceptible to plasmatic degradation by esterases and this is natural steroidal metabolic process [39,40]. Hence, the isoste
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The expression of GLUT receptors throughout the
2021-12-21
The expression of GLUT receptors throughout the body could be considered a potential source for off-target effects even for engineered glucose-conjugated nanomedicines, as there are at least 12 types of GLUT transporters in the body, including GLUT1 in erythrocytes and the blood-brain barrier, as we
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Piezo channels can be activated
2021-12-21
Piezo channels can be activated by many mechanical stimuli . While some of these stimulations directly mimic physiological forces experienced by W146 receptor , such as shear stress applied in a microfluidic chamber, the most commonly used modes of stimulation consist of stretching the membrane by
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Hardy et al had demonstrated the role of
2021-12-21
Hardy et al. had demonstrated the role of GPR40 in mediating the proliferative effect of the FFA oleate's in breast cancer cells, and found that such effect can be reversed by silencing of GPR40 [14]. Similarly we have observed that inhibition of GPR40 function by its antagonist GW1100 inhibited cel
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br Drug design Over the past decades the
2021-12-21
Drug design Over the past decades, the development of synthetic, direct fXa inhibitors has undergone four phase. Although these fXa inhibitors possess various scaffolds, most of them bind to the active site in a characteristic l-shaped conformation. In other word, they have a three-component syst
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br Conclusion In this research we have successfully formulat
2021-12-20
Conclusion In this research we have successfully formulated a PEGylated liposomal formulation encapsulating IRL-1620. The liposomal nanocarriers loaded with IRL-1620 were characterized for their particle size, PDI, zeta potential, and loading efficiency. We established that the treatment with IRL
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In this study we also investigated the
2021-12-20
In this study, we also investigated the role of GST po1 mg in relation to ASD. In univariable analyses, where the role of each GST gene (i.e., GSTM1, GSTT1, GSTP1) was individually assessed, we did not observe any significant associations between the GST genotypes and ASD. In contrast, a previous s
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br Cholecystokinin CCK CCK is secreted
2021-12-20
Cholecystokinin (CCK) CCK is secreted by enteroendocrine I-cells of the duodenum and jejunum in response to amino acids and lipids [14]. There are two forms of the CCK receptor, CCK1 which is expressed on pancreatic α- and β-cells while CCK2 is located on somatostatin-secreting δ-cells [8]. CCK r
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Excessive extracellular glutamate may induce
2021-12-20
Excessive extracellular glutamate may induce excitotoxic neuronal damage in disorders of the CNS (Schwartz et al., 2003). EAATs are considered to contribute to prevention of excitotoxicity by glutamate uptake. Our data revealed that expression levels of membrane EAAT proteins in astrocytes are much
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br Conclusion In summary a series of novel GPR
2021-12-20
Conclusion In summary, a series of novel GPR40 agonists bearing phenylpropiolic N1-Methylpseudo-UTP synthesis motif with favorable metabolic stability were prepared and evaluated for their activities as GPR40 agonists. Among them, compound 9 was identified as a structurally distinct GPR40 agonis
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The neurobiological mechanisms underlying DHK induced NOR le
2021-12-20
The neurobiological mechanisms underlying DHK-induced NOR learning and memory impairments remain unclear. Accumulated evidence shows that astrocyte-neuron lactate shuttle is of crucial important in synaptic plasticity and memory formation, and regulation of neuronal gene expression related to synapt
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