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It was speculated that could affect the protein translation
2021-11-29

It was speculated that could affect the protein translation or processing in the HCV replication cycle. The viral protein processing was thus investigated, to establish whether the HCV inhibition was determining an increased amount of unprocessed polyprotein, due to a block in the processing, or a
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br Amino acids The role of leucine Amino acid metabolism
2021-11-29

Amino acids: The role of leucine Amino L-α-Aminoadipic Acid sale metabolism plays a central role in brain physiology, as several amino acids serve as biosynthetic precursors for neurotransmitter synthesis [36]. In addition, the amino acids L-leucine and L-lysine may participate in ketogenesis. F
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In summary we have designed and optimized a
2021-11-29

In summary, we have designed and optimized a new series of 1,4-dioxycyclohexane GPR119 agonists. SAR studies led to the discovery of the preferred molecule that has potent and efficacious GPR119 activity across species. This lead compound exhibited an excellent ADME and safety profile, and demonstr
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The precise mechanisms of action
2021-11-29

The precise mechanisms of action of 4-PBA are as yet ambiguous. Its capacity as a chemical chaperone has been thoroughly documented for the ABC transporter family in particular (Prulière-Escabasse et al., 2007; Iram and Cole, 2014; Gordo-Gilart et al., 2016; Pomozi et al., 2017). 4-PBA has been clas
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To help resolve the question of
2021-11-26

To help resolve the question of simple binding versus transport, we reasoned that if quercetin is transported by GLUT1, we should be able to block its uptake by other GLUT1 inhibitors. We initially investigated the effects of two newly identified GLUT1 inhibitors, BAY-876 and WZB-117. WZB-117 was fi
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The main aim of our study was to identify whether
2021-11-26

The main aim of our study was to identify whether glucokinase and Irs2 were required for beta cell replication induced by short-term HF diet feeding. Glucokinase plays a critical role in regulating blood glucose levels by catalysing the rate-limiting biochemical reaction of glycolysis [26,27]. In pa
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br Introduction Calorie restriction CR in the absence of
2021-11-26

Introduction Calorie restriction (CR), in the absence of malnutrition, has beneficial effects on caffeic acid phenethyl ester function, including reducing the incidence of age-related neurodegenerative disease (Gräff et al., 2013), eliciting anti-depressant behavior (Lutter et al., 2008) and imp
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We tested formyl MYVKWPWYVWL which we had previously shown t
2021-11-26

We tested formyl-MYVKWPWYVWL, which we had previously shown to have essentially identical Kis for W190/N192, R190/K192 and R190/N190 [8] of 130 nM, for its ability to downregulate surface receptor (Fig. 5A). R190/K192 exhibited the lowest EC50 of 44±4 nM about 3 fold below the observed Ki and a maxi
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Another TKI used in cancer
2021-11-26

Another TKI used in cancer therapy is the Abl inhibitor imatinib mesilate which has also a beneficial effect on glucose homeostasis in diabetic humans [39], [40], [41]. Imatinib has a clear impact on NFκB activation and anti-apoptotic preconditioning of β-cells [39], attenuating islet inflammation [
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Besides its carcinogenic role WTAP
2021-11-26

Besides its carcinogenic role, WTAP was also discovered to participate in several physical processes in normal cells. As previously reported, WTAP was involved in cell proliferation, survival, apoptosis [7,29,30], eye development [8] and embryonic development [7] owing to its complex function in tra
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br Development of calibrators and controls for DiXaIs br Met
2021-11-26

Development of calibrators and controls for DiXaIs Method validation and comparison with reference technique (LC:MS) At this stage, anti-Factor Xa bioassays can be established for reliably measuring DiXaI concentrations in plasma, with the available appropriate drug specific calibrators and co
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The results show that pimarane and strobane diterpenoids exe
2021-11-26

The results show that -pimarane and -strobane diterpenoids exert inhibitory effects on FXa suggesting that they may have potential as FXa inhibitor. However, it should be noted that some compounds such as compounds , , , and are poorly bioavailable. Thus, the current study indicates that the number
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NeuroHIV is initiated by HIV crossing the blood
2021-11-26

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 finding of histamine action on ASICs also
2021-11-26

The finding of histamine action on ASICs also raises the question about possible action of other histamine receptor ligands. In the present work we selected several compounds and performed electrophysiological testing of their action on recombinant homomeric ASIC1a and ASIC2a. Nα-methylhistamine is
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Relative to the impact of moderate PAE
2021-11-26

Relative to the impact of moderate PAE on markers of histaminergic neurotransmission, there were four salient observations from the studies reported here. First, it does not appear that moderate PAE affects the number of HDC-positive neurons in the tuberomammillary nucleus of the ventral hypothalamu
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