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Hedamycin isolated from Streptomyces griseoruber belongs to
2020-03-16
Hedamycin, isolated from Streptomyces griseoruber, belongs to the highly cytotoxic pluramycin class of Micafungin (Figure 3(c)). It consists of a planar anthrapyrantrione chromophore attached to two amino sugar rings at one end and a bisepoxide-containing side-chain at the other end (Figure 3(c)).
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Given the potency enhancing effect of the butyl group this
2020-03-16
Given the potency enhancing effect of the 4--butyl group, this substitution was incorporated into the Eastern portion of the molecule for further SAR investigations (). Removal of the phenol group (SR19822) or moving it from the -position to the -position (SR19552) or led to significant loss of acti
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A comparative analysis of the cleavage activity
2020-03-16
A comparative analysis of the cleavage activity of different forms of the BoNT/A endopeptidase in reduced conditions with SNAPtide and full-length SNAP-25 substrate is summarized in Fig. 5, Fig. 6. The BoNT/A LC was found to be the most active against SNAPtide, a small peptide segment of the SNAP-25
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br Funding This work was supported by the
2020-03-16
Funding This work was supported by the grants from MSD, Terumo Life Science Foundation, Takeda Science Foundation, and Japan Diabetes Foundation. Disclosures Acknowledgments The authors thank C. Morimoto (Juntendo University, Tokyo, Japan) and K. Takeda (Immunology Frontier Research Center
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Inhibition of DHODH is reflected by an antiproliferative eff
2020-03-16
Inhibition of DHODH is reflected by an antiproliferative effect on peripheral blood mononuclear Ginkgolic Acid C15:1 sale (PBMCs), which can be measured by the inhibitory effect on their phytohemagglutinin (PHA) stimulated growth. The test was performed as described in the reference. Data for few s
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Our present data show that neuroleptics can affect
2020-03-16
Our present data show that neuroleptics can affect CYP3A via a direct interaction with the enzyme and a significant indirect mechanism (enzyme regulation) produced in vivo. The obtained results revealed interactions of the neuroleptics (added in vitro to control liver microsomes, Model I) with rat C
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Within the cluster of North
2020-03-16
Within the cluster of North African populations the Sousse population sample is somewhat different from the other six populations. One has to analyze more in depth the reasons of this isolation that has been shown by other genetic studies (Fadhlaoui-Zid et al., 2015). It seems that the particular ge
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Our previous studies have shown that in
2020-03-16
Our previous studies have shown that in a preimplantation mouse embryo the proportion of inner to outer cells (i.e. precursors of ICM and TE, respectively) is regulated by a different frequency of differentiative cell divisions at the 8- and 16-cell stages. Low number of inner blastomeres generated
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Because most fusion detection methods
2020-03-16
Because most fusion detection methods were developed to analyze paired-end reads (and especially Illumina data), they are not suitable for identifying fusion junction-spanning reads in single-end Ion Torrent libraries. Therefore, we developed the FusionDetect algorithm (implemented in the ChildDecod
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br Conclusion Our study demonstrates
2020-03-16
Conclusion Our study demonstrates that the effects of Epac activation are strongly conditioned by the steady-state Ca levels at which the myocyte is functioning. As intracellular Ca increases, the activity of CaMKII enhances and the phosphorylation of its SR substrates acquires different relevanc
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The role of Epac in the regulation of intracellular
2020-03-16
The role of Epac in the regulation of intracellular Ca homeostasis and contractility is still matter of debate. In rat adult cardiomyocytes, acute Epac stimulation decreased the amplitude of Ca transients [6], [9], [10] with either no changes [6] or increments [9] in cell shortening, suggesting an e
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The majority of serpins inhibit serine proteases but
2020-03-16
The majority of serpins inhibit serine proteases, but serpins that inhibit caspases or papain-like cysteine proteases have also been identified [4], [5]. Inhibitory serpins are ‘suicide’ or ‘single use’ inhibitors that use a unique conformational change to inhibit proteases. This conformational tran
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br Materials and methods br Results br Discussion GOS
2020-03-13
Materials and methods Results Discussion GOS potently inhibited SRD5A1 in COS-1 cells (Fig. 4A) and rat Leydig cells (Fig. 4B), possibly attenuating testosterone activation into DHT. It has been reported that gossypol inhibited human SRD5A1 with IC50 of 7 × 10−6 M [28]. Interestingly, gossy
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The two isoforms LDH A and LDH B
2020-03-13
The two isoforms LDH-A and LDH-B catalyze the same reaction, conversion of pyruvate to lactate at the end of glycolysis. LDH-A is expressed in the liver. Humans with a hereditary deficiency of the A or B LDH isoforms are free of symptoms, except for muscle rigidity and myoglobinuria following strenu
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Large yellow croaker Larimichthys crocea are widely cultured
2020-03-13
Large yellow croaker (Larimichthys crocea) are widely cultured in China but have inferior meat texture compared with wild fish. This result results from excess lipid deposition in the muscle, which reduces mechanical strength (Thakur et al., 2003). The liver is the central of lipid metabolism and st
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