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The chemical structure of BAs consists of a
2021-11-09

The chemical structure of BAs consists of a steroid nucleus with an acidic side chain. They are amphipatic molecules characterized by a hydrophilic α-face and a hydrophobic β-face. The hydrophobic pocket of the FXR LBD interacts with BAs largely through the β-face. The α-face contains several hydrox
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Emerging evidence has shown that pharmacological FXR agonism
2021-11-09

Emerging evidence has shown that pharmacological FXR agonism attenuates chronic alcohol treatment-induced liver injury and steatosis [18], [19], while whole-body FXR knockout worsens alcohol-induced liver injury [19]. This suggests that FXR plays an important role in ALD development. However, defici
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In stark contrast to this study Zhang and colleagues demonst
2021-11-09

In stark contrast to this study, Zhang and colleagues demonstrated that FFA4, along with FFA1, play roles in suppressing cell proliferation and promoting apoptosis in CRC nucleoside analogs treated with omega-3 PUFA [53]. In this study design, in vivo CRC was induced in mice upon treatment with the
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In addition to attenuating joint inflammation via T
2021-11-09

In addition to attenuating joint Gallein via T cells, Cpd43 could also decrease the severity of CIA/AIA by suppressing the function of innate leukocytes such as neutrophils and macrophages via FPRs, as has been shown in other acute inflammatory models including neutrophil/macrophage-mediated K/B × N
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Clinical data showed TAK was rapidly absorbed with a half
2021-11-09

Clinical data showed TAK-875 was rapidly absorbed with a half-life of 28-30h and clearance primarily through glucouronidation in the liver with minimal urinary clearance [30]. TAK-875 made the glycosylated hemoglobin (HbA1c) levels fall significantly from baseline after 24-week administration in onc
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Phosphorylation of the p Rel A dimer the most common
2021-11-09

Phosphorylation of the p50-Rel A dimer, the most common form of NF-κB, leads to ubiquitination of IκB proteins (Fig. 2). Poly-ubiquitination of IκB proteins identifies them for rapid degradation by 26S proteasomes, thereby allowing NF-κB dimers to undergo nuclear translocation and activate the trans
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Lastly the N position of this privileged pyrimidone was furt
2021-11-09

Lastly, the N-1 position of this privileged pyrimidone was further substituted by a variety of different aromatic, aliphatic or heteroaromatic linkers with carbonyl functionality. In this task, different N-1 substituted pyrimidones 20i–20xiv were generated and check against HIV IN 3′-processing and
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NeuroHIV is initiated by HIV crossing the blood brain barrie
2021-11-09

NeuroHIV is initiated by HIV crossing the blood–brain barrier (BBB) to enter the CNS. This is thought to occur primarily via the transmigration of infected CD14+CD16+ monocytes (Williams, 2014), using the monocytes as “Trojan Horses” (Peluso, 1985), although some studies suggest alternate routes of
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The most abundant form of Hat
2021-11-09

The most abundant form of Hat1p in the nucleus is apt to be in the form of the NuB4 complex [96]. In the context of sodium fluoride assembly, the function of the NuB4 complex may be similar to that ascribed for the cytoplasmic HAT1 complex. That is, the NuB4 complex may be involved in directing ne
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br Medium and long chain fatty
2021-11-08

Medium- and long-chain fatty vegf inhibitor receptors Clinical studies of ω3 fatty acids Clinical studies have established that dietary intake of ω3 fatty acids should be around 4g/day for treating very high triglyceride levels (≥5.7mmol/L) [36]. Low-dose supplementation with EPA + DHA (400mg
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Much of the understanding of this system has come from
2021-11-08

Much of the understanding of this system has come from several studies focussed on CB1. A significant amount of research has demonstrated that activation of the CB1 receptor by cannabinoid ligands stimulates food intake [10], reduces gastrointestinal motility [11], and increases lipogenesis [12] and
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In previous work we showed that benzophenanthridines do
2021-11-08

In previous work we showed that benzophenanthridines do not affect the surface expression of GlyT1 (Jursky and Baliova, 2011). The results from the surface biotinylation studies reported in Fig. 3 show that the surface expression of the Y370F mutant is not significanly affected by the alkaloids in
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br Material and methods br Results
2021-11-08

Material and methods Results Discussion Organisms have developed a variety of anti-glycation defense mechanisms. In Irsogladine to the aldose-reductase-pathway or 2-oxoaldehyde dehydrogenase-pathway, the glyoxalase system is the only mechanism, which is not restricted to liver [19]. This s
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MDV 3100 To test our refinement protocol we considered a ben
2021-11-08

To test our refinement protocol, we considered a benchmark set of 12 N-linked glycan-containing protein structures determined by X-ray crystallography at resolutions ranging between 1.9 Å and 3.5 Å and comprising a total of 133 glycan units. We identified four incorrect anomeric configurations and 2
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br GluR A knockout mice Genetically modified adult mice lack
2021-11-08

GluR-A knockout mice Genetically modified, adult mice lacking the GluR-A AMPA receptor subunit exhibit fast synaptic transmission in the hippocampus, mediated by the receptors formed from the remaining AMPA receptor subunits GluR-B and GluR-C (Sommer et al., 1991), but are deficient in a rapidly
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