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Docking experiments showed that Me
2020-12-07
Docking experiments showed that Me-MeGlcA3Xyl4 and MeGlc3Xyl4 were bound to EcXyn30A and the R293A variant in the same way as MeGlcA3Xyl4, having MeGlcA or its modified forms accommodated in the -2b subsite. All ligands were coordinated by the same RG7204 and no new interactions were observed. The
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A wealth of studies support the
2020-12-07
A wealth of studies support the key role of high NO in promoting higher blood flow and thus greater O2 delivery to working tissues in healthy Tibetans and thus partly compensate hypoxia induced low arterial O2 content [7,9,27]. We observed high eNOS mRNA, protein and enzyme activity in Ladakhi women
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PKA signalling in the nucleus
2020-12-07
PKA signalling in the nucleus was thought to be due to the translocation of the catalytic subunit upon activation from the Rimonabant to the nucleus via diffusion [72]. However, a new understanding has emerged, as both the regulatory and catalytic subunits have been identified in the nucleus and fu
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TG003 The contribution of local ETA
2020-12-07
The contribution of local ETA and ETB receptors towards heat hyperalgesia induced by inoculation of XC tumor TG003 in the paw of mice has been demonstrated by Baamonde and colleagues (Baamonde et al., 2004). Furthermore, using neuropathic and inflammatory nociception models, several studies have sh
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Overall the evidence and the
2020-12-07
Overall, the evidence and the results from in vivo studies clearly indicate that cyclosporine biotransformation can be induced by dasatinib co-administration through induction of CYP3A expression. However, further studies are needed to explore the role of P-gp modulation in DDIs. Conclusion In v
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Here we discuss implications of several
2020-12-07
Here, we discuss implications of several major families of RING-type E3 ubiquitin ligases (MDM, Cullin, GRAIL, TRAF, TRIM) as targets in inflammation and immunity, and provide insights into potential small molecule interventions to mediate the cellular responses (summarized in Table 1). We briefly c
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br Introduction Addiction to opioids such as morphine is a
2020-12-07
Introduction Addiction to opioids such as morphine is a chronic disorder that affects the mesocorticolimbic dopaminergic pathway in the brain. Activation of the pathway ultimately leads to dopamine release in the nucleus accumbens (NAc) (Di Chiara et al., 1998) and stimulation of dopamine recepto
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Thymine glycol severely inhibits DNA synthesis by replicativ
2020-12-07
Thymine glycol severely inhibits DNA synthesis by replicative DNA polymerases and requires the action of specialized DNA polymerases for translesion synthesis (e.g. Ref. [26]). Eukaryotic and archaeal RNAPs were shown to pause after nucleotide insertion opposite TG [27,28]. Surprisingly, we found th
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In this context we initiated a program to develop new
2020-12-07
In this context, we initiated a program to develop new antiviral chemotypes towards a host factor implicated in bromfenac replication: the host (human) dihydrofolate reductase (DHFR) [21]. We recently identified this enzyme as the molecular target of 1-aryl-4,6-diamino-1,2-dihydrotriazines, structu
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Previous studies from our lab
2020-12-07
Previous studies from our lab looked at the effect of interfering with crossover helix interactions in TS-DHFR. One study utilized peptide mimetics of the crossover helix to inhibit wild-type TS-DHFR noncompetitively, and with an IC of 230 μM. A second study used a virtual screening approach to iden
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br Authors contributions br Acknowledgements
2020-12-07
Authors’ contributions Acknowledgements Introduction Retinoic STF 31 is a key signalling molecule in healthy development and in differentiation of stem cells, albeit uncontrolled levels of retinoic acid can lead to mutagenesis [1]. In eukaryotes retinoic acid is made by oxidation of all-tr
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In addition to through direct regulation of cell
2020-12-07
In addition to through direct regulation of cell differentiation, DDR2 may raise the abundance of myofibroblast subsets through advancing the recruitment of its precursor cells. One such evidence is that DDR2 can regulate lung fibroblast proliferation and migration. Another possibility rests on the
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Despite low respiratory rates in citrus fruit prolonged peri
2020-12-07
Despite low respiratory rates in citrus fruit, prolonged periods of storage may cause significant changes in the levels of organic acids (Echeverria and Valich, 1988). V-ATPase and V-PPase catalyze the electrogenic H+ translocation from the cytosol to the vacuolar lumen to generate an inside-acid pH
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br Proteases with special focus
2020-12-07
Proteases with special focus on cysteine proteases Vaccination using cysteine proteases as antigens with special emphasis on DNA-vaccines Concluding remarks In spite of the great potential of DNA vaccines, the technology has not been as revolutionary as expected in higher mammals. In fish,
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As previously stated the most unexpected finding from this
2020-12-04
As previously stated, the most unexpected finding from this series of compounds was the identification of a dimethyl isoxazole side chain that gave dramatically improved binding over the parent compounds. Holding this piece of the molecule constant, a series of analogs were made to further understan
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