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Compound was prepared from chloroindole by acylation
2021-07-19
Compound was prepared from 6-chloroindole () () by acylation, to give , and subsequent reduction to give . The thiazole was then installed using conditions developed by Buchwald and co-workers to give . Hydrolysis of the ester yielded the thiazole Rapamycin australia derivative (). Derivatives a
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br Acknowledgments br Introduction br Endothelin receptors
2021-07-19
Acknowledgments Introduction Endothelin receptors Shortly after the discovery of ET‐1, two types of seven transmembrane G protein‐coupled receptors were cloned called endothelin receptor A (ETA) (Arai et al., 1990) and ETB (Sakurai et al., 1990). The affinity of the ETA receptor for ET-3 is
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br Introduction As a serine proteinase
2021-07-19
Introduction As a serine proteinase and a sub-family of the chymotrypsin-like proteinase, Glutamyl endopeptidase (GE), which is mainly found in Bacillus species, specifically cleaves negatively charged amino SM-164 residues (Glu/Asp) (Yokoi et al., 2001). Madsen et al. (Madsen & Qvist, 1997) rep
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br Conclusions When the authors joined the
2021-07-17
Conclusions When the authors joined the field of oxysterol analysis around the turn of the century, oxysterols and cholestenoic acids were mostly considered as uninteresting intermediates of cholesterol metabolism. Some oxysterols had been shown to have biological activity, but the most studied o
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How does an increase in E affinity
2021-07-17
How does an increase in E2 affinity for the RING domain favor higher activity and polyubiquitination by the E2? Binding of the RING domain to the E2 positions the donor Ub in the E2~Ub conjugate in a closed complex [16], [17], [18] that increases the reactivity of the thioester [60]. A higher affini
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In the SUMOylation pathway SCE as an
2021-07-17
In the SUMOylation pathway, SCE1 as an E2 enzyme has an important role in mediating the conjugation of SUMO to target proteins. The accumulated SUMO conjugates in plants are associated with abiotic stress responses (Castro et al, 2012). We performed a drought stress analysis on WT plants, induced by
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A second advance came with the discovery that conformational
2021-07-17
A second advance came with the discovery that conformationally-flexible benzamide analogs having an N-phenylpiperazine moiety possessed good affinity and modest selectivity for D3 versus D2 receptors [3,[14], [15], [16]]. This observation spawned a significant effort by medicinal chemists to develop
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br Materials and methods br Results br Discussion ParI
2021-07-17
Materials and methods Results Discussion ParI, the first C5-DNA-MTase from a psychrophilic bacterium to be characterized, displays DNA methylation activity in vivo and in vitro. Its biophysical characteristics are consistent with large regions of disorder including thermal unfolding transit
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br Materials and Methods br
2021-07-17
Materials and Methods Results Discussion HSCs have been identified as major collagen-producing Streptomycin sulfate in the injured liver (1), and activation of HSCs has become the central link for liver fibrosis (2). The factors that regulate the biological behavior of HSCs include soluble
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br Conflict of interest br Acknowledgements
2021-07-17
Conflict of interest Acknowledgements This work was supported by the Biotechnology Research Center, China Three Gorges University, Yichang, China (No. 2016KBC05), the National Natural Science Foundation of China (No. 31370600 and 31300508), the Zhejiang Science and Technology Major Program on
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Six substrate recognition sites SRS SRS
2021-07-17
Six substrate recognition sites (SRS1-SRS6) have been identified at positions 102-123, 204-209, 238-244, 301-319, 374-382 and 483-492 (Table 2, underlined residues) based on Gotoh's proposal [30]. CYP3A163 displays the similar characteristic long sequences between helices F and G presenting two addi
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In contrast to PEGylated proteins which tend to
2021-07-17
In contrast to PEGylated proteins which tend to have reduced gc1 in the body relative to their native counterparts, proteins conjugated to albumin tend to accumulate in certain locales in vivo. This means that albumin-based drug carrier systems have particular applications in the field of chemother
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To extend these toxicity minimization
2021-07-17
To extend these toxicity minimization strategies to 3D tissues, a more complicated mass transfer model is necessary to account diffusion in the interstitial space, as well as transport across cell membranes. Until recently, tissue mass transport in cryobiology was modeled using classic spatially dep
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Nowadays it is possible to detect
2021-07-17
Nowadays it is possible to detect the AChE inhibitors by several methods such as gas chromatography-mass spectrometry [11], ion mobility spectrometry [12] and lab-on-chip devices [13,14]. However, almost all instrumental detection techniques that are able to conclusively determine the presence of th
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Since ET was discovered first and showed
2021-07-16
Since ET-1 was discovered first and showed a wide variety of actions not only on the cardiovascular system but also on various other tissues, much information has accumulated on ET-1 compared with the two other peptides. The method for measurement of ET-1 levels in plasma or various tissues by means
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