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To evaluate the ability of
2023-10-24

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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NOS is classified into three isoforms endothelial eNOS
2023-10-24

NOS is classified into three isoforms: endothelial (eNOS), neuronal (nNOS), and inducible (iNOS), iNOS is expressed in macrophages (Eisenstein, Huang, Meissler Jr, & al-Ramadi, 1994) and osteoblast-like cells (Riancho et al., 1995) and is involved in the regulation of inflammatory reactions (Eisenst
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To further investigate the role of cholesterol in
2023-10-24

To further investigate the role of cholesterol in the Rh2-induced cytotoxicity, we then focused on the U937 cell line, which is cholesterol auxotroph and considered as a valuable model to study the importance of cholesterol in membrane structure and function (Billheimer et al., 1987), and used the e
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Recent results suggest that TARPs are not the only
2023-10-24

Recent results suggest that TARPs are not the only auxiliary AMPAR subunits. Using a proteomic strategy (affinity purification of native AMPAR complexes followed by mass-spectrometric analysis), cornichon-related proteins (CNIHs) have been recently identified as components of the AMPAR protein micro
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There are some limitations and further experiments that are
2023-10-24

There are some limitations and further experiments that are required. First, to our surprise, measurement of the cardiomyocyte cross-sectional area in Akt1−/−/iAkt2 KO mice showed comparable areas to WT mouse despite of reduced heart weight. In addition to measuring cardiomyocyte cross-sectional are
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Extracellular ATP and downstream purinergic
2023-10-24

Extracellular ATP and downstream purinergic signaling have also been proposed to contribute to dental pulp tissue healing and dentin regeneration. Mechanical and thermal stimulation of external dentin can induce ATP release in dental pulp through pannexins [13]. Cold stimulation was also reported to
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As an alternative to chronic receptor
2023-10-24

As an alternative to chronic receptor blockade, we have been targeting adenosine kinase (ADK) – an astrocyte-based enzyme that catalyses the phosphorylation of adenosine, as a means to modify Bialaphos sodium salt adenosinergic signalling (Boison, 2006, Etherington et al., 2009). Up-regulating ADK
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br Acknowledgment br Introduction Vascular smooth muscle cel
2023-10-24

Acknowledgment Introduction Vascular smooth muscle cells (VSMC) exhibit the capacity to switch between a differentiated (contractile) and a dedifferentiated (synthetic) phenotype [1]. Synthetic VSMC express a lower amount of contractile proteins such as Smooth muscle 22α (sm22α) and α-Smooth m
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A rational approach for the design of
2023-10-23

A rational approach for the design of new steroid compounds as possible competitive inhibitors of CYP17 include chemical modification at C17 of the enzyme's natural substrates, pregnenolone (1) and progesterone (2), introducing groups with moderate to strong dipole properties at C20, such as oxime a
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IC values were obtained for an expanded version of the
2023-10-23

IC50 values were obtained for an expanded version of the fragment library using the previously described mobility shift assay. Subsequently, Ki values were estimated from IC50 values to allow better comparison of the activity against targets which were measured at different substrate concentrations
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As the effects of baclofen on primary afferent activity are
2023-10-23

As the effects of baclofen on primary afferent activity are not reproduced by GABAA receptor agonists like muscimol and isoguvacine, this ionotropic receptor may play minimal role in the modulation of primary afferent activity. However, it is important to note that post-synaptic GABAA receptors rema
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Protein microarrays represent just one of a variety of
2023-10-23

Protein microarrays represent just one of a variety of experimental approaches that can be used to generate datasets of relevance to pathway mapping. Other approaches include protein Calpain Inhibitor XII synthesis profiling techniques, such as antibody arrays [29], tissue arrays [30] and 2-dimensi
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To date LOX is the only LOX isoform
2023-10-23

To date, 12-LOX is the only LOX isoform that has been identified in the platelet [17]. Interestingly, while 12-LOX is highly expressed (∼14000 molecules/platelet) in the platelet, 12(R)-LOX expression is absent in the hematopoietic lineage and has therefore not been reported to be expressed in plate
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ITD 1 synthesis Introduction Lipoxygenases LOXs are key
2023-10-23

Introduction Lipoxygenases (LOXs) are key enzymes that catalyze the polyunsaturated fatty acids (PUFAs) such as arachidic ITD 1 synthesis (AA), linoleic acid (LA) and others unsaturated fatty acids (Brash, 1999). LOXs are expressed in immune, neural, epithelial, tumor cells and other cells (Claess
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Synthesis of the pterin carboxamides was achieved as shown i
2023-10-23

Synthesis of the pterin-7-carboxamides was achieved, as shown in , based on a previously reported method that utilizes DBU as a key additive to dissolve pterin in organic solvents and accelerate the reaction., With this method, the pterin-amino 9-Phenanthrol synthesis conjugates (–) were readily o
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