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More recently Vismodegib was administered in combination wit
2022-05-09

More recently, Vismodegib was administered in combination with Gemcitabine in a pilot clinical trial that enrolled 23 patients affected by metastatic pancreatic adenocarcinoma. This type of malignancy is the most frequent form of pancreas cancer and is ranked in fourth place for cancer mortality in
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In an effort to further improve the intrinsic
2022-05-09

In an effort to further improve the intrinsic potency, we evaluated the effect of the C4-substituent of the triazole (). Replacement of the phenyl group with a cyclohexyl or with a 2-pyridyl substituent led to losses in potency. Increasing the size of the substituent to a bi-phenyl or naphthyl gr
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br Activation of soluble guanylate cyclase The molecular ste
2022-05-09

Activation of soluble guanylate cyclase The molecular steps involved in sGC activation have evolved significantly over the last several years. The key studies are outlined below, but here we provide an overall summary. The activation mechanism of sGC was initially proposed to be relatively simple
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As previously discussed even though glucose is the major fue
2022-05-07

As previously discussed, even though glucose is the major fuel of the brain, neuronal cells may use alternative fuels such as ketone bodies in metabolically challenging situations in which glucose availability is limited [6]. Ketogenesis takes place mainly in the liver, although astrocytes can also
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With this goal in mind we proceeded to explore
2022-05-07

With this goal in mind, we proceeded to explore the C5-heteroaryl class of pyrazole-acids. Initial efforts, focused on a thiophene replacement, demonstrated little improvement. The 2-thiophene derivative (0.25μM and 0.24μM), a surrogate to the phenyl moiety, demonstrated only a modest boost in activ
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One clue to how evolution
2022-05-07

One clue to how evolution has solved such spatiotemporal challenges comes from studies revealing that lymph node (LN) organization is more complex than originally presumed, suggesting that steady-state microanatomical features are crucial for effective immune responses (reviewed by Qi et al., 2014).
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In conclusi http www apexbt
2022-05-07

In conclusion, Glu transactions in glia cells are mediated through Glu receptors and transporters. From a biochemical perspective, the specificity of the cascades has started to be elucidated. A model of our present findings is depicted in Fig. 6. Acknowledgements This work was supported by Gran
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About epilepsy no specific seizure type has been identified
2022-05-07

About epilepsy, no specific seizure type has been identified because GLUT1-DS is associated with a wide range of epilepsies: patients develop seizures in infancy and early childhood, which are, frequently, do not respond to anticonvulsant medication. In infants, seizures are described as brief, subt
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br Acknowledgements br Introduction High
2022-05-07

Acknowledgements Introduction High-intensity noise exposure has long been known to induce damage in the peripheral and central auditory system, often resulting in auditory pathologies such as hearing loss, tinnitus and hyperacusis (Syka, 2002; Roberts et al., 2010). Within the inner ear, struc
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Imiquimod In conclusion our results show that multiple
2022-05-07

In conclusion, our results show that multiple receptor populations can be expressed when α4, β3 and δ mRNAs are injected into Xenopus oocytes and include β3 homomeric; α4β3; and β3δ receptors. The previously unidentified β3δ can be differentiated pharmacologically from either β3, α4β3 and α4β3δ rece
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In this study we have investigated the expression of FXR
2022-05-07

In this study, we have investigated the expression of FXR and TGR5 in CCA tissues in two independent cohorts of patients and determined their association with tumor clinicopathological parameters. The expression of both BA receptors was also evaluated in CCA human cells and normal human cholangiocyt
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The improved glucose tolerance of
2022-05-07

The improved glucose tolerance of Ffar1R258W/R258W mice on HFD was unexpected. In combination with similar fasting blood glucose levels, the significant lower fasting plasma insulin of mutant mice compared to wild-type mice is indicative of improved insulin sensitivity. However, peripheral insulin r
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A common feature of ferroptosis is the
2022-05-07

A common feature of ferroptosis is the iron-dependent accumulation of lipid-ROS and the subsequent depletion of polyunsaturated fatty (S)-Crizotinib phospholipids (PUFA-PLs) [118]. The PUFA chains of membrane lipids are more susceptible to both enzymatic and non-enzymatic oxidation, which results i
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In order to understand the determinants of high affinity
2022-05-07

In order to understand the determinants of high affinity of with amide side chain, an X-ray crystal structure of human liver FBPase in complex with was determined (). The position of phosphonate group and tricyclic scaffold of is similar to those of with no side chain, which suggests the formati
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Sumoylation is involved in regulating protein protein intera
2022-05-07

Sumoylation is involved in regulating protein-protein interactions, subcellular protein localization, protein stability, and transcriptional factor activity (reviewed in [29]). The small ubiquitin-like modifier (SUMO) protein is covalently attached to a lysine residue in a Ψ-K-X-D/E consensus sequen
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