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The compounds f and a e were found to be
2022-09-20
The compounds 8f and 9a–e were found to be potent inhibitors of both isoforms of GSK-3 as characterized by IC50 values in the low nanomolar range. In addition, all of them showed good selectivities against other kinases. Substituents in the ortho- and para-positions of structure 8 and 9 lead to pote
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Likewise and considering the aforementioned biological actio
2022-09-20
Likewise, and considering the aforementioned biological actions of ketogenic diet-derived MCFA on neuronal excitability, it could be postulated that specific receptors for fatty acids could also be involved. For example, the GPCR for medium to long chain fatty acids, FFA1/GPR40, might also contribut
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Next to their indirect effect
2022-09-20
Next to their indirect effect on ASBT expression, microbiota are also directly involved in BA homeostasis and FXR-FGF15/19 signaling. Different species of intestinal microbiota have the ability to biotransform BAs mainly by deconjugation and subsequent de-hydroxylation, the latter resulting in more
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Previously we have shown that the natural flavonoid
2022-09-19
Previously, we have shown that the natural flavonoid compounds that possess C-4 ketone group and C-5 hydroxy group, such as baicalein, luteolin, myricetin and quercetin, effectively inhibit human GLO I. Considering our interest in inhibitors of GLO I and based on the rationale mentioned above, struc
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To investigate if such an effect is observed in
2022-09-19
To investigate if such an effect is observed in native GlyT1, we introduced S605D and S605A mutations into GlyT1 and transfected these DNA constructs into N2a cells. For an internal control of calpain cleavage, we also introduced the first 100 amino-acids of the rat GlyT2N terminus upstream of the m
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Molecular dynamics studies have proved
2022-09-19
Molecular dynamics studies have proved an effective means of characterising transition state pathways between the inward- and outward-facing states, and providing the relative propensity for each state. For example, long-timescale simulations of the membrane-embedded LeuT dimer, totalling ∼21 μs, ha
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The ER EK polymorphism is located in the transactivation
2022-09-17
The ER22/23EK polymorphism is located in the transactivation domain of the GR gene. A single nucleotide polymorphisms (SNPs) has been identified in both of the two adjacent codons (22 and 23). These SNPs are fully linked and are associated with relative GC resistance[32], [44]. Although no associati
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Two pathways have emerged to explain the beneficial
2022-09-17
Two pathways have emerged to explain the beneficial metabolic effect of Roux-en-Y bypass [Fig. 3]. Firstly, the rapid delivery of nutrients to the distal small intestine and bowel might up-regulate secretion of a physiological stimulus that improves glucose homeostasis. As such, GLP-1 represents an
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TNF-alpha, recombinant rat protein receptor In summary our f
2022-09-17
In summary, our findings provide the evidence and the mechanistic understanding of the protective effects of GIP receptor agonist, D-Ala2GIP, in the MPTP-induced neurotoxicity in mice. The observed protective effects are potentially due to reduced oxidative stress and attenuation of dopamine loss in
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While the apparent complexity of gap junction
2022-09-17
While the apparent complexity of gap junction regulation presents challenges, new technologies continue to propel the field forward. Advances in microscopy are increasingly able to capture rapid dynamics at the plasma membrane (e.g., biosensors [67] and lattice light sheet microscopy [100]) and to d
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A frequent complication of SIRS and
2022-09-17
A frequent complication of SIRS and sepsis is the development of increased airway resistance and lung inflammation [2], [3]. For example, Uhlig et al. [3] demonstrated that rat lungs exposed to endotoxin present increased airway resistance due to constriction of terminal Eltrombopag receptor [3] Mor
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br Material and methods br
2022-09-17
Material and methods Acknowledgements and funding The authors thank Katharina Elsässer for technical support and Emma Esser for careful editing of the manuscript. We also thank Marcus Conrad for providing Liproxstatin-1 and advisory comments and discussion on the manuscript. This work was part
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Tariquidar methanesulfonate, hydrate Previous evidence sugge
2022-09-17
Previous evidence suggests that PRC2 is an important regulator of chromatin looping interactions in embryonic stem Tariquidar methanesulfonate, hydrate . The new study by Donaldson-Collier and colleagues provides the first evidence that similar processes may be at play in lymphoma. It is still larg
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Septic shock a condition where endothelium derived substance
2022-09-17
Septic shock, a condition where endothelium-derived substances most likely play an important role, is often accompanied by cardiac dysfunction, pulmonary hypertension, systemic hypotension and impaired oxygen utilisation with systemic acidosis (Vincent, 1998). Experimental endotoxaemia shows a simil
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There are limited studies on antibody responses
2022-09-17
There are limited studies on antibody responses against HIV-1 integrase antigen. According to previous studies, almost 5 percent of individuals infected with HIV never raise anti-integrase apelin receptor (Rikhtegaran Tehrani et al., 2015; Chang et al., 1985). If this rate is identical in individual
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