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In untreated rodent or human hepatocytes PXR or CAR is
2019-08-28
In untreated rodent or human hepatocytes, PXR or CAR is stabilized by cytoplasmic co-chaperone partners like heat shock protein 90 (HSP90, Fig. 1). Upon ligand binding, the nuclear receptors are freed and translocated into the nucleus, identified as a pivotal step in PXR- or CAR-mediated transactiva
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Mitophagy is a selective autophagic process which
2019-08-28
Mitophagy is a selective autophagic process which leads to the degradation of damaged mitochondria in response to metabolic or environmental stress conditions. In this study, we found that LFS-01 treatment significantly enhances p62 in a time-dependent manner. We found that the upregulation of p62 i
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Behaviors were compared between saline and amphetamine
2019-08-28
Behaviors were compared between saline and amphetamine pre-treatment groups at 24h and 2 weeks following the last treatment, or between pre-treatment groups that received vehicle or ASV-30 infusions, using separate two-way ANOVAs. Significant effects were analyzed further using Student–Newman–Keuls
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The crystal structure of LiCoO
2019-08-28
The crystal structure of LiCoO2 is presented in Fig. 1. We can notice that the Li and Co atoms occupy the centers of two different edge-sharing [CoO6]-octahedra, which results in formation of separate Li and Co layers. Hence, the layered structure of LiMO2 is able to intercalate lithium into transit
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br Cytochrome P monooxygenases Cytochrome P monooxygenases
2019-08-27
Cytochrome P450 monooxygenases Cytochrome P450 monooxygenases (P450s) belong to one of Nature’s most versatile group of enzymes for C–H functionalization and are able to perform challenging regioselective and stereoselective activations of remote, unactivated C(sp3)–H bonds, for which there are
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The photocleaving properties of were studied by performing X
2019-08-27
The photocleaving properties of 1 were studied by performing ΦX174 photocleavage assays. Light irradiation of the mixtures of increasing amounts of 1 with supercoiled DNA caused>90% supercoiled form relaxation and approximately 5% of linearization for the higher concentrations of 1 (1:10bp and 1:2bp
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Compound was advanced to a chronic efficacy study
2019-08-27
Compound 52 was advanced to a chronic efficacy study in db/db mice maintained on a high fat diet. Animals were dosed with 0.5% methylcellulose vehicle, xanthine oxidase 52 (1, 3 or 15mg/kg, po, Q.D.) or 1 (0.3mg/kg) for 14days. Over the course of the study body weight and food intake were measured d
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Studies of Jelski and Szmitkowski show that differences
2019-08-27
Studies of Jelski and Szmitkowski show that differences of alcohol dehydrogenase (ADH) and aldehyde dehydrogenase (ALDH) activity between sphingosine 1-phosphate receptor modulator of many cancers and healthy tissue may be one of the factors intensifying carcinogenesis [7]. Moreover, changes of ADH
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CaneCPI showed strong inhibitory activity against
2019-08-27
CaneCPI-4 showed strong inhibitory activity against recombinant falcipain-2 and falcipain-3, with IC values of 11.9±0.4nM and 42.3±0.8nM, respectively (Table 1, Supplementary material). Falcipains are involved in hemoglobin cleavage, with generation of two fractions: the heme and the globin. The hem
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Experiments on the rat model of E coli pyelonephritis
2019-08-27
Experiments on the rat model of E. coli pyelonephritis, performed to investigate the relationship between the acute inflammatory processes and the permanent kidney damage (Brooks et al., 1974), have demonstrated a positive correlation between the degree of free radical-mediated renal injury and the
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Hydroxy Bupropion Acidic substituents showed moderate bioche
2019-08-27
Acidic substituents () showed moderate biochemical activity, but these compounds showed reduced cellular potency. Additional compounds bearing a carboxylic Hydroxy Bupropion were also prepared and tested (data not shown). All of acidic compounds showed low cellular potency regardless of their bioch
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AMPK is a master regulator of metabolic homeostasis
2019-08-27
AMPK is a master regulator of metabolic homeostasis, its broad spectrum of metabolic activities makes it an attractive target for treatment of metabolic and related disorders including Diabetes and Obesity (Madhavi et al., 2018). It controls lipid metabolism through its target genes PPAR-γ, C/EBP-α
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These findings further extend our knowledge of how
2019-08-27
These findings further extend our knowledge of how P4 and/or E2 can mediate anxiety and fear responses. Female rats in behavioral estrous and ovx rats administered systemic P4 and/or E2 demonstrated significantly less anxiety in the open field and/or elevated plus maze, compared to diestrous rats, a
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br Role of ERK signaling
2019-08-27
Role of ERK signaling in preventive and therapeutic potential of flavonoids in neurodegenerative diseases ERK is one of the main pharmacological targets of natural phenolic compounds and contributes to several therapeutic approaches including anti-atherogenic, anti-cancer, anti-colitis, anti-arth
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Biochemically the primary function of PPIP K is kinase media
2019-08-27
Biochemically, the primary function of PPIP5K2 is 1-kinase-mediated phosphorylation of 5-IP7 to form 1,5-IP8 (Shears, 2018). To a lesser extent, PPIP5K2 also phosphorylates IP6 to produce 1-IP7. Furthermore, PPIP5K2 has been shown to catalyze a reverse reaction, that is, dephosphorylation of 1,5-IP8
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