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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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br Materials and methods br Results br Discussion
2020-07-22
Materials and methods Results Discussion Plg plays important roles in various physiological processes, such as fibrinolysis, proteolysis, cell migration, differentiation, tissue remodeling, and inflammation [6], [7], [8]. We herein found that Plg deficiency enhanced insulin secretion, and
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br Alcohol and the amygdala br Alcohol and the
2020-07-22
Alcohol and the amygdala Alcohol and the CRF1 system Given the marked effects of alcohol on inhibitory neurotransmission in the amygdala and the regulation of amygdalar GABAergic activity by CRF and activity at the CRF1 receptor, the CRF system is a logical site for the actions of alcohol in t
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br Introduction Abdominal aortic aneurysm
2020-07-22
Introduction Abdominal aortic aneurysm (AAA) is a daily concern in vascular surgery, as successful treatment is exclusively achieved by open or endovascular repair. Its prevalence is 2–11% among male smokers, and rupture the major complication, is associated with unacceptably high morbidity and m
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The chemical structures of I
2020-07-22
The chemical structures of I3C, 3MOI, and 3MI and the A-54556A responsible for 3MI metabolism in rainbow trout and carp are shown in Fig. 4. Discussion To determine the individual CYP450 isoforms involved in 3MI metabolism, we used specific inhibitors for CYP1A, CYP3A and CYP2E1. Our results su
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Likewise the conserved cysteine in the E protein
2020-07-22
Likewise, the conserved cysteine in the E2 protein is the only residue shown to be essential for the transfer of Ub/Ubl from E2 to the HECT ligases (Dye and Schulman, 2007, Wu et al., 2003). However, all other terminal Ub/Ubl transfer reactions involving E2 enzymes suggest a critical role for the ta
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The inhibition of mRFP Ub E formation
2020-07-21
The inhibition of mRFP-Ub–E1 formation by ginsenosides Re was not in time-dependent in vitro (Fig. 4B). Fifty micrometres ginsenoside Rg1 decreased E1 activity to 0.24- to 0.36-fold over 30min. This finding suggests that ginsenoside Rg1 may irreversibly inhibit mRFP-Ub–E1 formation or a tight-bindin
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br Conclusions In Summary a multilayer screening of
2020-07-21
Conclusions In Summary, a multilayer screening of xanthones of natural origin (Xanthone-NPs) was undertaken against Pf-DHFR. The Re-rank score of screened compounds was size normalized and interaction profile was generated using experimentally known inhibitors. Three compounds X5, X113A and X164B
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