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In the course of an internal FAAH program many
2022-01-11
In the course of an internal FAAH, program,, , , , , , , , , , , , , many very similar compounds were profiled in vivo with particular interest paid to their ability to penetrate the BBB. The compounds profiled were heteroaryl piperazinyl and piperadinyl ureas; a class of compounds, reported on pr
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Microglia after activation can show
2022-01-11
Microglia after activation can show prominently pro-inflammatory but also anti-inflammatory characteristics [46]. Although the ageing process is not a pathological process, many of the age-associated changes resemble those observed under pathological conditions. An increase number of pro-inflammator
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Histamine functions as a key neurotransmitter in multiple ci
2022-01-11
Histamine functions as a key neurotransmitter in multiple circuits to control various behaviors. In Drosophila photoreceptor, histamine is produced de novo by histidine decarboxylase (Burg et al., 1993); meanwhile, maintaining normal histamine content also depends on the histamine recycling pathway
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Intracellular signaling pathways leading to IR injury are in
2022-01-11
Intracellular signaling pathways leading to IR injury are initiated by an increase in reactive oxygen species (ROS). This occurs principally at the time of initiation of reperfusion, which is accompanied by the re-admission of oxygen to the ischemic tissue. The resulting cascade of downstream events
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br Heme oxygenase inhibitors Historically
2022-01-11
Heme oxygenase-1 inhibitors Historically, the first class of competitive HO-1 inhibitors was represented by MPs, heme analogs in which the central iron benfotiamine receptor of heme is exchanged by another element, such as zinc, cobalt, tin, or chromium. These molecules compete with heme for bin
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miRNAs post transcriptionally regulate gene expression
2022-01-11
miRNAs post-transcriptionally regulate gene egfr pathway by cleaving mRNA or inhibiting translation of target gene transcripts. Vita analysis of HBV genome sequence suggested that miR-185-5p may not directly act on HBV mRNAs, which suggested that miR-185-5p might suppress HBV gene expression and re
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Beside its role in NF B and IL activation
2022-01-11
Beside its role in NF-κB and IL-1β activation, the NRLP3 pathway is closely involved in another essential pathophysiologic mechanism such as the cellular calcium homeostasis. Full activation of the NRLP3 inflammasome requires decreased extracellular K concentrations resulting in decreased osmotic pr
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Human GPR hGPR was originally isolated
2022-01-11
Human GPR55 (hGPR55) was originally isolated in 1999 as an orphan GPCR with high levels of expression in human striatum (Sawzdargo et al., 1999) (Genbank accession # NM_005683.3). hGPR55 was mapped to human chromosome 2q37, and in the human CNS it is predominantly localized to the caudate, putamen,
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Overall this study provides compelling evidence
2022-01-11
Overall, this study provides compelling evidence that overexpression of catalase coupled with an enriched diet of OM3 fatty acids are metabolically beneficial. This combination was shown to increase adipose tissue expression of the GPR120/FFAR4, which by interacting with the Nrf2 pathway, resulted i
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It appears that not all GPR
2022-01-11
It appears that not all GPR119 agonists require a high dose to elicit acceptable Schisandrol B control. According to preclinical data presented at the GTCbio Diabetes Summit, a 3mg/kg dose of AR-7947 was enough to induce similar blood glucose-lowering effects compared to those achieved by 30mg/kg s
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Indeed in women with different causes of epithelial layer da
2022-01-11
Indeed, in women with different causes of epithelial layer damage, HIV infection rates have been reported to be very high [2], [3]. As observed from in vivo studies, disruption of the epithelium due to pathogens [45], [46] or chemical irritants [47], has resulted in women being at a higher risk of H
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Neither GIP nor GIPR SNPs were associated with occurrence of
2022-01-10
Neither GIP nor GIPR SNPs were associated with occurrence of fractures in the OPRA cohort (Table 4). Discussion The basis for this study lies in the role of glucose-insulinotropic peptide (GIP) hormone in the regulation of insulin secretion as well as its anabolic effect on osteoblasts and inhib
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Most of the above mechanisms
2022-01-10
Most of the above mechanisms are implicated in attenuation of myocardial I/R injury. However, the role of GalR2 receptor activation in cardioprotection remains unclear because of the lack of receptor subtype selectivity of peptides G2 and G3. It has been shown that Ala5-galanin (2–11) (G4) has a hig
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br Conclusions br Introduction Bioinformatics analysis
2022-01-10
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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DZNep is a PRC inhibitor that inhibits S adenosylhomocystein
2022-01-10
DZNep is a PRC2 inhibitor that inhibits S-adenosylhomocysteine hydrolase, resulting in cellular accumulation of S-adenosylhomocysteine. S-adenosylhomocysteine is a competitive inhibitor of methyl donor for methyltransferases [38]. DZNep targets EZH2 by reduction in the level of the enzyme H3K27me3 a
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