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br Materials and methods br Results Bgal from Alteromonas sp
2022-01-19
Materials and methods Results Bgal from Alteromonas sp. ML117 had an open reading frame of 3126 bp encoding 1042 amino orphan receptor residues with a predicted mass of 120 kDa and a theoretical pI (isoelectric point) of 5.44. The recombinant Bgal contained a His tag, as well as other additio
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Interestingly transgenic mice that constitutively
2022-01-19
Interestingly, transgenic mice that constitutively express active FXR in the intestine (iVP16FXR) are protected from chemically-induced and genetically-induced cholestasis. This protective effect is attributed to the induction of intestinal FGF15 and repression of hepatic Cyp7a1 expression, downregu
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According to its major function as master
2022-01-19
According to its major function as master regulator of BA homeostasis, FXR has been shown to have a specific tissue distribution; it is expressed along the entire gastrointestinal tract with a peak in the liver and ileum, as well as in the kidney, and adrenal glands [30], [66], [135]. Low FXR expres
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br Results and discussion br Conclusion In the continued
2022-01-19
Results and discussion Conclusion In the continued SAR study of our previous heterocycle scaffolds represented by Riociguat 2, we focused especially on improving their drug-like physicochemical properties directed by lipophilicity, LE and LLE. After explored several heterocyclic scaffolds, the
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In summary the SAR of a series of phenylpropanoic acid
2022-01-19
In summary, the SAR of a series of phenylpropanoic acid-free fatty corticotropin-releasing factor receptor agonists is described which resulted in the identification of potent FFA4 agonists. The superior pharmacokinetic properties of compound led to its selection as an in vivo tool compound which af
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Whether ferroptosis specific inhibitor could promotes spinal
2022-01-19
Whether ferroptosis specific inhibitor could promotes spinal cord repair is a question worth to explore. A potent and stable ferroptosis specific inhibitor is essential for in vivo study. Ferrostatin-1 (Fer-1), the first generation of ferroptosis inhibitor, was shown actively suppressing ferroptosis
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The suboptimal trypsin selectivity profile
2022-01-19
The suboptimal trypsin selectivity profile of DPC423 prompted us to investigate additional P moieties for potency and selectivity. Glycinamide P () showed low nanomolar binding affinity against fXa which suggested that this P moiety sits deeper into the S pocket of fXa. To further elaborate on this
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jsh receptor Due to the importance of gene regulation in can
2022-01-18
Due to the importance of gene regulation in cancers, HDAC inhibitors have been studied extensively in cancer biology and are in current clinical use as anti-tumor therapies [17]. The HDAC inhibitors vorinostat, romidepsin, and belinostat have been approved for certain T-cell lymphomas, and panobinos
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To solve the atomic structures of several individual domains
2022-01-18
To solve the atomic structures of several individual domains and a complete molecular architecture of sGC, tangible experimental research work has been done which resulted in a cryo-electron density map of R. norvegicus. However, the full structure of the human sGC remains to be determined. In the p
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Acknowledgments br INTRODUCTION AND OBJECTIVES br
2022-01-18
Acknowledgments INTRODUCTION AND OBJECTIVES METHODS RESULTS CONCLUSIONS Introduction Class 3 alcohol dehydrogenase (EC 1.1.1.1), also known as ADH5 chi polypeptide in humans, was first identified by Koivusalo et al. [1] as a NAD+-dependent hydroxymethylglutathione (HMGSH) oxidase. By
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GPR levels were not changed by any
2022-01-18
GPR40 levels were not changed by any treatment. GPR40 has the same agonists as GPR120 but only a 10% homology [35] despite using the same intracellular signaling cascades [7]. Previous data on the ability of exercise to modulate G protein coupled receptors in general are scarce. The long-chain fatty
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Considering that loss of LAG expression results
2022-01-18
Considering that loss of LAG-3 69 8 results in increased CD4+ T cell homeostatic expansion, and that the ability of a cell to proliferate is tightly coupled to its metabolic profile, we hypothesized that LAG-3 regulates naive CD4+ T cell metabolism. Our results indicate that, indeed, Lag3-deficient
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Overall the multiple nucleic acid hybridization method is us
2022-01-18
Overall, the multiple nucleic INCB-024360 hybridization method is useful for detecting specific transcripts within tissues of nematodes. The present study suggests that Peq-pgp-11 and Peq-pgp-16 mRNAs are expressed in many tissues of Parascaris. Our results indicate that Pgps could protect nematode
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Previous studies have demonstrated that
2022-01-18
Previous studies have demonstrated that cannabinoid potentiation of GlyR α3 subunits contributes to cannabinoid-induced analgesia. For instance, Dehydroxylcannabidiol (DH-CBD), a chemically modified cannabinoid, can alleviate acute pain and chronic inflammatory pain by targeting spinal α3 GlyRs (Xio
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To examine the possible role of mGluRs in the LH
2022-01-18
To examine the possible role of mGluRs in the LH/PFA in the hypercapnic ventilatory response, a nonspecific antagonist of mGluRs, MCPG, was microinjected into the LH/PFA. MCPG elicited a significantly increased hypercapnic ventilatory response in awake rats, but not during sleep, in the light and da
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