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The first rationally designed dual
2023-05-30

The first rationally designed dual mPGES-1/5-LO inhibitor was reported in 2008 and represents a structural derivative of pirinixic p-Chlorophenylalanine - a synthetic agonist of PPARα with lipid-lowering properties (Koeberle et al., 2008b). Further α-alkyl- and α-aryl-substituted derivatives have b
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The ATX LPA signaling axis has been implicated
2023-05-30

The ATX–LPA signaling “axis” [5] has been implicated in a perplexing variety of physiological and pathophysiological processes, including vascular and neural development [5], [26], [27], [28], [29], tumor progression and metastasis [30], [31], lymphocyte trafficking [22], bone development [32], neur
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We also showed that steatosis induced an additional
2023-05-30

We also showed that steatosis induced an additional increase of ASK1 activation that was associated to the exacerbation of hepatocyte and liver damage and was unrelated to ER stress. Indeed, several settings, also different to ER stress, can induce ASK1 activation and many of them involve oxidative
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br Technical Note Fungal spoilage of dairy
2023-05-29

Technical Note Fungal spoilage of dairy products remains a major concern for dairy manufacturers despite the use of preventive and control approaches, including the use of chemical preservatives. Among methods that are increasingly used by industries for microbial contaminant control, biopreserva
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It is noteworthy that in both
2023-05-29

It is noteworthy that in both cases there is a higher risk for prematurity [44], [61], [97], [98] and for deliveries of newborn small for GA [89], [95], [97], [98]. sFlt-1:PlGF has been showed to be inversely correlated with GA at birth, since 86% of pregnant women who gave birth at glycoprotein inh
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Recently two distinct small molecule inhibitors of PHGDH
2023-05-29

Recently, two distinct small-molecule inhibitors of PHGDH were identified using high-throughput screens, both of which inhibit de novo serine biosynthesis and show selective toxicity to cancer pergolide sale with high SSP flux [50,51]. The inhibitor NCT-503, which has an IC50 of 2.5μM, reduces the
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raloxifene hydrochloride br Materials and methods br Results
2023-05-29

Materials and methods Results and discussion Conclusions In this study, for the first time to the best of our knowledge, the stability of pure hsALDH has been studied under various conditions. The enzyme exhibited low storage stability both at 4°C and 25°C, which could be improved to a good
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To guide our attempts at
2023-05-29

To guide our attempts at achieving AKT potency and selectivity against p70S6K and other kinases from (p70 S6K IC: 0.004 μM) and , we took advantage of exploiting the subtle sequence differences in the active sites of the AGC family kinases, we utilized the information around crystal structure of AK
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Adenosine is a ubiquitous homeostatic
2023-05-29

Adenosine is a ubiquitous homeostatic purine nucleoside that accumulates extracellularly in response to metabolic stresses such as hypoxia and inflammation. Activation of either G protein-coupled adenosine receptors (ARs; A1R, A2AR, A2BR, and A3R) by extracellular adenosine can modulate cell signali
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Further evidence for ACh GABA
2023-05-29

Further evidence for ACh/GABA cotransmission had also been observed in the cortex. Extensive axonal arborization from cholinergic BF neurons exists throughout the cortical layers, allowing direct observation of cholinergic synaptic terminals. One study in the visual cortex of cat examined immunolabe
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In addition to the data provided by the Ki
2023-05-29

In addition to the data provided by the Ki16425 treatment in the K/BxN arthritis model, new findings from the study of two new LPA receptor antagonists confirm the involvement of the LPA pathway in the pathogenesis of experimental arthritis. In the study by Miyabe et al., the authors reported the tr
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Our results suggest that plasma membrane and a
2023-05-29

Our results suggest that plasma membrane and a3-containing V-ATPases represent an important and novel target in the development of drugs to limit breast cancer metastasis. That knock-down of a3 has been shown to reduce metastasis of melanoma cells in an in vivo mouse model suggests that this role ma
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CHK has been reported to be
2023-05-29

CHK1 has been reported to be the kinase responsible for H3.3S31 phosphorylation in human ALT cancer N,N-Dimethylsphingosine . However, in our study, knockdown of CHK1 in HEK293F (Figs. S1c and S6) or HeLa S3 (data not shown) cells did not result in a significant decrease in H3.3S31ph, which is in ag
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We used the lead compound C to demonstrate that small
2023-05-29

We used the lead compound C4 to demonstrate that small molecule ACL inhibitors can recapitulate ACL knockdown (KD) in modulation of cancer stemness. We have shown previously that ACL KD reduced the CSC population in multiple cancer cell lines. The E-snail cells are an established CSC model system.
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br Experimental section br Competing interests br Author
2023-05-29

Experimental section Competing interests Author's contributions Acknowledgement This research is partially supported by a seed fund for the Center for Drug Discovery and Translational Research (LS) and a research grant by Fujifilm (VPS and LS). The Sponsors played no roles in study desig
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