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br Author Contributions Statement br Conflicts of interest b
2020-03-09

Author Contributions Statement Conflicts of interest Acknowledgments We thank T. Ishii, H. Inaba, and S. Nakamura (Department of Cell Biology, TMDU) for kindly gifting BACCS and technical assistance; S. Kaneko, Y. Ishida, and R. Usumi (Department of Orthodontic Science, TMDU) for experiment
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The compounds were ranked based
2020-03-09

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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Each of the CYP enzymes alluded to
2020-03-09

Each of the CYP450 enzymes alluded to above are highly selective catalysts, in that, the three aryl coupling reactions en route the biosynthesis of 1 are catalyzed by three different CYP450 enzymes in a sequential manner (Fig. 1). In sharp INCB3344 is the recently described marine bacterial CYP450
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Pyrazolopyrimidines are bioisostere of purine exhibit promis
2020-03-09

Pyrazolopyrimidines are bioisostere of purine exhibit promising antitumor activity by competitively binding to the ATP active site of different kinase JNK-IN-7 [16,17]. Several compounds of this family were found to induce apoptosis and/or reduce cell proliferation in various solid tumour and leuka
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AMD is equally active against a broad range
2020-03-09

AMD3100 is equally active against a broad range of HIV-1 and HIV-2 strains, but not against simian immunodeficiency virus (SIV) strains in human PBMC (De Clercq et al., 1994). At this moment it is not clear what coreceptor SIV is using in human PBMC, but it does not seem to be CXCR-4 (Feng et al., 1
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br Acknowledgments This work was supported
2020-03-09

Acknowledgments This work was supported by Natural Science Foundation of China (No: 81501485). We are particularly grateful to Dr. Dan Yang and Dr. Yi Zhang for their assistance and facilities in helping this experiment and manuscript. Oral squamous cell carcinoma (OSCC), the most common malig
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Acidic substituents showed moderate biochemical activity but
2020-03-09

Acidic substituents () showed moderate biochemical activity, but these compounds showed reduced cellular potency. Additional compounds bearing a carboxylic ESI-09 were also prepared and tested (data not shown). All of acidic compounds showed low cellular potency regardless of their biochemical activ
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The identification of a functional leucine rich NES
2020-03-09

The identification of a functional leucine-rich NES mediating 8E7 nuclear export led us to analyze the interaction between 8E7 and CRM1 nuclear export receptor. HeLa cell lysates containing EGFP-8E7, EGFP–8cE7, EGFP-16E7–NES (as a positive control), or EGFP (as a negative control) were incubated wit
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Previously we have shown that complexes of protein PKs
2020-03-09

Previously, we have shown that complexes of protein PKs with inhibitors that comprised sulfur or selenium atoms in aromatic structures were phosphorescent at room temperature, while the long-lifetime signal emitted by the free inhibitor was negligible.34, 35, 36 This phenomenon was caused by stabili
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Another interesting finding from the
2020-03-09

Another interesting finding from the present study is that silencing of ERRγ suppressed the expression of HSD17B1 in extravillous trophoblasts. HSD17B1 is a key enzyme in regulating estrogen activity and has been shown to promote the proliferation and migration of estrogen-dependent breast cancer pd
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br Results and discussion br Conclusions In conclusion we ha
2020-03-09

Results and discussion Conclusions In conclusion, we have developed rational strategies that allowed us to successfully identify a series of novel analogs structurally related to to modulate the activity of estrogen-related receptors (ERRγ and ERRβ), which are constitutively active. All of the
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To our knowledge this is the first
2020-03-09

To our knowledge, this is the first report of an oncocytoma expressing alpha-enolase or causing autoimmune retinopathy and optic neuropathy. Although generally considered benign, oncocytomas have rarely been associated with paraneoplastic syndromes, including tumor-induced hypertension, erythrocytos
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HOIP s ability to build linear Ub
2020-03-07

HOIP\'s ability to build linear Ub chains arises from a unique domain that follows directly after the RING2 domain, the linear ubiquitin chain-determining domain (LDD) (Fig. 1). Structures have revealed that the LDD is structurally integrated into RING2, creating a single RING2–LDD unit (Fig. 2D) [4
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Conventional configurations for alkanolamine and acid gas
2020-03-07

Conventional configurations for alkanolamine and carnosic acid mg gas are not suitable to represent the chemical reaction between acid gas and alkanolamines. Nevertheless, Dowell et al. [17] have successfully represented the phase behaviour of CO2-water-MEA systems by using SAFT-VR [18] without any
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Cot MAP K is the sole MAP
2020-03-07

Cot (MAP3K8) is the sole MAP3K that activates the MEK1/2-Erk1/2 following the activation of the TLR/IL-1 receptor superfamily as well as some receptors of the TNF receptor family [8], [9], [10] and mediates the production of chemokines and cytokines in different cell systems [reviewed in [11]]. Thus
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