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With the narrow SAR of the tail
2019-10-01
With the narrow SAR of the tail favouring the ortho sulfone group, we examined the remaining position open to substitution at the pyrazole 3-position, in an attempt to at least moderate the excessive human PPB (). Lipophilic groups in this position maintained huge shifts in potency in the absence or
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In a previous study we reported
2019-10-01
In a previous study we reported that the systemic administration of the α1-adrenergic receptor antagonist prazosin attenuates the deficit in IT-901 reward function associated with precipitated nicotine withdrawal (Bruijnzeel et al., 2010). One of the aims of the present experiments was to investiga
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There was a measurable worsening but not a statistically
2019-10-01
There was a measurable worsening, but not a statistically significant change in the baseline and follow-up best ear hearing scores, where the mean worsening change was 11.9 dB (95% CI: −1.11–24.86, p-value = 0.070). However, of the 16 patients, 14 (87.5%) were found to have clinically significant wo
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Our study has several limitations As this
2019-10-01
Our study has several limitations. As this study was performed at a single institution, it had a limited sample size and was not powered to detect specific differences in assay performance by organ group or waitlist status. In the two CMV seropositive subjects with potential passive antibodies, the
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The present study sought to determine if chlorodifluoroaceto
2019-10-01
The present study sought to determine if chlorodifluoroacetophenones, such as 3 and 4, were amenable to a radiolabelling methodology to generate potential 18F imaging agents with high cholinesterase affinity. A number of procedures have been reported for the synthesis of trifluoromethyl ketones, inc
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More recently it was discovered that
2019-10-01
More recently, it was discovered that BChE hydrolyzes the neuropeptide gut hormone, ghrelin [25], [26], [27], [28]. Nonetheless, because the enzyme reaction is very slow, those who first reported this finding were initially reluctant to attribute a real physiological role for that phenomenon. Our ow
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br Acknowledgements br Introduction Endothelial cells consti
2019-10-01
Acknowledgements Introduction Endothelial CRT 0066101 pathway constitute a unique source of humoral factors that may regulate the functions of other cell types via paracrine or endocrine pathways [1]. Among the many molecules originated from the endothelium, nitric oxide (NO) plays versatile
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br In some but not all human vessels a
2019-10-01
In some, but not all, human vessels, a small population of ETB (usually SYBR Safe DNA Gel Stain with atherosclerotic lesions did not show any increase. In agreement, in experimental medicine studies in both heart failure patients and volunteer controls, selective ETA antagonism (BQ123) caused the
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While oxysterols were most extensively studied
2019-10-01
While oxysterols were most extensively studied for its potent ability to mediate feedback regulation of cholesterol biosynthesis, some early investigations showed that the enzymes involved in its syntheses were highly upregulated in macrophages and dendritic cells—an indication of possible roles in
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DUBs are involved in cell
2019-10-01
DUBs are involved in 6-Chloromelatonin mass regulation and DNA damage pathways and since, in cancer and different stress conditions all the proteins which regulate cell cycle and DNA damage/repair are either up/down regulated (Singh et al., 2013, Singh et al., 2011, Kumar and de Massy, 2010, Gupta e
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br Regulation of p via the ubiquitin proteasome pathway
2019-10-01
Regulation of p53 via the ubiquitin-proteasome pathway Studies into regulation of p53 via PTM processes that involve phosphorylation, acetylation, ubiquitination, SUMOylation, neddylation, and methylation are being increasingly reported [23], [24]. Phosphorylation and acetylation of p53 stimulate
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br Activity based probes br
2019-10-01
Activity-based probes Characterization of coronavirus-encoded DUBs with activity-based probes To study the activity of specific DUBs, investigators frequently take advantage of the ~10kDa (monoUb or Ubl ABP) or ~20kDa (DiUb ABP) increase in MW on probe labeling. SDS-PAGE analysis or blotting f
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br Application of D receptor PET in psychiatric disorders br
2019-10-01
Application of D1-receptor PET in psychiatric disorders Discussion Compared to other markers of the DA system, only a limited number of studies have investigated D1-R in psychiatric disorders. In schizophrenia, which is the most studied condition with a total of 83 identified unique patients,
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Introduction Maintenance of genome integrity is
2019-10-01
Introduction Maintenance of genome integrity is essential for life, and faithful DNA replication and repair ensure this. One of the most important parameters for DNA maintenance is the regulation of optimal concentrations of the four 5′-deoxyribonucleoside-triphosphates (dNTPs) the precursors for D
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Thus DGK active sites remain ill defined and combined with
2019-10-01
Thus, DGK-active sites remain ill-defined and, combined with the lack of crystal structures for mammalian DGKs, have limited our understanding of substrate and inhibitor binding. As a result, current DGK inhibitors consist of compounds with poor specificity within the DGK superfamily (de Chaffoy de
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