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The presence of different LO splice
2023-12-26
The presence of different 5-LO splice variants was first demonstrated in human PD 123319 ditrifluoroacetate tumour cells and in dimethyl sulfoxide-differentiated HL-60 cells [40] and a correlation between the 5-LO splicing pattern and the malignancy of the brain tumours was found. Later, other spli
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NLX a k a F or befiradol exhibits
2023-12-26
NLX-112 (a.k.a. F13640 or befiradol), exhibits nanomolar affinity at 5-HT1A receptors, and, in MK-4827 Racemate to the 5-HT1A receptor agonists listed above, it presents exceptional selectivity and high efficacy at these receptors (Colpaert et al., 2002, Newman-Tancredi et al., 2017). Additionally,
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The syntheses of a and b are shown in
2023-12-26
The syntheses of 27a and 27b are shown in Scheme 5. Substituted naphthalene 21c was brominated using N-bromosuccinimide (NBS) and 2,2′-azobis(2-methylpropionitrile) (AIBN) to yield 25, which was subjected to lactam cyclization to form 26a and 26b, respectively. Deprotections of each Bedaquiline synt
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Most of lipid lowering agents have many therapeutic problems
2023-12-26
Most of lipid-lowering agents have many therapeutic problems with severe side effects, while dietary fibers as lipid lowering therapy are safer. Chitosan (CS) is a dietary fiber biodegradable, biocompatible and has many health benefits including wound healing, antiinflammatory, anti-cancers, immune-
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Wound healing without blastema formation causes
2023-12-26
Wound healing without blastema formation causes partial restoration of lost tissue, and gives rise to fibrotic scars. Healing by fibrotic scarring rather than by regeneration leads to tissue dysfunction, and can place a huge burden for the health of the animal [4]. Therefore, understanding the molec
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The regulation of gene expression by
2023-12-26
The regulation of gene expression by glucocorticoids can be mediated either by the canonical mechanism that involves the interaction of the glucocorticoid receptor (GR), a transcription factor activated by the hormone, with glucocorticoid response element (Ye et al., 2007), or by the non-canonical m
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AMP activated protein kinase AMPK is a key cellular energy
2023-12-26
AMP-activated protein kinase (AMPK) is a key cellular energy sensor that maintains energy homeostasis at the cellular and whole-organism level (Hardie et al., 2012). Functionally, the AMPK pathway sustains adenosine triphosphate (ATP) production through activation of fatty MP-470 oxidation and auto
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For patients who have taken advantage of the anti
2023-12-25
For patients who have taken advantage of the anti-TKIs and whose follow-up has been succeeded, some partial response has been noticed with 45% (9/20) for gefitinib, 39% (9/23) for erlotinib and 56.5% (13/23) for crizotinib. A disease progression has also been observed with 35% (7/20) for gefitinib,
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As noted earlier the PfkB
2023-12-25
As noted earlier, the PfkB family of carbohydrate kinases can phosphorylate the hydroxymethyl group of a wide variety of sugar moieties [1], [3]. Recent searches of the Swiss-Prot database with the two conserved sequence motifs found in these proteins (Accession nos. PS00583 and PS00584) identified
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UNC 0631 Sperm total motility and hyperactivated motility ar
2023-12-25
Sperm total motility and hyperactivated motility are mediated by PLD-dependent UNC 0631 polymerization [20]. Reduction of PIP2 synthesis inhibited actin polymerization and motility, and increasing PIP2 synthesis enhanced these activities. Furthermore, sperm demonstrating low motility contained low
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Previous reports indicate that the expression of
2023-12-25
Previous reports indicate that the expression of AChRs and their clustering on myotubes are critical factors required to induce contacts on muscle fibers in a natural biological system [14], [15], [16], [17], [18], [19]. For instance, in NMJ development in the mouse, AChRs are pre-patterned at sites
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Anti LT therapy by LO
2023-12-25
Anti-LT therapy by 5-LO inhibition has been hampered by occurring liver toxicities by Zileuton or the clinical phase II compound Atreleuton [36], [37] However both compounds possess a thiophene as well as an N-hydroxyurea moiety. These features could be linked with reactive thiophene intermediates [
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The gene SRD A encodes the reductase enzyme which converts
2023-12-25
The gene SRD5A2 encodes the 5-α-reductase enzyme, which converts testosterone into dihydrotestosterone. Although dihydrotestosterone levels are considerably lower than testosterone, dihydrotestosterone has a five-fold stronger binding capacity to the androgen receptor and, thereby, a considerably mo
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All scientific data over the years
2023-12-25
All scientific data over the years points that 5α-reductase inhibitors undoubtedly are an effective treatment for BPH and associated LUTS, having a favorable risk-benefit profile. In contrast, although some studies indicated positive results, there is still no consensus about their use in BPH or PC
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br ATX LPA pathway in animal models of rheumatoid arthritis
2023-12-25
ATX–LPA pathway in animal models of rheumatoid arthritis Several animal models have been used to characterize the mechanisms involved in the pathogenesis of arthritis and to test new therapeutic strategies. The collagen-induced arthritis (CIA) model (Courtenay et al., 1980, Luross and Williams, 2
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