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One of the possibilities of HO targeting
2021-09-30

One of the possibilities of HO-1 targeting is gene therapy. So far, the majority of preclinical studies have focused on recombinant adeno-associated viral (rAAV) vectors as DNA carriers. They not only provide stable, long-term transgene expression in non-dividing NU 1025 but also have very limited i
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GPR belongs to the G protein coupled receptor family and
2021-09-30

GPR84 belongs to the G protein-coupled receptor family, and it was first identified from human peripheral blood neutrophils [,]. GPR84 is now considered to be a member of receptor for medium chain fatty SB431542 (MCFA) with carbon chain lengths of 9–14 []. GPR84 is mainly expressed in bone marrow,
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The difference in the expression of
2021-09-30

The difference in the expression of functional FFARs between neutrophils and monocytes/macrophages suggests that the role of FFA2R may be restricted to the very early phase of acute inflammation where neutrophils are dominating players called into action, whereas GPR84 may have a broader functional
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In both families GPR A mRNA in kidney fat
2021-09-30

In both families, GPR109A mRNA in kidney fat was positively correlated with NEFA as a tendency. A positive correlation between this fat depot and insulin was observed in lean-type cows. In fat-type cows, mesenteric GPR109A mRNA correlated positively with insulin and negatively with urea on a moderat
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Lamina II SG spinal cord neurons play an important role
2021-09-30

Lamina II (SG) spinal cord neurons play an important role in regulating nociceptive input from the periphery [20,21]. Moreover, lamina II neurons are concentrated with glycinergic or GABAergic inhibitory interneurons. Therefore, it is possible that β-alanine might modulate nociceptive transmission i
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br Discussion Our results indicate that marked changes in
2021-09-30

Discussion Our results indicate that marked changes in the relative distribution of AMPA receptors in microsomal and synaptic fractions occur during the postnatal period, and that these changes are correlated with changes in different populations of AMPA binding sites. At early postnatal ages (PN
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br Materials and methods br Results
2021-09-30

Materials and methods Results Discussion The global pandemic of T2DM has mandated a search for new types of therapeutic agent and several long-acting analogs of naturally occurring incretins, particularly derivatives of GLP-1, have already been adopted in clinical practice [29]. This study
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AD is an irreversible and progressive neurodegenerative dise
2021-09-30

AD is an irreversible and progressive neurodegenerative disease affecting the WIN 64338 hydrochloride which insidiously destroys memory, thinking skills and cognition. Originally described in 1906 by German physician Alois Alzheimer, AD is characterized by the presence of intraneuronal neurofibrill
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A way to identify what
2021-09-30

A way to identify what subunit interfaces contribute to the pharmacology of agents is to utilise binary GABAARs as tool receptors to ascertain possible binding sites for particular ligands. These receptors can help identify subunits and subunit interfaces that contribute to receptor pharmacology. In
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Since our new compound Fex could be a
2021-09-29

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 Digoxigenin-11-dUTP mg with transwell experiments.
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With the identification of small nonpolar substituents
2021-09-29

With the identification of small nonpolar substituents at R3 of the phenylpropanoic acid ring providing improved activity at FFA4, exploration of the benzyl SAR was undertaken (). Small substituents were well tolerated at both the and positions (–) with the 2-bromo- (), 2-isopropoxy- (), and 3-met
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The canonical tumor suppressor p has
2021-09-29

The canonical tumor suppressor p53 has also been implicated as a transcriptional mediator of ferroptotic death (Jiang et al., 2015, Tarangelo et al., 2018, Wang et al., 2016, Xie et al., 2017). Specifically, p53 negatively regulates transcription of SLC7A11, the cystine-glutamate antiporter (Xc-) (J
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CTGF is an established YAP TAZ target gene
2021-09-29

CTGF is an established YAP/TAZ target gene which plays a central role in tissue remodeling. Downregulation of CTGF mediates collagen loss in chronologically-aged human skin whereas persistent activation of CTGF can result in excessive deposition of collagen and fibrotic disorders [63]. The authors f
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Several recent studies have linked clock
2021-09-29

Several recent studies have linked clock function with the cell cycle and reported that clock components, such as PER1, PER2, BMAL1, and CRY1/2 decrease cell proliferation or improve the action of anti-cancer drugs in different cancer cell lines. Moreover, certain types of human cancer show an alter
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In an effort to further improve the intrinsic potency we
2021-09-29

In an effort to further improve the intrinsic potency, we evaluated the effect of the C4-substituent of the triazole (). Replacement of the phenyl group with a cyclohexyl or with a 2-pyridyl substituent led to losses in potency. Increasing the size of the substituent to a bi-phenyl or naphthyl group
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