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Among the compounds prepared at
2022-05-11

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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br Conclusion Membrane transporters remain
2022-05-11

Conclusion Membrane transporters remain relatively understudied in human disease, especially TBI (Cesar-Razquin et al., 2015), and considerably less is known in terms of expression, function and substrates of membrane transporters in pediatric patients. However, their importance in maintaining DN
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In summary activated A AR exacerbated the reverse
2022-05-11

In summary, activated A2AR exacerbated the reverse transport function of endothelial EAATs through a direct or indirect pathway depending on PKA and glutamate levels in response to OGD in vitro, but A2AR inhibition quickly restored the normal transport function. Moreover, the key mechanisms by which
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The neurobiological mechanisms underlying DHK
2022-05-11

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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As early as glucagon was shown to
2022-05-11

As early as 1957, glucagon was shown to increase ion channels expenditure in rodents in both pair-feeding studies and through directly increasing oxygen consumption [23], [24]. This has more recently been confirmed in man, through indirect calorimetry during glucagon infusions [25], [26], [27]. Thi
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Recently several studies addressed cytological
2022-05-11

Recently, several studies addressed cytological and biochemical features of oocyte aging. It was reported that cytological changes associated with the mammalian post-ovulatory oocyte aging include chromatin disorganization, abnormal meiotic spindle location or its disruption, partial exocytosis of c
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br Conclusions br Introduction Bioinformatics analysis
2022-05-11

Conclusions Introduction Bioinformatics analysis shows that there are about 300,000 G-rich sequences in human genome if searching with the consensus sequence (G3+N1-7G3+N1-7G3+N1-7G3+) [1], and their localizations are non-random. These G-rich sequences always localize in functional regions, su
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Activation of FXR or TGR has overlapping but also
2022-05-11

Activation of FXR or TGR5 has overlapping but also differing effects on metabolic regulation and inflammation [1]. In this report, we demonstrate that in addition to preventing the progression of obesity, NAFLD, and atherosclerosis, activation of BA receptors can also promote regression of these com
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Based on the previous report that
2022-05-11

Based on the previous report that FXR regulated PEPCK indirectly [20], we speculated that FXR may regulate gluconeogenesis by regulating some key transcription factors associated with gluconeogenesis. Finally, by using HS218 as a probe, we found that FXR binds to PGC-1α promoter and directly regulat
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br Future perspectives A plethora of reports from
2022-05-11

Future perspectives A plethora of reports from in vivo and in vitro human and animal studies have demonstrated the potential role of FGFR signalling in human carcinogenesis, whether it be in an oncogenic or tumour suppressive capacity. It is still not well understood how FGFRs can act as tumour s
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Histone acetylation is regulated by two
2022-05-10

Histone acetylation is regulated by two groups of enzymes, histone acetyltransferases (HATs) and deacetylases (HDACs), with antagonizing functions (Wang et al., 2009b). Among members of HATs, p300 and CBP are homologous. Both are global transcriptional co-activators (Ogryzko et al., 1996), and play
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br Acknowledgments br Introduction Histone
2022-05-10

Acknowledgments Introduction Histone deacetylases (HDACs) related to tumor suppressor genes have become promising targets for the treatment of cancer [1,2]. Under the normal physiological conditions, Histone acetyltransferases (HATs) and histone deacetylases (HDACs) together regulate the acety
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br Experimental br Acknowledgment br Introduction
2022-05-10

Experimental Acknowledgment Introduction Hepatitis C virus (HCV) belongs to Flaviviridae, is a blood-borne pathogen which infects about 180 million individuals throughout the world; most of the cases lead to end stage liver diseases, fibrosis, cirrhosis and hepatocellular carcinoma (Choo et
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HBV is an enveloped double stranded
2022-05-10

HBV is an enveloped, double-stranded DNA virus, which is transcripted into four major transcripts [6]. Among them, the 3.5 kb pregenomic RNA (pgRNA) directs the translation of HBV polymerase, core protein and acts as template for reverse transcription. So viral transcription is a key step of virus l
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br Structural studies of the cyclase catalytic
2022-05-10

Structural studies of the cyclase catalytic domains Structural determinants for catalytic activity The structure of the active αβGCcat structure has remained elusive. However, several studies have suggested how specific structural elements are involved in αβGCcat transitioning from the open in
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