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Acidic substituents showed moderate biochemical activity but
2020-11-28
Acidic substituents () showed moderate biochemical activity, but these compounds showed reduced cellular potency. Additional compounds bearing a carboxylic ω-Agatoxin TK synthesis were also prepared and tested (data not shown). All of acidic compounds showed low cellular potency regardless of their
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Since its inception ADEPT approach
2020-11-28
Since its inception, ADEPT approach has been widely reported by many groups using a variety of enzymes and prodrugs (see reviews) [12], [14]. Both mammalian and non-mammalian enzymes have been utilised. Of the mammalian variety, human β-glucuronidase in combination with many prodrugs [17], [18] and
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Interestingly from our consensus SBVC protocol only
2020-11-27
Interestingly, from our consensus SBVC protocol only few compounds (less than 150) have been scored with a full ‘ consensus’. That means that these compounds appear in the top 5% of the database when ranked by every scoring function independently. After visual inspection, we have realized that two a
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br Results br Discussion Here we establish a key kinase
2020-11-27
Results Discussion Here we establish a key kinase cascade that acts at PCs to promote homolog pairing and synapsis. CHK-2 phosphorylates the zinc finger proteins that specify PCs, which, in turn, primes their recruitment of PLK-2 (Figure 7D). By recruiting these two kinases, PCs serve as signa
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Finally we demonstrated for the first
2020-11-27
Finally, we demonstrated for the first time that the physiological combinations of estradiol and progesterone levels of premenopausal and postmenopausal women efficiently stimulated the growth of T47D spheroids while clinically relevant concentrations of TPA and UPA suppressed the growth of T47D sph
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The previously described endogenous patterns of IGF induced
2020-11-27
The previously described endogenous patterns of IGF-1-induced kinase signaling, and resulting interaction between MAPK and PI3K, differ across neuronal sub-types. In R28 retinal neuron-like cells, IGF-1 treatment elicits prolonged activation (at least 80 min) of both PI3K and MAPK (Kong et al., 2016
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br Management of Hypertension The aim of treating
2020-11-27
Management of Hypertension The aim of treating HT is to reduce the risk of adverse cardiovascular outcomes: mainly coronary artery disease, stroke, and death. For this reason, the decision whether to initiate pharmacological treatment or not will depend not only on BP values, but also on the over
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EPAC activation in VSMCs and
2020-11-27
EPAC activation in VSMCs and ECs reverses several processes involved in the development of in-stent restenosis. Of particular relevance is the ability of EPAC1 to induce SOCS3 gene expression, as SOCS3 exerts multiple protective effects in both cell types, while immunohistochemical studies have show
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The MOF system described by Farha and coworkers
2020-11-27
The MOF system described by Farha and coworkers combines rational design of the support and good experimental results regarding activity and stability. However, a further increase in the speed of enzyme loading into the MOF and a decrease in leaching are still required. How can the design rules prop
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The GH family includes also xylanases
2020-11-27
The GH30 family includes also xylanases which are not MeGlcA-dependent. Most of them are grouped to GH30_7 subfamily that includes XynIV from Trichoderma reesei showing exo- and endo-xylanase activity [11] and XYLD from Bispora sp. MEY-1 [12] having activity towards glucuronoxylan and arabinoxylan,
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The current study demonstrates a link between
2020-11-27
The current study demonstrates a link between heme metabolism and mitochondrial Co-I, which deficits instigate abnormalities in the metabolism of heme and its downstream targets both in-vitro in patients and healthy subjects derived LCLs and in-vivo in brains of SZ-rat model. A further study of the
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br General mechanism of NHEJ NHEJ is
2020-11-27
General mechanism of NHEJ NHEJ is an amazingly versatile pathway that can select specific enzymes which bind to, process, and finally mediate the direct re-ligation of a wide range of DSBs including those that are complex, have incompatible ends, and contain Auranofin damages [7], [8], [9], [10]
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br Material and methods br
2020-11-27
Material and methods Results and discussion Conclusions Acknowledgements S. De thanks DST, New Delhi for generous grant of the SERC Fast Track Scheme No. SR/FT/CS-057/2008. R. Kundu thanks the University of Kalyani for financial assistance. We are grateful to Prof. K. Bhattacharyya of IA
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br Conclusion br Funding source br
2020-11-26
Conclusion Funding source Ethical approval Conflict of interest statement Introduction Traditionally, schizophrenia (SZ) was thought to be associated with neuronal dysfunction; however, the current hypothesis that myelin and, specifically, oligodendrocytes are also involved in the dev
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br DDR in atherosclerosis and
2020-11-26
DDR1 in atherosclerosis and vascular disease The Canadian group of Bendeck, explored the role of DDR1 in repair following arterial injury in rats [30]. DDR1 protein levels, assessed via Western blots prepared from arterial extracts taken at various times after injury, showed DDR1 protein dramatic
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