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br Materials and methods br Results Aberrant A
2021-10-15
Materials and methods Results Aberrant Aβ has been suggested to be an initiating factor for glutamate excitotoxicity in AD pathology. To investigate whether Aβ1-42 alters glutamate uptake in astrocytes, neurons, and astrocyte-neuron co-cultures, we used synthetic Aβ1-42 peptide. Aβ1-42 has fas
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In prostate cancer PCa glucose metabolism plays a major
2021-10-15
In prostate cancer (PCa), glucose metabolism plays a major role in progression [14]. Androgens can activate the metabolic regulator AMP-activated kinase (AMPK), promoting oxidative phosphorylation (OXPHOS) [15]. Besides, androgens increase GLUT1 [16], which overproduction has been described in the m
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Different from stable transfection transient expression
2021-10-14
Different from stable transfection, transient expression was also found to yield γ-secretase with robust proteolytic activity []. Co-transfection of all four, but not any three, components of human γ-secretase yielded high expression levels. This observation strongly suggests the co-folding nature o
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Pertussis Toxin Cys loop GABA receptors are well
2021-10-14
Cys-loop GABA receptors are well-studied targets for insecticides and also play an important role in nematode biology. These receptors are also targets for the anthelmintic piperizine (Accardi et al., 2012). The nematode GABA receptor most studied is the UNC-49 receptor which plays a role in muscle
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br Molecular aberrations in the
2021-10-14
Molecular aberrations in the FGFR signaling pathway Non–small cell lung cancer Small cell lung cancer Integrated Psora 4 analysis revealed focal amplification of FGFR1 in 6% of SCLC cases. In another study with PD173074, Pardo et al. used two human SCLC xenograft models, H-510 and H-69, an
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Receptor interactions and binding mode of in hGPR
2021-10-14
Receptor interactions and binding mode of in hGPR40 were determined by docking studies. The compound was docked in the rebuilt co-crystal structure of hGPR40 (PDB ID: ) using MOE for loop modeling and energy minimization and Glide for molecular docking. The docking site used for the docking simulat
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We examined the expression of
2021-10-14
We examined the expression of notch-1 in the brains of mice following morphine or oxycodone tolerance. The results showed that notch-1 levels did not change following morphine or oxycodone tolerance, with or without the treatment of IRL-1620. This indicates the possibility that morphine or oxycodone
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br Conflict of interest br Author contributions br Introduct
2021-10-14
Conflict of interest Author contributions Introduction 2-Quinolones [quinoline-2(1H)-ones], while less prominent than the isomeric 4-quinolones, nevertheless enjoy significant attention as scaffolds in compounds exhibiting a variety of biological activities. These include: 4-aryl-6-chloroqu
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br Materials and methods br Results br Discussion
2021-10-14
Materials and methods Results Discussion In this report, we have analyzed the function of an orphan GPCR, and GPR84, using genetically-deficient mice. The expression of GPR84 in the T and PF-3758309 synthesis in the spleen prompted us to examine the functional responses of these cells under
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In order for cytokines to exert
2021-10-14
In order for cytokines to exert any effect on the NSC population, they must first bind to specific receptors on the cell surface. Numerous pro- and anti-inflammatory cytokines are able to exert effects on the NSC population, including IL-1β through IL-1R1 and IL-1R2, TNFα through TNFR1 and TNFR2, IL
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PF 04418948 One of the most common dietary approaches agains
2021-10-14
One of the most common dietary approaches against obesity-associated diseases is the increase in the consumption of ω3 polyunsaturated fatty acids [18], [19]. Since seminal paper by Bang and Dyeberg in which the low prevalence of coronary heart disease among the Inuit was associated with the high ma
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H together with T also forms a binding site for
2021-10-14
H109, together with T112, also forms a binding site for H+ (Chen et al., 2004; Harvey et al., 1999). H+-binding at this site also inhibits GlyR-mediated currents. Notably, the vicinity of neurons experiences changes in pH, to a mild extent in physiological conditions such as when neurons fire (Chesl
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398 Introduction l Glutamate is a major
2021-10-14
Introduction l-Glutamate is a major excitatory neurotransmitter in the mammalian central nervous system (CNS) that contributes not only to fast synaptic neurotransmission, but also to complex physiological processes like memory, learning, plasticity, and neuronal cell death [30], [81]. Glutamate is
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Tail group SAR of the imidazole
2021-10-14
Tail group SAR of the imidazole derived analogs is shown in . The previous SAR study from the discovery of AMG 837 revealed that a simple un-substituted meta-biphenyl tail group was less favorable in terms of potency. Efforts to introduce polarity to the tail group were not successful. When a methyl
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At the second step blind
2021-10-14
At the second step, blind docking simulation of 150 independent runs was performed with smaller grid box. Structures of open (1v4t.pdb), semi-closed (4dch.pdb) and two structures of closed configuration of GK (pdb codes are 1v4s and 3vev) were used for simulation (for detailed explanations on can se
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