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Traditional methods for HATs activity assays
2022-03-02
Traditional methods for HATs activity assays mainly depend on radioisotope labelling of histone substrates, which is limited by the complex procedures, hazards and wastes of radioactive materials. Hence, various alternative approaches such as electrochemical analysis, fluorescence and colorimetric a
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It is an exciting time for translational histamine research
2022-03-02
It is an exciting time for translational histamine research, since preclinical studies show potential value for histamine receptor ligands. As reviewed above, there are several concerns for future studies of histamine and its role in the CNS. 1) Because of the availability of HDC-Cre mice (Williams
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The H autoreceptors distributed mainly in the
2022-03-02
The H3 autoreceptors distributed mainly in the CNS act as a negative feedback on histamine synthesis and release from histaminergic neurons. Histamine is involved in many physiological functions such as sleep-wake regulation, circadian and feeding rhythm, thermal regulation, locomotion, learning, co
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Finally worth of mention are few
2022-03-02
Finally, worth of mention are few papers that report on the discovery of HO-2 selective inhibitors. In 2013, starting from the screening of a PRX-08066 library, the above-mentioned Canadian research group identified Clemizole (Table 6) as a new hit compound for the development of the first series o
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Finally we find that in
2022-03-01
Finally, we find that in the absence of Aurora B, Sgo1 is delocalized from centromeres and found along chromosome arms, as reported after depletion of Bub1 (Kitajima et al., 2005, Riedel et al., 2006). The increased arm cohesion observed in the absence of Aurora B activity is dependent on the prese
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Compound was synthesized in a racemic fashion with
2022-03-01
Compound was synthesized in a racemic fashion with this study and plans for an enantioselective synthesis could be developed based on the activity of racemic . Synthesis of compound followed a slightly different synthetic route due to the ineffectuality of the S2 reaction on the secondary position (
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While NR upregulation in the spinal cord is known
2022-03-01
While NR1 upregulation in the spinal cord is known to contribute to pathological pain [7], [22] and furthermore, NR1 expression in the spinal cord has been shown to be reduced by continuous administration of the GlyT1-inhibitor ALX5407 [23], little is known about possible expressional changes of NR1
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br Conclusion br Introduction The intracellularly generated
2022-03-01
Conclusion Introduction The intracellularly generated metabolite methylglyoxal (MG, 2-oxopropanal) acts as a potent electrophile causing irreparable cellular damage if allowed to build to cytotoxic concentrations [1], [2], [3], [4], [5], [6]. The glyoxalase (Glx) system is an enzyme couple cri
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TXA has been shown to be a competitive
2022-03-01
TXA has been shown to be a competitive antagonist on the GABAA receptor and potentially also the glycine [7], [12], [15] receptor. Furtmuller et al. showed that TXA right-shifted the GABA CRC by one order of magnitude [7], while in our study TXA similarly right-shifted the GABA EC50 value from 0.33
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br Acknowledgement This work was supported in part by
2022-02-28
Acknowledgement This work was supported in part by grants from the Ministerio de Economía y Competitividad from Spain (BFU2011-23034). Introduction The glutamate hypothesis of schizophrenia emerged from observations in the 1960s that phencyclidine and similar psychotomimetic agents produce sc
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Caffeine decreased EAAT and EAAT
2022-02-28
Caffeine decreased EAAT1 and EAAT2 AS601245 levels in P2 fraction, as well as [3H]d-aspartate uptake; however, as soon as caffeine is removed from incubation, [3H]-d-Aspartate uptake is recovered to control levels, eliminating the possibility of caffeine as a cell death inducer. In resume, our dat
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To synthesize the azaindole based compound Suzuki coupling o
2022-02-28
To synthesize the 7-azaindole based compound , Suzuki coupling of 6-chloro-7-azaindole with 4-CFO-phenylboronic pdtc sale was carried out in the presence of Pd(dppf)Cl·CHCl to supply biaryl in quantitative yield (). Iodination at the C-3 position resulted 3-iodo-7-azaindazole . Alkylation of the
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br Funding This work was supported by the National
2022-02-28
Funding This work was supported by the National Institutes of Health (RO1DK097550 to JT, RO1AG046619 to WAB and TS, and T32AG000057 to EMR, and T32DK007012 to SG) and by the Veterans Affairs Puget Sound Health Care System Research and Development. Introduction In mammals, two isoforms of grow
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The current gold standard for diagnosing BAM
2022-02-28
The current gold standard for diagnosing BAM or BAD is the measurement of BA turnover rate with radiolabelled tauroselcholic (75selenium) fura (also known as the SeHCAT retention test). SeHCAT test involves the use of a synthetic analogue of naturally occurring conjugated taurocholic acid and measu
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br Rationale The present study was motivated
2022-02-28
Rationale The present study was motivated to get further insight into the molecular recognition processes of 2-alkyl(amino)ethyl-1,1-bisphosphonates taking compounds 12–14 as reference structures. We have recently demonstrated that TcFPPS inhibitors 12 and 13 bind to the allylic site of the enzym
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