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The third challenge is to understand the
2021-08-10
The third challenge is to understand the mechanisms of drug resistance. There are several different mechanisms of ES tumor to develop drug resistance. First, cancer stem cells are capable of proliferate and generate tumor cells with new sets of mutations which may harbor different protein targets [1
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In our previous research we
2021-08-10
In our previous research, we have focused on the discovery of novel VEGFR-2 inhibitors as anti-angiogenesis agents. Numbers of biphenyl-aryl urea incorporated with salicylaldoxime including BPS-7 have been developed as potent and selective VEGFR-2 inhibitors (Fig. 3) [12], [13], [14], [15], [16], [1
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Our previous work has demonstrated that two glutamate residu
2021-08-10
Our previous work has demonstrated that two glutamate residues (Glu-305 and Glu-331 in murine and human TPP II) in the active site are important for exopeptidase activity in mTPP II [17]. At least one of these, Glu-331, seems to form a salt bridge to the N-terminal amino group of the substrate, posi
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Another example of negative regulation is the
2021-08-09
Another example of negative regulation is the inhibition of the yeast endosome-associated DUB Doa4 by Rfu1 (free ubiquitin chains 1). In a yeast genetics screen, deletion of Rfu1 was serendipitously found to alter global ubiquitin levels [69]. DUBs can regulate these levels by liberating conjugated
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Current therapeutic interventions are directed both to preve
2021-08-09
Current therapeutic interventions are directed both to prevent (primarily by proper glycemic control) and to treat the advanced stages of diabetic retinopathy, when vision has already been significantly affected. Although these therapies can be very effective in preventing, delaying or reducing visi
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In attempts to further purify His Artemis numerous matrices
2021-08-09
In attempts to further purify [His]6-Artemis, numerous matrices were assessed including anion and cation exchange, and Thymidine receptor interaction chromatography. The results from these matrices were universally poor (data not shown). Fractionation via adsorption chromatography on a hydroxyapati
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As for antiviral activity eight
2021-08-09
As for antiviral activity, eight out of 23 synthesized compounds were active against influenza B virus with EC50 values in the range of 0.19–39 μM. Four of the eight influenza B hits were active against influenza A and two were also active against RSV (4 and 6, EC50 = 0.40 and 1.8 μM, respectively).
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The compounds were ranked based on the Glide XP
2021-08-09
The compounds were ranked based on the Glide XP Score, as shown in . All 15 compounds were subject to a radiometric assay previously used in our lab to evaluate their ability to inhibit DHFR steady-state activity in recombinant TS-DHFR (A). Compound demonstrated greater than 50% inhibition of DHFR
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br Introduction Biocatalysis can be used to synthesize chira
2021-08-09
Introduction Biocatalysis can be used to synthesize chiral building blocks, such as monomers for polymer materials, and precursors for pharmaceuticals [[1], [2], [3], [4]]. Enzymes are very suitable for catalyzing reactions with high enantioselectivity to obtain chiral products. For instance, alc
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br Acknowledgements br This work was supported by grants fro
2021-08-09
Acknowledgements This work was supported by grants from the National Natural Science Foundation of China (Grant No.: 30260088) and the prophase research for National “973” Project of China (Grant No.: 2007CB116203). The DNA sequences of Hbvp1 and the Hbvp1 promoter were deposited in GenBank, an
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Studies of LRRK tagged with green fluorescent protein reveal
2021-08-09
Studies of LRRK2 tagged with green fluorescent protein revealed the presence of monomeric LRRK2 in the ampk inhibitors of living cells, while LRRK2 oligomers were found in the proximity of the plasma membrane, suggesting that both oligomerization status and compartmentalization of LRRK2 defines its
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br Materials and methods br Results br Discussion CDK and
2021-08-09
Materials and methods Results Discussion CDK and their regulatory cyclins form a family of heterodimeric kinases that are particularly important for regulation of Phos-tag Acrylamide receptor progression and transcription in tumor cells. These kinases therefore constitute biomarkers of pro
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br Materials and methods br Results br
2021-08-09
Materials and methods Results Discussion In our tissue array, we demonstrated that 14-3-3 tau mRNA and protein expression levels decreased in the preeclamptic placentas. 14-3-3 proteins are considered to be important in the functional regulation of trophoblasts and maybe associated with adv
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Here although tibolone reduced the expression
2021-08-09
Here, although tibolone reduced the expression of inflammatory genes such as IL6, IL1β, TLR4 and MIR155-3p, in the presence of PA stimulation, it increased the expression of TNF gene. It should be noted that TNF has pleiotropic effects in the CNS, therefore its increased expression does not always i
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br Sources of funding br Disclosures br Acknowledgments br I
2021-08-06
Sources of funding Disclosures Acknowledgments Introduction Insulin secretion from pancreatic β cells is a fundamental process to maintain blood glucose homeostasis. During glucose-stimulated insulin secretion, high glucose causes closure of ATP-sensitive K+ channels (KATP channels), sub
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