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The question remained as to
2020-05-14

The question remained as to why hCrm1 was functional and mCrm1 was not in terms of Rev and HIV mRNA nuclear export, and previously we proposed three possibilities (Elinav et al., 2012). One was that human Madecassic acid had a positively acting factor that somehow stabilized the hCrm1 and Rev-RRE c
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The results showed that ethanol and acetaldehyde production
2020-05-14

The results showed that ethanol and acetaldehyde production was not affected by the presence of CPA-7. We observed that the concentration of ethanol increased throughout the assay up to 95–179 μL L-1 regardless of the treatment. The acetaldehyde concentration reached its highest values after 6–9 day
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Besides having a remarkable progestogenic effect
2020-05-14

Besides having a remarkable progestogenic effect, an additional characteristic of DRSP is its strong antimineralocorticoid effect and antiandrogenic action [11]. DRSP is characterized by an antimineralocorticoid effect that is stronger when compared to progesterone. The decreasing synthesis of proge
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Proinflammatory cytokines induce ER stress in
2020-05-14

Proinflammatory cytokines induce ER stress in many mammalian cell systems.32, 33, 34 Our results demonstrate that these cytokines also trigger ER stress in trophoblast JEG-3 cells. However, the severity of stress is likely low grade because only the PERK-EIF2A arm of the UPRER pathway was activated.
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istradefylline The strand domain swap in the UbV XR dimer
2020-05-14

The β strand domain swap in the UbV.XR dimer appears to be a unique arrangement for a Ub-based dimer. In solution, free Ub has a KD of ∼5 mM for the monomer-dimer equilibrium, and the two subunits in the dimer adopt a range of relative orientations involving residues from Ub’s β sheet (Liu et al., 2
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Concerning family A GPCRs although it
2020-05-14

Concerning family A GPCRs, although it has been described that several receptors are able to operate as monomers (Arcemisbéhère et al., 2010; Bayburt et al., 2011; Chabre & le Maire, 2005; Ernst, Gramse, Kolbe, Hofmann, & Heck, 2007; Hanson et al., 2007; Kuszak et al., 2009; Whorton et al., 2007), e
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In conclusion we have discovered two new derivatives and
2020-05-14

In conclusion, we have discovered two new derivatives ( and ) that are potent inhibitors of DHODH. H and C NMR spectroscopic data revealed that these compounds undergo ready isomerisation at room temperature in -DMSO, but the docking studies indicate that there is neither conformation nor configurat
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Mitochondrial depolarization induced by DHODH
2020-05-14

Mitochondrial depolarization induced by DHODH inhibition (Figure 5A) may also contribute to the selective effects of DHODH inhibitors on KRAS mutant cells. If so, the effect may arise more from pro-apoptotic effects of mitochondrial depolarization (Lemasters et al., 1998) than from impaired oxidativ
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Interestingly all three lesions that significantly inhibited
2020-05-13

Interestingly, all three lesions that significantly inhibited transcription – CPD, εA and the AP site, – promoted insertion of Dimesna residues opposite the damaged nucleotide. Thus, bacterial RNAP seems to follow the so-called ‘A-rule’ for incorporation of nucleotides opposite AP-sites and bulky l
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MTX and MTXPGs block the activity of the key enzyme
2020-05-13

MTX and MTXPGs block the activity of the key enzyme DHFR (Fig. 1), which converts folates to their active forms – dihydrofolate (DHF) and tetrahydrofolate (THF). MTXPGs also potently inhibit thymidylate synthase (TS). Furthermore, during dTMP synthesis, TS utilizes the cofactor 5,10-methylene THF, w
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br Discussion Cytomegalovirus CMV is a herpes virus that cau
2020-05-13

Discussion Cytomegalovirus (CMV) is a herpes virus that causes primary infection in normal hosts and re-activation infection in compromised hosts with impaired CMI, e.g., organ transplants. Following primary infection, which may be severe, CMV becomes latent in lymphocytes. Reactivation may occur
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Nevertheless because of the preclinical work
2020-05-13

Nevertheless, because of the preclinical work and the interference with EWS–FLI1 transcriptional activity, we believe that there may be a role for ET-743 in Ewing sarcoma. An analysis of the pharmacokinetic data published in the phase II clinical trial shows that at most the drug spent 5 to 6days ou
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Previous studies from our lab
2020-05-13

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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That DGAT mediated hepatic steatosis did not lead
2020-05-13

That DGAT-mediated hepatic steatosis did not lead to insulin resistance was clearly demonstrated in Liv-DGAT2-low mice by their normal blood glucose and plasma insulin levels, normal glucose and insulin tolerance, normal insulin sensitivity by hyperinsulinemic-euglycemic clamp studies, and normal he
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The first purpose of the current
2020-05-13

The first purpose of the current study was to characterize a standardized experimental model of postprandial hyperlipidemia in various rodent species. To our knowledge this study provides the most comprehensive and systematic evaluation of rodent models of postprandial hyperlipidemia to date. We ada
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