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br Acknowledgements br Introduction Protein translation dema
2021-11-17
Acknowledgements Introduction Protein translation demands high fidelity. There are number of molecular checkpoints to fulfill this demand. Among these, insuring that a particular tRNA gets aminoacylated by its conjugate amino acid, which in turn is catalyzed by a particular aminoacyl-tRNA synt
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Here we examined whether complete ablation of GIP
2021-11-17
Here, we examined whether complete ablation of GIP production could reduce weight gain in the absence of the adipocyte hormone leptin, a condition that results in extreme hyperphagia, obesity, hyperinsulinemia, and insulin resistance, in both mice [24] and humans [25]. We found that Lepob/ob mice be
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Initially we carried out gap FRAP experiments
2021-11-17
Initially, we carried out gap-FRAP experiments using the two-photon configuration of the confocal microscope. A SR101-positive astrocyte was targeted and a 5 × 5 μm square area was exposed to a laser illumination (5 flashes of 5 s each during 25 s). This procedure resulted in a bleaching of this ast
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Since our new compound Fex could be a new
2021-11-17
Since our new compound Fex-3 could be a new FXR ligand, we try to demonstrate that Fex-3 was an intestinal-restricted FXR agonist which only activated FXR in the intestine not in the liver or other organs. Initially, we investigated this in Caco-2 AG-490 with transwell experiments. From and , we fou
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In the previous paper we described the
2021-11-17
In the previous paper, we described the design and synthesis of tricyclic thiazoles as FBPase inhibitors, and a series of SAR studies led to the identification of phosphate 3 and difluoromethylenephosphonate 4 exhibiting potent FBPase inhibitory activities (IC50=13, 47nM, respectively) (Fig. 2). In
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MMV s distinct mode of inhibition
2021-11-17
MMV019313's distinct mode of inhibition addresses key impediments in the development of PfFPPS/GGPPS inhibitors as antimalarial drugs. First, it is the first non-bisphosphonate inhibitor of Plasmodium FPPS/GGPPS with drug-like physicochemical properties satisfying the “Rule of 5” (Van Voorhis et al.
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We notice that previous reports of arsenic exposure
2021-11-17
We notice that previous reports of arsenic exposure are not completely consistent with each other, in terms of exposure-changed histone acetylations. In an early investigation, As exposure (7.5 μM) of HepG2 proton pump inhibitors increased H3K9ac after 24 h, when analyzed by methods of immunofluore
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In the present study fasting blood glucose and insulin level
2021-11-17
In the present study, fasting blood glucose and insulin levels were not significantly different between GA patients and control cases. Normal mammalian cells typically acquire fatty acids from the circulation owing to insulin, which is the most lipogenic hormone in the subset of adult tissues, inclu
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br Parkinson disease Idiopathic PD is a hypodopaminergic
2021-11-17
Parkinson disease Idiopathic PD is a hypodopaminergic movement disorder of uncertain etiology that affects 3% of persons over age 65 (Dexter and Jenner, 2013). Cardinal signs of this common neurodegenerative condition include bradykinesia, rigidity, rest tremor and postural instability. Autonomic
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However despite medicinal chemistry efforts lead
2021-11-17
However, despite medicinal chemistry efforts lead to considerable improvement in potency and selectivity of new HO-1 inhibitors, still have not identified inhibitors in the low nanomolar range. Therefore, due to the possible in vivo non-specific effects at high dosage, novel strategies should be dev
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Introduction Hepatocellular carcinoma HCC is
2021-11-17
Introduction Hepatocellular carcinoma (HCC) is the fifth most lethal malignant tumor worldwide and is the second leading cause of cancer-related death [1]. For HCC patients, wst-1 virus (HBV) infection is the important causative risk factor in Asia-Pacific regions [[2], [3], [4]]. In China, more th
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In contrast the sGC activator BAY relaxed the
2021-11-17
In contrast, the sGC activator BAY 58-2667 relaxed the CC in a concentration-dependent manner (Figure 4B), a response that was significantly increased in the CC of sGCβ1ki/ki mice compared with WT mice. The finding that BAY 58-2667 also possessed a corporal relaxing effect in WT mice is suggestive b
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Because of its excellent GPR potency good
2021-11-16
Because of its excellent GPR119 potency, good hERG selectivity and favorable rat t, ASP015K sale was scaled-up and further profiled. The synthetic protocols described in , were both suitable for a multi-gram scale synthesis of compound . An off-target screen was performed against an extensive panel
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Recently a G protein coupled receptor GPR a was
2021-11-16
Recently, a G-protein-coupled receptor, GPR109a, was identified as a molecular target for niacin. Mechanistic studies have suggested that the benefits of niacin therapy may result from the activation of GPR109a located on adipocytes. Recent experiments have shown that niacin activation of GPR109a re
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br Differences among flavivirus vaccines and
2021-11-16
Differences among flavivirus vaccines and implications for CD4 T cell immunity There are currently three classes of flavivirus vaccines in use – live-attenuated virus (for immunoprophylaxis against YF and JE), whole inactivated virus vaccines (JE, TBE) and chimeric vaccines (JE, DEN). The chimeri
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