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No specific inhibitor of KCC has progressed
2022-01-29
No specific inhibitor of KCC has progressed to clinical trials, however, although compounds like H74 were shown to specifically target KCC over the related Na+-K+-2Cl− cotransporter (NKCC) (Ellory et al., 1990). This molecule, or its related analogues, represent compounds of promise. Simple Mg suppl
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With rare exceptions the biological
2022-01-29
With rare exceptions, the biological role of γ-secretase cleavage of substrates other than Notch 1 has been ignored during proof of concept preclinical repurposing studies. For example, in the GSI AD trial, many individuals noted changes in hair color, apparently due to inhibition of tyrosinase, ano
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By association a possible mechanism which
2022-01-29
By association, a possible mechanism which may underlie the progression of seizures is long-term potentiation (LTP). Indeed, LTP shares many common mechanisms with seizures activity both anatomically and physiologically, and has been implicated as a mechanism of acute epileptogenesis (Wasterlain et
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The typical pharmacophore for GPR agonists contains four par
2022-01-28
The typical pharmacophore for GPR40 agonists contains four parts: head (acid moiety), central (phenyl ring), linker and tail (aromatic carbocyclic or heterocyclic ring) [20]. On the other hand, the chemical features that are required for the PPARγ agonists include hydrogen bond donors and acceptors
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LMWHs are currently recommended for
2022-01-28
LMWHs are currently recommended for the treatment of VTE in patients with cancer. Compared to vitamin K antagonists, LMWHs are more effective in reducing the risk of recurrent VTE without increasing the risk of bleeding [13]. However, a post hoc analysis of this Calcitriol previous study showed no
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Obesity may be associated with
2022-01-28
Obesity may be associated with allergic diseases (including atopy, asthma, and allergic rhinitis) in children.9, 10, 11 Furthermore, body mass index (BMI) may be associated with bronchial hyper-responsiveness.9, 12 Nevertheless, the relationship between histamine skin reactivity and BMI is poorly un
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Hypoxia HIF and Inflammation Cellular responses to hypoxia a
2022-01-28
Hypoxia, HIF, and Inflammation Cellular responses to hypoxia are essential for life and are now recognized to be dysregulated in a wide range of disease processes. The key players in these pathways are a family of transcription factors, the hypoxia-inducible factors (HIFs; see Glossary), as well as
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Introduction Heme is an important small
2022-01-28
Introduction Heme is an important small molecule and an essential cofactor for a variety of enzymes (George, 1948; Morrison and Stotz, 1954; Maehly, 1952; Igo et al., 1961). During cellular respiration, heme populates cytochromes and serves as an electron acceptor in the electron transport chain (M
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However HDACi can also increase the
2022-01-28
However, HDACi can also increase the acetylation of other transcription factors that regulate p65 transcriptional activity. The HDACi-induced activation of p65 can be negated by acetylated STAT1, which can specifically bind to p65 and inhibit its transcriptional activity 81, 82, 83. Interestingly, a
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br Conclusion The following is the supplementary data relate
2022-01-28
Conclusion The following is the supplementary data related to this article. Conflict of interest Author contributions Heart transplantation is the most important treatment for end-stage heart failure. Ischemia/reperfusion injury is a common condition during transplantation surgery and is
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Previous studies have shown that zinc interacts with other a
2022-01-28
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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The neuronal glycine receptor HSOR
2022-01-28
The neuronal glycine receptor/3α-HSOR/allopregnanolone pathway may also be extended to the central nervous effects of gelsemine and koumine in brain. 3α-HSOR is expressed in certain brain regions in rats and humans, such as the limbic system including hypothalamus, hippocampus and amygdala, in addit
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Shikonin represents naphtoquinonic compound isolated
2022-01-28
Shikonin represents naphtoquinonic compound isolated from the Chinese plant Lithospermum erythrorhizon[20]. Shikonin treatment inhibits AKT and ERK signaling pathways and induces apoptosis through FOXO transcription factors and mitochondrial pathway [21], [22]. Recent results suggest inhibition of l
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FPR family Human FPR was first defined biochemically in as
2022-01-27
FPR family Human FPR was first defined biochemically, in 1976, as a high affinity binding site on the surface of neutrophils for the prototypic N-formyl peptide formyl-methionine-leucyl-phenylalanine (fMLF). It was then cloned in 1990, by Boulay et al. from a differentiated HL-60 myeloid leukemia-c
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br Materials and methods All studies
2022-01-27
Materials and methods All studies were performed in 230–250g timed-pregnant Sprague Dawley rats (Harlan, Indianapolis, Indiana). Animals were housed in a temperature controlled room with a 12:12 light:dark cycle. All experimental procedures in this study were in accordance with the National Insti
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