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In addition to G coupling it
2020-07-24
In addition to Gα coupling, it is important to consider that the transition from goal-directed to habitual drug taking also relies on striatal D2R-A2AR heterodimers. Following cocaine self-administration, D2R-A2AR density is increased in the NAc, leading to greater antagonism of the inhibitory (anti
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Regarding their reported beneficial properties on
2020-07-24
Regarding their reported beneficial properties on the digestive tract, the aim of this study was to evaluate the effect of water extracts of three Hypericum sps., HP, HA, HU and some of the main phenolic compounds (Ch, R and Q) on DNA protection against oxidative and alkylating DNA damage induced by
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ARA metabolites which are produced through cytochrome P CYP
2020-07-24
ARA metabolites, which are produced through cytochrome P450 (CYP450) enzymes influence cardiovascular homeostasis. Human CYP4A11 and CYP1A2 metabolize ARA to 20-hydroxyecostearonic 74 (20-HETE) [11], which is a vasoconstrictor [12], platelet activator [13] and naturetic in the kidney [14]. On the o
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Data presented herein suggest that competent IL
2020-07-24
Data presented herein suggest that competent IL-18BP production in epithelial Kaempferol is implemented by epigenetic means based on demethylation of a single CpG site at −45 bp/−44 bp (CpG2) of the human IL18BP promoter. In contrast, retarded IL-18BP production in monocytic cells associates with C
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Our approach relied on measurement of bulk
2020-07-24
Our approach relied on measurement of bulk solute diffusivity in the three tissue types of interest. Our diffusivity values (Table 3) are on the order of 10−6 cm2/s and are comparable to the PG diffusion coefficient in water at infinite dilution, which is about 10−5 cm2/s at room temperature, as we
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In addition to PDCA we
2020-07-24
In addition to 2,4-PDCA, we also tested other broad-spectrum 2OG oxygenase inhibitors as vCPH inhibitors. N-Oxalyl glycine (NOG, IC50 = 21.2 ± 2.1 µM), a close 2OG isostere, and IOX1 (IC50 = 47.2 ± 2.7 µM), which is a relatively broad-spectrum JmjC demethylase inhibitor, were not as potent in inhibi
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In the present study DRD decreased
2020-07-24
In the present study, DRD3 decreased in the VTA of OA when compared with the control group. It is reported that DRD3 in the VTA control the firing rate of dopaminergic neurons and inhibition of these receptors enhance firing in the VTA-projecting neurons [18]. A study also indicated that morphine tr
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br Benefits and risks of traditional combined oestrogen
2020-07-23
Benefits and risks of traditional combined oestrogen–progestogen HRT regimens Combined oestrogen–progestogen regimens were developed to reproduce the short- and long-term benefits of oestrogen replacement therapy (ERT) and to simultaneously provide appropriate protection against oestrogen-related
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br Discussion The N terminal
2020-07-23
Discussion The N-terminal domain of DDRs has long been recognized as a member of the DS superfamily (Johnson et al., 1993, Karn et al., 1993), and its role in collagen binding is understood in atomic detail (Carafoli et al., 2009, Ichikawa et al., 2007). Our crystal structure shows that the secon
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br Introduction Prostaglandins are important local mediators
2020-07-23
Introduction Prostaglandins are important local mediators in a host of reproductive processes including ovulation, fertilization, embryonic development, luteal regression, and parturition (Ushikubi et al., 2000). Prostaglandin E2 (PGE2) is among the more versatile prostanoids, and its effects app
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PI K is a lipid kinase and
2020-07-23
PI3K is a lipid kinase and generates phosphatidylinositol-(3,4,5)-trisphosphate, which is a second messenger critical for the translocation of Akt to the cytoplasmic membrane. The phosphorylation of Ser473 Akt is important in the cell survival by regulating the eNOS among other targets (Dimmeler et
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br Genes involved in oxysterol metabolism The main
2020-07-23
Genes involved in oxysterol metabolism The main enzymes that participate in the metabolism of oxysterols generally belong into one of two groups: transferases or oxidoreductases [22]. The following chapter describes those genes of oxysterol metabolism whose polymorphisms have been associated with
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Here we describe preparation of three stable conjugates
2020-07-23
Here, we describe preparation of three stable conjugates that are linked by either oxyester, disulfide, or isopeptide bonds (Fig. 10.1). Each of these conjugates depends upon the prior purification of E2 and ubiquitin proteins that have been engineered to favor specific linkages. For the oxyester- a
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A growing body of data indicates that endothelial NOS eNOS
2020-07-22
A growing body of data indicates that endothelial NOS (eNOS) is a rate-limiting enzyme for the synthesis of nitric oxide (NO), its downstream nrf2 inhibitor molecule. High pathological concentrations of NO produced from inducible NO synthase (iNOS) induce apoptosis, whereas a reduction in the conce
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sigma receptor The potential off target activity of against
2020-07-22
The potential off-target activity of against other ATP-dependent enzymes, such as kinases, was also investigated. Encouragingly, there was no significant inhibition of ATP binding to 97 human kinases, when was evaluated at 10μM within a DiscoveRx scanEDGE® kinome screen (, ). All together, these d
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