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FXR agonists represent an attractive class of drugs
2021-09-26
FXR agonists represent an attractive class of drugs for patients with PFIC. Synthetic and semi-synthetic FXR agonists, with higher affinity and potency to activate FXR, have been successfully tested in animal models of cholestasis. In these murine models, the semi-synthetic steroidal FXR ligand obet
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A frequent complication of SIRS
2021-09-26
A frequent complication of SIRS and sepsis is the development of increased airway resistance and lung inflammation [2], [3]. For example, Uhlig et al. [3] demonstrated that rat lungs exposed to endotoxin present increased airway resistance due to constriction of terminal Adapalene receptor [3] More
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Magtanong et al observed that caspase dependent apoptotic
2021-09-26
Magtanong et al. (2019) observed that caspase-dependent apoptotic lipotoxicity of saturated fatty acids is suppressed by exogenous MUFAs. This may explain the ability of MUFAs to prevent atherosclerosis, in contrast to the pathogenicity of saturated fatty acids. Moreover, MUFAs may promote while PUF
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The primary or in transit site of
2021-09-26
The primary or in-transit site of metastasis for many cancers, including melanoma, are nearby sentinel lymph nodes (LNs) [6]. As such, sentinel LN biopsy is a common procedure to diagnose and stage melanoma progression [7,8]. Sentinel LNs are often the primary site of metastasis due to tumor cell-st
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Experiments show that CSD propagation can be slowed or inter
2021-09-26
Experiments show that CSD propagation can be slowed or interrupted by pre-existing lesions or areas of high astrocytic density (Chen et al., 2006), and reduced expression of astrocytic gap junctions significantly increases the size of ischemic infarcts (Nakase et al., 2003). By decreasing the gap ju
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Cellular inhibition is caused by
2021-09-26
Cellular inhibition is caused by the hyperpolarization of the cell and is mediated by both synaptic and extrasynaptic GABAARs. Synaptic GABAARs are sensitive to high concentrations of GABA released at the synapse and mediate phasic inhibition. In contrast, extrasynaptic GABAARs mediate tonic inhibit
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Hydantoin in region F bridging the phenoxybenzene
2021-09-26
Hydantoin in region F bridging the phenoxybenzene and benzimidazole moieties was replaced by cyclic building blocks, diketopiperazine (25) and imidazolidinone (26), and linear bonds, amide (27) and urea (28). Analogs 25–28 possessing the linkers other than hydantoin were not tolerated in LBD of FXR
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Recent evidence indicates that prolonged vasoconstriction of
2021-09-26
Recent evidence indicates that prolonged vasoconstriction of conductance and resistance arteries involves VSMCs 87 8 polymerization, through activation of small GTPases [4] and a subsequently transition to a more solid rheology [5]. Actin polymerization occurs in two steps, nucleation and elongatio
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In this current study we not only demonstrated the
2021-09-26
In this current study, we not only demonstrated the growth-inhibitory effects of the 2nd generation analog SL-1-39 on the HER2+ breast cancer cells, MDA-MB-453 and SKBR3 (Table 1), but we also demonstrated that the decrease in cell number was associated with an interruption of Oxaliplatin progressi
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Of xenobiotic quinones thymoquinone methyl isopropyl
2021-09-24
Of xenobiotic quinones, thymoquinone (2-methyl-5-isopropyl-1,4-benzoquinone; Fig. 1) is one of the most thoroughly studied for its pharmacological properties. It is the most active component of Nigella sativa, commonly called black cumin2, 3, the essential oil of the seeds of which are used for trea
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12-O-tetradecanoyl phorbol-13-acetate Lactate induced GPR ac
2021-09-24
Lactate-induced GPR81 activation was confirmed with a fluorimetric imaging plate reader (FLIPR) assay, in which lactate induced a [Ca2+] flux in CHO cells stably expressing Gqi5 and HA-GPR81 but not vector control (Fig. 1C). The EC50 of lactate in the FLIPR assay was 4.3±0.73mM, a value well within
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The first described synthetic FFA active agonist GW
2021-09-24
The first described synthetic FFA1 active agonist, GW9508 (4- [(3-phenoxyphenyl)methyl]amino benzenepropanoic acid), was immediately shown to also activate FFA4, although with some 100-fold lower potency [38]. Therefore, in the initial absence of FFA4-selective synthetic agonist ligands, GW9508 was
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Level of CD and other blood parameters in
2021-09-24
Level of CD4 and other blood parameters in patients before and after intervention are presented in Table 2. The mean of the CD4+ level before treatment in the intervention and placebo groups was 161.5 ± 291.1 and 159.9 ± 337.4, respectively (P = 0.232), which increased after treatment in both groups
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pkm2 Several groups studied CTD mouse models which largely m
2021-09-24
Several groups studied CTD mouse models, which largely mimicked the symptoms (i.e. impaired cognition and autistic-like behaviour) of the human disease (Kurosawa et al., 2012; Baroncelli et al., 2016; Stockebrand, 2018). The CRT-1 knockout mice showed a drastic deterioration in the GABAergic system,
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AR-12 australia The following are the supplementary data rel
2021-09-24
The following are the supplementary data related to this article. Conflict of interest Acknowledgements This work was supported by JSPS KAKENHI Grant Numbers 24770068 and 15K07152. Introduction Aminoacyl-tRNA synthetases (aaRSs) help maintain the genetic code by recognizing their cognate
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