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Among the compounds prepared at this stage the cyclopropylme
2022-02-22
Among the compounds prepared at this stage, the cyclopropylmethylenoxy analogue attracted our most attention since it demonstrated particularly good in vitro potency at GlyT1 (16nM), no activity at the GlyT2 isoform up to the highest concentration tested (30μM), good physical properties with modera
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Due to the high structural
2022-02-22
Due to the high structural similarity between GlxI and FosA, it is possible that GlxI directed evolution experiments could produce FosA enzymatic activity in a GlxI enzyme. Although the current investigation was unable to detect FosA activity by mutation of a key metal liganding residue in the activ
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br Materials and methods br Results br
2022-02-22
Materials and methods Results Discussion The redox domain that spans the region between amino cysteine protease inhibitors positions 35 and 127 of the major human AP endonuclease, APE1, regulates the sequence-specific DNA binding of various transcription factors [[52], [85]]. The existent c
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The GlyR is pentameric with each subunit consisting of an
2022-02-22
The GlyR is pentameric, with each subunit consisting of an extracellular ligand binding domain (LBD), four transmembrane (TM) segments, and a large intracellular loop between TM3 and TM4. Binding of neurotransmitter produces conformational changes that are rapidly transmitted to the membrane-spannin
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In spite of the similarities of caffeine s effects in
2022-02-22
In spite of the similarities of caffeine's effects in L929 cells and erythrocytes, a major difference can be identified in the magnitude of inhibition (35% versus 90%). It initially seems reasonable to conclude from this finding that the reduced magnitude of caffeine inhibition in L929 cells is simp
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Because of the relationship between carbohydrate
2022-02-22
Because of the relationship between carbohydrate consumption and chronic diseases such as obesity and type II diabetes (Hu, van Dam, & Liu, 2001), there is mounting interest to evaluate the quality of Iohexol through analysis by glycemic index (GI) and Englyst assay, for example (Englyst, Kingman,
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thiotepa mg br Material and methods br Results br Discussion
2022-02-22
Material and methods Results Discussion Accumulating evidence suggests that the hippocampus is sensitive to noise-induced hearing loss and other forms of sensory deprivation, which deprives the hippocampus of sensory information required for its normal operations such as spatial navigation
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In accordance with its similarity to classical NLSs
2022-02-22
In accordance with its similarity to classical NLSs, Importin α3 was recently reported as a nuclear transport receptor for Ci (). We therefore superimposed the Gli1 NLS model with the Importin α2 structure (3EFX), which has a structure similar to Drosophila Importin α3 () (Fig. 4.4B). Gli1 NLS fitte
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br Materials and methods br Results br
2022-02-22
Materials and methods Results Discussion Our study demonstrates that human GIP(3-30)NH2 is a selective GIPR antagonist that inhibits both GIP-mediated cAMP signaling, β-arrestin recruitment, and GIPR internalization. Furthermore, we demonstrate that human GIP(3-30)NH2 binds with high affini
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The RAS RAF MEK ERK pathway also known as the
2022-02-21
The RAS/RAF/MEK/ERK pathway (also known as the MAPK/ERK pathway) is one of the most important signaling pathways in PDAC. Activation of the MAPK/ERK pathway promotes PDAC growth and apoptosis resistance in response to gemcitabine [43,44]. We previously demonstrated that inhibition of GPX4 can overco
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The release of FBPase and
2022-02-21
The release of FBPase and aldolase from subcellular structures of muscle was dependent on the presence of the crowding agent imitating the physiological conditions – PEG 8000 (Table 1). The amount of both enzymes associated with structures of muscle reference 4 was about 6–7 times higher in the pre
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G P also plays a critical role
2022-02-21
G6P also plays a critical role in regulating HK2 binding to mitochondria. Elevated levels of intracellular G6P weaken HK2 binding to mitochondria, causing the enzyme to translocate to the cytoplasm and facilitate anabolic glucose metabolism. Acidosis similarly induces HK2 translocation from mitochon
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The transcription factor Nrf is a master
2022-02-21
The transcription factor Nrf2 is a master regulator of cytoprotective responses to endogenous and exogenous stresses caused by reactive oxygen species (ROS) and electrophiles [6]. Nrf2 promoter polymorphisms are significantly associated with the development of gastric mucosal inflammation, either in
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br The value of a model of the
2022-02-21
The value of a model of the complex forensic science matrix There have been various models proposed to address the complexity inherent to forensic reconstruction [15], [16], [17]. It is possible to argue that embracing the value of holistic models is important if we are to reclaim the ‘endeavour
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br Materials and methods br Results br Discussion An HMC
2022-02-21
Materials and methods Results Discussion An HMC is a blinding type of cataract frequently observed in Asian countries due to the appallingly high incidence of high myopia in those areas [4], [5] and typically features earlier onset and more rapid progression of nuclear cataract [1], [2]. Th
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