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To evaluate the ability of both sets of compounds
2024-03-21
To evaluate the ability of both sets of compounds to inhibit the activity of 15-LOX an initial screen was performed, whose results are shown in . The comparison of inhibition values would seem to indicate that, in the HYD series, an electron donor group at the position increases and an electron att
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As previously mentioned when hypoxia treated cells become re
2024-03-21
As previously mentioned when hypoxia-treated cells become re-oxygenated they sustain a significant amount of DNA damage which has been attributed to the formation of reactive oxygen species . This finding represents more than just an interesting in vitro phenomenon as within a tumor, cells have been
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The amino hydroxy methyl isoxazolepropionic acid AMPA recept
2024-03-21
The α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic 4112 (AMPA) receptor is also enriched in postsynaptic striatal neurons (Bernard et al., 1997, Kondo et al., 2000, Reimers et al., 2011). Its activity is subjected to the regulation by a mechanism involving phosphorylation (Lu and Roche, 2012). For
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LOXs and CYPs are a series of
2024-03-20
LOXs and CYPs are a series of iron-containing enzymes that metabolize arachidonic raf inhibitors to form biologically active products, such as epoxyeicosatrienoic acids (EETs) hydroperoxyeicosatetraenoic acids (HETEs), prostaglandins, leukotrienes and thromboxanes [6]. Among these mediators, 12/15LO
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We also investigated the transmittance of
2024-03-20
We also investigated the transmittance of actin polymerized with and without ABP. The presence of actin in the solution results in an increment in turbidity as other proteins provided jnk inhibitor synthesis features [21], [32]. While G-actin showed a transmittance peak positioned at 241 nm, F-acti
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Serum soluble sCD is a shedding product from
2024-03-20
Serum soluble sCD21 is a shedding product from the ectodomain of membrane CD21 after B cell activation (Masilamani et al., 2003, Masilamani et al., 2004a, Masilamani et al., 2004b, Grottenthaler et al., 2006, Hoefer et al., 2008), which resembles the ligand-binding capacity of intact CD21 (Wu et al.
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In the previous study we demonstrated
2024-03-20
In the previous study, we demonstrated the importance of the mPFC postsynaptic 5-HT1A receptor in the sustained antidepressant effects, because a sustained antidepressant effect was obtained with intra-mPFC injection, but not systemic injection of 8-OH-DPAT, a 5-HT1A receptor agonist (Fukumoto et al
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However although in vitro studies
2024-03-18
However, although in vitro studies in heterologous systems have provided very important indications of potential novel pharmacology, the studies with endogenous receptors in native tissues are essential to provide evidence for GPCR heteromerization in vivo and to confirm its physiological relevance.
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br Introduction Nausea and vomiting are among the most
2024-03-18
Introduction Nausea and vomiting are among the most distressing side effects associated with chemotherapy in cancer patients (Billio et al., 2010). Severe emesis can negatively affect a patient's nutritional state, ability to work and motivation, which can, in turn, interfere with the clinical co
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br Acknowledgements We thank Dr Stefan Schulte Merker and
2024-03-18
Acknowledgements We thank Dr. Stefan Schulte-Merker and his group members at the Hubrecht Institute (Utrecht, the Netherlands) for their invaluable support of the zebrafish studies. Our work is supported by grants from the Dutch Cancer Society (KWF) and the Netherlands Organisation for Scientific
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Having taken a step back from affinity
2024-03-18
Having taken a step back from affinity to gain better exposure and solubility, we started work to replace the unstable oxazolinone, and address the selectivity over the hERG channel. Keeping in mind the binding mode of the series from crystal structures, triazole was identified as another mildly aci
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Investigating these possibilities will illuminate whether ce
2024-03-18
Investigating these possibilities will illuminate whether QX 314 bromide possess mechanisms to differentially detect ACLY-generated versus ACSS2-generated acetyl-CoA as well as define the functional relationship between histone acetylation levels and cellular functions and phenotypes. Given that AC
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Because ASK signaling in microglia and astrocytes is importa
2024-03-18
Because ASK1 signaling in microglia and astrocytes is important during EAE, we hypothesized that a combination therapy that targets T cells along with microglia and astrocytes would further ameliorate the severity of EAE. We tested this hypothesis by applying valproic NPI-0052 (VPA)—a short-chain f
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Knowledge about adipose tissue has evolved considerably over
2024-03-18
Knowledge about adipose tissue has evolved considerably over the last two decades. Always been described as an inert tissue having the function of stocking lipids, adipose tissue is now recognized as a real organ with both metabolic and endocrine functions secreting various factors into the blood to
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Thiol are reduced by two major redox systems glutathione
2024-03-18
Thiol are reduced by two major redox systems, glutathione/glutaredoxin (GRX) and thioredoxin (TRX), which have been extensively studied in plants [13], [14], [15]. Glutathione, a thiol-containing tripeptide, exists in a reduced (GSH) or an oxidized form (GSSG). It has a major role as a redox buffer.
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