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The compounds were ranked based on the Glide XP Score
2021-04-26
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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With regard to the DGATs we
2021-04-26
With regard to the DGATs, we have found that the majority of algal species encode at least one DGAT1, although it appears to be absent from Ostreococcus and Micromonas, as is the case for yeast, S. cerevisiae. More surprising is the presence of multiple DGAT2 genes in algae, with the exception of C.
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TAK-242 receptor The anxiolytic like responses produced by a
2021-04-26
The anxiolytic-like responses produced by anti-SVG-30 suggests that CRF2 receptors mediate not only the elicitation of anxiety behavior induced by prior stress, i.e. conditioned freezing, but also unconditioned anxiety behavior induced by exposure to the unfamiliar environment of the elevated plus m
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Regarding the mechanism of action of CRF
2021-04-26
Regarding the mechanism of action of CRF, several studies have shown that low doses of CRF may preferentially activate CRF1 receptors in glutamatergic projection neurons, serotoninergic neurons or glutamatergic collaterals in the medial prefrontal cortex (Vertes, 2004). Indeed, prosencephalic inacti
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br Introduction The offspring of rodents emit vocalizations
2021-04-26
Introduction The offspring of rodents emit vocalizations when isolated from their dam. The majority of vocalizations by rat pups are in the ultrasonic band frequency of 30–50 kHz (Insel et al., 1986). Maternal separation-induced ultrasonic vocalizations are believed to represent distress signals
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Concerning firmness postharvest calcium dips for whole fruit
2021-04-26
Concerning firmness, postharvest calcium dips for whole fruit have been demonstrated to preserve firmness, cell wall structure (Glenn and Poovaiah, 1990), nutritional quality (Goldberg, 1984) and fruit flavour (Ortiz et al., 2009). Similarly, combinations of calcium treatment (0.5–4%) with packaging
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In recent years neuroimaging studies have
2021-04-26
In recent years, neuroimaging studies have increasingly demonstrated acute effects of THC on Neostigmine Bromide function, the vast majority of them involving a cognitive challenge (Bossong et al., 2014b). For example, without affecting performance accuracy, THC caused reductions in activity during
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Cx platin could improve the level of
2021-04-26
Cx-platin could improve the level of cellular uptake and DNA platination, hence triggering distinct DNA damage repair pathways. The data (Fig. 3B, C and D) demonstrated that Cx-platin could increase the foci number of γH2AX in cancer cells, preventing the efficient DSBs repair. This gives a good exp
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br Discussion The membrane PVase activity
2021-04-26
Discussion The membrane PVase activity components were discriminated in this work by pre-incubating with PMSF, mipafox, paraoxon or PMSF + mipafox to irreversibly inhibitPVase activity to discriminate the enzymatic components, (EPα, EPβ, EPγ and EPδ). The concentrations employed to discriminate t
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IAA sensitive Cl channels were shown to
2021-04-26
IAA-94-sensitive Cl channels were shown to mediate cardioprotection due to IPC (Diaz et al., 1999) and cyclosporine A (Diaz et al., 2013). CLIC-like channel activity was also observed in cardiac mitoplast (Misak et al., 2013) but the molecular identity of these intracellular Cl channels and their pr
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A putative SHBG receptor SHBG R
2021-04-26
A putative SHBG Bikinin synthesis (SHBG-R) has been postulated for about thirty years [66], [69], [70]. The characterization of this receptor has been researched by several groups. There are different ideas on how this receptor works. On the one hand Fortunati et al. provide evidence that SHBG is al
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At one time the biological effects of cAMP were thought
2021-04-26
At one time, the biological effects of cAMP were thought to be mediated exclusively by Protein Kinase A (PKA). Consistent with this, PKA inhibitors have been shown to reverse the effects of cAMP-elevating agents on VSMC proliferation [5]. However, we recently reported that cAMP-mediated inhibition o
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Oxamic acid In the present study promoting bile acid synthes
2021-04-26
In the present study, promoting bile Oxamic acid synthesis by activating EP4 receptors was shown to exert protection against hepatic steatosis. This finding may be relevant for treatment of non-alcoholic fatty liver disease, a major cause of liver disease and prominent indication for liver transplan
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Treatment with AAV EP also improved aspects of
2021-04-26
Treatment with AAV9-EP4 also improved aspects of adverse cardiac remodeling. The increased collagen deposition noted in the peri infarct and remote zone after MI was substantially attenuated by use of AAV9-EP4 and there were significant reductions in the number of macrophages and T AVE 0991 infiltr
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Many studies have documented that
2021-04-26
Many studies have documented that enolase acts as a plasminogen-binding protein and this interaction is involved in the tissue invasion and pathogenicity of the causative agents (Almeida et al., 2004; Avilan et al., 2000; Marcilla et al., 2007; Mundodi et al., 2008; Vanegas et al., 2007). Furthermor
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