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To further investigate the possible interaction of L
2021-12-28

To further investigate the possible interaction of L1 with β1-sGC, a protein-ligand docking experiment was performed. Calculations were carried out with the program GOLD (version 5.2) [18], [34] and performed with the chemPLP scoring function [19], [34]. The ten lowest energy solutions presented a r
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After establishing improved GSNOR potency some of the potent
2021-12-28

After establishing improved GSNOR potency, some of the potent inhibitors were further evaluated for microsomal stability and CYP inhibition studies (). Majority of the tested analogs revealed high metabolic stability in human and rat liver microsomes, and moderate to low stability in mouse liver mic
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resazurin mg br Conclusion br Conflict of interest
2021-12-28

Conclusion Conflict of interest References and recommended reading Papers of particular interest, published within the period of review, have been highlighted as: Acknowledgements Introduction Free fatty acids (FFAs) are essential nutrients that contribute to various cellular functio
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daprodustat mg br Lactate metabolism L Lactate
2021-12-28

Lactate metabolism L-Lactate is an intermediate metabolite in glucose metabolism. Glucose can be broken down to pyruvate, and pyruvate can be either further oxidized to acetyl-CoA and enter the TCA cycle, or reduced to L-lactate by lactate dehydrogenase (LDH). In turn, LDH can oxidize L-lactate t
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XAP044 receptor In this study we describe the role
2021-12-28

In this study, we describe the role of a specific species of LPI in the secretion of GLP-1 from enteroendocrine L-cells and primary cell preparations. We further demonstrate the specific role of GPR119 in LPI-dependent GLP-1 secretion. To achieve this, we downregulated GPR119 and GPR55 protein expre
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Trypanosomatid GLO enzymes are monomeric and
2021-12-28

Trypanosomatid GLO2 enzymes are monomeric and contain a zinc–iron binuclear metal center (Irsch and Krauth-Siegel, 2004, Silva et al., 2008), similar to all other glyoxalases II. As mentioned, in T. brucei there are two GLO2 genes but only one encodes an enzyme with glyoxalase II activity (Irsch and
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SMI-4a The occurrence of MDR in
2021-12-28

The occurrence of MDR in cancer patients undergoing chemotherapy can be mimicked in the laboratory by culturing cancer SMI-4a in the presence of chemotherapeutic drugs, thereby enforcing the evolution of acquired drug resistance. This has been described in multiple model systems including the rhabdo
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br Conclusion Until recently astrocytes were
2021-12-28

Conclusion Until recently, astrocytes were recognized solely for their maintenance role in the regulation of p-nitro-Cyclic Pifithrin-α homeostasis. Nowadays, this idea has changed, it is clear that these cells play a crucial role in the regulation of neuronal activity and signal transmission. In
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Activation of Akt signaling is common
2021-12-28

Activation of Akt signaling is common in nearly all of the human malignancies (Altomare & Testa, 2005). It has been reported that microRNA-200c targets Akt signaling pathway to inhibit cell apoptosis of pituitary adenoma (Liao et al., 2014). In addition, Akt signaling pathway regulates the expressio
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A pooled overall survival analysis at year
2021-12-27

A pooled overall survival analysis at 1year showed no difference in survival between the two study arms, although these studies were not designed or powered to demonstrate a survival benefit. Among the 979 total patients in both ROMANA 1 and 2, about 55% continued on to the ROMANA 3 trial. That tria
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D appears to be important
2021-12-27

D83 appears to be important for receptor function as a mutation to an alanine produced a non-functional channel. Interestingly, maintaining the charge as in D83E produced only a small reduction in GABA sensitivity. Other mutations at this position which included residues capable of hydrogen bonding
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Freinkel first reported in the late s that
2021-12-27

Freinkel first reported in the late 1960s that maternal hypertriglyceridemia benefits the fetus during starvation by increasing maternal consumption of triglyceride for ketone body synthesis giving the basis for “accelerated starvation” theory [4,5]. This maternal metabolic reprogramming during peri
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Before cell motility assay cells were pretreated with GW
2021-12-27

Before cell motility assay, JANEX-1 were pretreated with GW1100 (1 μM), which is an antagonist of GPR40 [20], [21]. GW1100 increased the cell motile activity of MG63-R7 cells in the presence of GW9508, similar as observed with MG-63 cells (Fig. 4A). Moreover, to confirm the effects of GPR120 on the
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The biological activity at GPR a of each of
2021-12-27

The biological activity at GPR109a of each of the 4-functionalized-5-alkyl-pyrazole-3-carboxylic acids (–) was measured using a cAMP whole cell Dynamic2 Homogenous Time-Resolved Fluorescence (HTRF) assay (). Twelve compounds were found to exhibit an EC below 1μM, and of these seven exhibited EC valu
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perhexiline synthesis Originally identified as a GPCR upregu
2021-12-27

Originally identified as a GPCR upregulated on Burkitt lymphoma cells upon Epstein-Barr virus infection (Birkenbach et al., 1993), Ebi2 was later found to play critical roles in immunity by regulating the migration of activated perhexiline synthesis to extrafollicular sites for early plasmablast re
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