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br Acknowledgement This work was supported by National Scien
2021-12-27

Acknowledgement This work was supported by National Science Foundation (21475047, 21705051, 21874048), the Science and Technology Planning Project of Guangdong Province (2016B030303010), the Program for the Top Young Innovative Talents of Guangdong Province (2016TQ03N305) and the Foundation for H
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To efficiently develop bioactive ligands even if the
2021-12-27

To efficiently develop bioactive ligands even if the structural information of the target protein is unknown, we have presented a three-dimensional structural diversity-oriented strategy based on structural properties of a chiral cyclopropane. Our strategy has allowed us to design and synthesize a s
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Apoptosis is one of critical toxic
2021-12-27

Apoptosis is one of critical toxic mechanisms of benzene metabolites. In this work, overexpression of HIF-1a could significantly reduce the increase in cell apoptosis caused by 40 μM BQ. At the meanwhile, anti-apoptotic protein Bcl-2 level was significantly elevated in HIF-1a overexpression cells th
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VDAC interacts with hexokinase and is implicated
2021-12-27

VDAC interacts with hexokinase and is implicated in NLRP3 activation in response to noxious stimuli including monosodium urate, silica, and alum (Zhou et al., 2011). Hexokinase dissociation may allow VDAC to carry out this role. It will be informative to block or silence VDAC to explore its function
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Nevertheless the frequency of CTCs was
2021-12-27

Nevertheless, the frequency of CTCs was higher in patients with metastatic breast cancer, which is to be expected because cancer DL-Menthol from the original clone that caused the metastasis probably had features favoring their spread throughout the body. When we take HER2+ CTC counts ≥ 3 as a “str
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Lastly certain populations of immune cells may
2021-12-27

Lastly, certain populations of immune cells may be Hh responsive. Although PC have not been demonstrated in healthy liver-resident macrophages or lymphocytes, macrophages in injured livers have been shown to produce Hh ligands[58], [100], [101] and treating liver-derived macrophages with neutralisin
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The rat model was validated with another agonist
2021-12-27

The rat model was validated with another agonist of GPR109A, acipimox. Acipimox has been shown to induce vasodilatation in man, by a mechanism dependent on the release of vasodilator prostaglandins (Edlund et al., 1990, Pontiroli et al., 1992). Acipimox is a weaker agonist of the GPR109A receptor (L
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Because HIV does not infect neurons the neurotoxicity
2021-12-27

Because HIV does not infect neurons, the neurotoxicity in HAND is thought to result from the neuroinflammation evoked by the release of viral proteins and cytokines from infected microglia and macrophages (Ellis et al., 2007; Saylor et al., 2016). Viral tropism is determined by gp120 binding to CD4
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To shed more light on the binding of
2021-12-27

To shed more light on the binding of benzophenanthridine to GlyT1, we studied how the replacement of certain residues around the sanguinarine sensitive cysteine 475 previously identified (Jursky et al., 2012) affects GlyT1 inhibition of by these alkaloids. Based on these results we propose a putativ
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Previous studies have shown that zinc interacts with
2021-12-27

Previous studies have shown that zinc interacts with other allosteric modulators at the glycine receptor (Kirson et al., 2013, McCracken et al., 2010, McCracken et al., 2013). Of note, the chelation of zinc via tricine decreases the effects of alcohol at α1-, α2-, and α3-containing glycine receptors
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There were significant differences in
2021-12-27

There were significant differences in mRNA expression levels observed for 7 out of 15 analyzed genes. This observation suggests, that selection of a reference/control group may influence interpretation of gene expression studies performed in liver pathologies. This study directly evidenced that anal
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Transcriptional translational modulators The discovery that
2021-12-27

Transcriptional/translational modulators. The discovery that β-lactam antibiotics like ceftriaxone enhance the in vivo expression of EAAT2/GLT-1 [31] has pioneered a completely new approach to EAAT modulation, with several additional EAAT activators following in its trail (Figure 2b) [32, 33, 34•, 3
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br Ligand binding free energies In order to compute
2021-12-27

Ligand-binding free energies In order to compute the absolute free Vatalanib associated with binding a ligand to a flexible iGluR LBD, a theory that accounts for all the principal thermodynamic contributions from ligand docking and LBD closure had to be developed. This was accomplished using an
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5-alpha reductase inhibitors To confirm that these were bona
2021-12-27

To confirm that these were bona fide interactions, we investigated whether the potassium channel subunits or Tmem263 formed complexes with GLT-1 or DAT after immunoprecipitation. Lysates of HEK-293 cells previously cotransfected with HA-GLT-1 or HA-DAT, and either YFP-Kv7.3, YFP-Kv7.2 or YFP-Kv7.5 w
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Transmembrane AMPA receptor regulatory proteins TARPs
2021-12-27

Transmembrane AMPA receptor regulatory proteins (TARPs) are a relatively newly discovered protein family. Prototypic TARP, stargazin, was found by a spontaneous mutation in ataxic stargazer mouse line as a homologous protein to γ1 calcium channel subunit (Letts et al., 1998). The role of stargazin i
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