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GSK is inhibited by serine phosphorylation at a residue
2021-10-13
GSK-3 is inhibited by serine AMG-208 at a residue its N-terminus (Ser 9 in GSK-3β and Ser 21 in GSK-3α) [52], [53], [54]. This raised the possibility that the N-terminal tail may function as a pseudo-substrate by mimicking the pre-phosphorylated substrate. The interaction mode of the pseudo-substra
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A subsequent modeling study by a different group was based
2021-10-13
A subsequent modeling study by a different group was based on the bovine rhodopsin homology model using the 1L9H construct [38]. However, the site-directed mutagenesis data and docking suggested that the niacin-binding pocket is different to that described in the aforementioned report, but similar t
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With this goal in mind we proceeded to explore
2021-10-13
With this goal in mind, we proceeded to explore the C5-heteroaryl class of pyrazole-acids. Initial efforts, focused on a thiophene replacement, demonstrated little improvement. The 2-thiophene derivative (0.25μM and 0.24μM), a surrogate to the phenyl moiety, demonstrated only a modest boost in acti
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Enzyme linked immunosorbent assay ELISA is a rapid and
2021-10-13
Enzyme-linked immunosorbent assay (ELISA) is a rapid and simple test widely used for the detection of humoral immune responses following infection/vaccination. However, commercially available ILTV ELISA use the whole virus as the detecting antigen and therefore may not be sensitive for the detection
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However it is unclear whether
2021-10-13
However, it is unclear whether the parent and transition metal substitution in Keggin-type phosphomolybdic Sunitinib will reveal the best effects on α-glucosidase. Therefore, the Keggin-type H3PMo12O40 (abbreviated as PMo12) and three transition metal-substituted POMs (Na4PMo11VO40, Na6PMo11FeO40 a
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br Introduction Glucose is the major carbon source in
2021-10-13
Introduction Glucose is the major carbon source in most organisms. Cancer SRT 1720 in particular require a steady source of energy to maintain growth and proliferation, and preferentially use glycolysis for their energy supply even under aerobic conditions. Glucose uptake in mammals is mainly me
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br GLP R expression in the vascular endothelium Immunohistoc
2021-10-13
GLP-1R expression in the vascular endothelium Immunohistochemistry studies utilizing GLP-1R antibodies that have now been demonstrated to be non-specific [46], initially identified GLP-1R protein expression in both mouse mesenteric artery SMCs and heart coronary SMCs [7]. However, evidence for VS
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Deregulation of HH signaling pathway in epidermal keratinocy
2021-10-13
Deregulation of HH signaling pathway in epidermal keratinocytes is a primary event leading to the formation of BCC (see above). Overexpression of SHH in HaCaT keratinocytes grown in organotypic cultures induces a basal cell phenotype and increases invasiveness. This behavior is linked to increased E
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br Methods br Results br Discussion Previous work by the
2021-10-13
Methods Results Discussion Previous work by the Hirano group investigated the effect of GIP in murine atherosclerotic models and found infusion of GIP (1–42) by osmotic mini-pumps to decrease lesion size after 4 weeks in non-diabetic as well as in diabetic ApoE−/− mice [8], [9]. Mechanistic
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The canonical tumor suppressor p has also been implicated as
2021-10-12
The canonical tumor suppressor p53 has also been implicated as a transcriptional mediator of ferroptotic death (Jiang et al., 2015, Tarangelo et al., 2018, Wang et al., 2016, Xie et al., 2017). Specifically, p53 negatively regulates transcription of SLC7A11, the cystine-glutamate antiporter (Xc-) (J
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Macroautophagy hereafter referred to as autophagy depends on
2021-10-12
Macroautophagy (hereafter referred to as autophagy) depends on an intracellular lysosome-dependent degradation system that maintains cellular metabolism and homeostasis [11]. Genes involved in these processes are termed autophagy-related genes (ATGs), which regulate autophagosome formation and compl
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cck 1303 receptor More specific quantitative assays for DiXa
2021-10-12
More specific quantitative assays for DiXaIs are based on the inhibition of chromogenic or clotting activity of Factor Xa. During drug development, Kubitza developed an endogenous Anti-Factor Xa assay [45], which is very sensitive to Rivaroxaban drug concentration. This assay was based on Factor Xa
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While IN inhibitors are a relatively new addition to
2021-10-12
While IN inhibitors are a relatively new addition to the clinician's palette of drugs to formulate HAART regimes, resistance to both INSTIs and LEDGINs has been observed. For example, even within Australia where it is estimated that 25,313 people are currently living with HIV and the infection rate
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br Statistical analysis The mean standard deviation median r
2021-10-12
Statistical analysis The mean, standard deviation, median, range, frequency, and percentage were used for data description. The chi-square (x2) test was used for analyses the differences in categorical variables in the 2-way table. Overall survival (OS) was defined as the time interval between t
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Another interesting approach is to use partial agonists as
2021-10-12
Another interesting approach is to use partial agonists as starting point to develop specific antagonists like done in earlier decades [64], [65]. Possible indications for an attenuation of the NO/sGC signalling pathway might be specific neuronal disorders: an involvement in the aetiology of migrain
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