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GYKI 52466 dihydrochloride For the first series we decided t
2024-04-18
For the first series we decided to verify the effects induced, on the ALR2 inhibitory properties, of an additional steric hindrance on the carbon in α position with respect to the carboxylic group, by introducing a methyl group (R2=Me). Therefore, we synthesized a series of new α-alanine derivatives
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Blocking the action of CREB
2024-04-18
Blocking the action of CREB with the C646 inhibitor together with increasing Akt activation with the SC79 agonist is particularly interesting as it significantly reduced wound closure time from 7 days (which is required for complete closure of control hTECs exposed to DMSO) to only 4 days (when hTEC
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AdipoR and AdipoR have been reported to be present
2024-04-18
AdipoR1 and AdipoR2 have been reported to be present in almost all type of tissues and low TG4-155 levels have been observed in white adipose tissue (Inukai et al., 2005). These receptors have been observed to become deregulated with the onset of obesity, resulting in a reduced level of APN express
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Constitutive tyrosine kinase activity of
2024-04-18
Constitutive tyrosine kinase activity of BCR/ABL fusion genes causes uncontrolled cell growth and is also thought to be responsible for a variety of changes in normal cellular functions like differentiation, adhesion, migration and apoptotic response in CML. Therefore it is important to know the exp
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br Introduction Clinical manifestations of Alzheimer s disea
2024-04-18
Introduction Clinical manifestations of Alzheimer's disease (AD) are mainly characterized by progressive intellectual deterioration, memory impairment, cognitive impairment, and psychiatric symptoms. The pathogenesis of AD remains unclear, mainly containing genetic factors, neurotransmitter disor
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br Material and methods br Results br
2024-04-18
Material and methods Results Discussion Clinical gene therapy trials with viral vectors have been in use for treatment of various genetic disorders and diseases, however efficacious, targetable and highly reliable non-viral delivery systems are needed for safe and long-term applications. De
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br Materials and methods br Results
2024-04-18
Materials and methods Results Discussion The brain is endowed with the 5-LOX enzymatic system (Lammers et al., 1996, Lindgren et al., 1984), but its physiological and pathological roles are still not clear. Inflammation is a characteristic of many neurodegenerative diseases such as Alzheime
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The reaction of LOX with unlabeled AA generated products fro
2024-04-18
The reaction of 5-LOX with unlabeled AA generated products from hydrogen abstraction at C7 (95% 5-HETE) with minor products derived from abstraction at C10 (5% 8-HETE). With 7,7--AA the selectivity remained skewed towards C7 hydrogen abstraction (59%) compared to C10 hydrogen abstraction products (4
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LO is a soluble kDa
2024-04-18
5-LO is a soluble 78 kDa enzyme, composed of an α-helix-rich catalytic domain and a regulatory β-sheet-rich C2-like domain. Depending on the cell type, 5-LO may be located in the cytosol, in the nucleoplasm, or in both compartments (Werz, 2002). Upon cell stimulation by agents that elevate intracel
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The most potent compounds within
2024-04-18
The most potent compounds within the current series of compounds were therefore , , , , and , with 9-Phenanthrol possessing the best selectivity towards the lyase reaction in comparison to the hydroxylase reaction, indeed, this compound was found to possess an IC value of 1210nM against the 17α-O
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Curcumin br The embryological and physiological roles of ATX
2024-04-18
The embryological and physiological roles of ATX ATX is a vital enzyme that is needed for early embryological development. ATX knockout (KO) (ENPP2−/−) embryos die in utero on average at day 9.5 with vascular and neural tube defects [30], [73], [74], [75]. In these mice, malformations in the alla
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Because the V ATPase inhibitors that have been employed
2024-04-18
Because the V-ATPase inhibitors that have been employed in these studies (including bafilomycin and concanamycin), are membrane permeant, they inhibit all the V-ATPases in the cell. This is important since it is possible that intracellular V-ATPases, in addition to those present at the plasma membra
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Production of reactive oxygen species ROS
2024-04-17
Production of reactive oxygen species (ROS) during RSV infection is one the important ways that neutrophils can injure the lungs [2], [24], [25]. Lipoxygenases are considered as an important source of producing ROS inside the IMR-1 sale [26]. Several studies have indicated that the 12/15-LOX is a p
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Furthermore low affinity sites that share no
2024-04-17
Furthermore, low-affinity sites that share no structural homology with the aforementioned sites have been described in the transmembrane domain. It has been discovered that, in α1βγ2 receptors, potentiation of GABA-activated currents by high concentrations of diazepam is biphasic, with a high- and a
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To enhance the accuracy of SEs in eliminating cancer cells
2024-04-17
To enhance the accuracy of SEs in eliminating cancer cells, the mAb recognized by specific orthopoxvirus variola on tumor cells were fused with SEs. Fab C215 or C242 fused with SEA promoted apoptosis in human colon carcinoma cells via Fas (Dohlsten et al., 1994, Litton et al., 1996). SEB-incorporat
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