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The nitrophenols b d were prepared
2020-11-12
The nitrophenols 34b–d were prepared as described in Scheme 3b. Nitration of phenols 39b–d with 1equiv of sodium nitrate in the presence of hydrochloric BIO-acetoxime gave an inseparable mixture of 34b–d and 40b–d (1:1). This synthetic problem was successfully avoided as described below. Nitration
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We should also note that oxygen pressure
2020-11-12
We should also note that oxygen pressure of Krebs solution bubbled with 95% O2+5% CO2 as we used in our study is reported to around 400 mmHg in several studies [48], [49], which is higher than normal arterial O2 pressure (80–100 mmHg). Although superoxide generation at elevated O2 tensions are noted
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It is noteworthy that little is known as
2020-11-12
It is noteworthy that little is known as to the role of autophagy in regulation of eNOS phosphorylation and eNOS uncoupling. eNOS monomers, but not eNOS dimers could be degraded by ubiquitination [39], harbingering the existence of protein degradation pathways in modulation of eNOS turnover and acti
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As with all meta analysis this study certainly
2020-11-12
As with all meta-analysis, this study certainly has some limitations. First, our results were derived from unadjusted analyses due to lack of raw data, and lack of further adjusted analyses for age, gender and co-morbidity conditions may impact the reliability of our findings [63]. Second, obvious h
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Nrf and HO are key factors in the
2020-11-12
Nrf2 and HO-1 are key factors in the regulation of oxidative stress in the body. Research has shown that KLF2 can activate Nrf2 and HO-1 [14]. To investigate the mechanisms by which KLF2 regulates eNOS uncoupling and oxidative stress, Nrf2 was inhibited or HO-1 was knocked down in KLF2 overexpressin
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Our study revealed elevated basal Akt phosphorylation in die
2020-11-12
Our study revealed elevated basal Akt phosphorylation in diet-induced obesity, the effect of which was reversed by ETAKO. Activation of Akt promotes cardiac hypertrophy via a number of cellular mechanisms including activation of its downstream targets such as mTOR and GSK3β [45, 46]. Short-term acti
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Materials and methods br Results Assay of botulinum
2020-11-12
Materials and methods Results Assay of botulinum toxin activity is critical for the risk-assessment, diagnosis, and treatment of botulism cases. The frequently encountered active forms of the toxin are; L chain (inside intoxicated neuronal cells), BoNT (in the blood stream of a botulism patient,
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To further confirm the roles of the CYP enzymes
2020-11-12
To further confirm the roles of the CYP450 enzymes involved in the metabolism of Dip in rat liver microsomes, we utilized not only chemical inhibitors but also a correlation analysis and a panel of recombinant rat CYP450 enzymes to evaluate the contribution of CYP450 enzymes. The results of the corr
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With respect to bone metabolism and
2020-11-12
With respect to ‘bone metabolism and ossification’-related genes, treatment of SaOS-2 osteoblast-like Belinostat with MS-10 up-regulated IGFBP-4, TG2, and SOST. Up-regulation of IGFBP-4 in SaOS-2 cells inhibits DNA and protein synthesis induced by IGF-1 (Kudo et al., 1995, Kudo et al., 1996). In ad
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E is a classical initiator protein and as
2020-11-12
E1 is a classical initiator protein and, as such, plays several roles in the initiation and catalysis of viral DNA synthesis. E1 must first recognize a specific segment of the viral Q-VD(OMe)-OPh known as the “origin of DNA replication”, or “ori” for short. For most PV types examined to date, the m
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br Discussion Although DNA has a
2020-11-11
Discussion Although DNA has a limited chemical stability it has long been known that DNA in blood stains may remain relative stable for weeks, months, or even years at ambient temperature,1, 2, 3, 4, 5, 6 and samples (e.g., reference samples) that have been transferred to a matrix, e.g., FTA® pap
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Since the initial identification of DNA ligase inhibitors
2020-11-11
Since the initial identification of DNA ligase inhibitors by a structure-based approach [[18], [26]], there have been several reports describing LigI inhibitors using computer modelling and derivatives of the original DNA ligase inhibitors [[49], [50], [51]]. While these studies have shown that the
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We demonstrated that cells expressing less DHODH were less s
2020-11-11
We demonstrated that PPADS tetrasodium salt expressing less DHODH were less sensitive to DHODH inhibitors regardless of their oncogenic status. Based on the proliferation speed of cells, Kant et al. (1989), showed that slow-growing squamous cell carcinoma was more sensitive to BQR than fast-growing
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br Acknowledgements br Membrane bound proton translocating
2020-11-11
Acknowledgements Membrane-bound proton-translocating inorganic pyrophosphatases (H-PPase; EC 3.6.1.1) belong to a recently identified category of proton pumps, distinct from F-, P-, and V-ATPases, which utilize pyrophosphate hydrolysis as the driving force for H movement across biological membr
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We have previously reported DAPK inhibitors discovered throu
2020-11-11
We have previously reported DAPK inhibitors discovered through our structure-based virtual screening (SBVS) research program. In this paper, we describe the general protocol of our in silico approach, and the strategy used to develop hit compounds. In addition, the studies conducted on the structure
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