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LO is a soluble kDa enzyme composed
2023-08-28
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 intracell
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br Funding br Introduction The interest in the
2023-08-28
Funding Introduction The interest in the effects of endocrine disrupting chemicals (EDCs) in the aquatic environment continues to increase over the past decade, specifically those that act on steroidogenic pathways. EDCs that include synthetic androgenic and estrogenic compounds can severely
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Moreover showed reduction in fibroblast growth factor induce
2023-08-28
Moreover, showed 73% reduction in fibroblast growth factor–induced neovascularization in a mouse corneal micropocket assay at a dose of 100mg/kg and 50% reduction at 50mg/kg. Both results were highly statistically significant (Pprotoporphyrin ix have recently shown only moderate efficacy (40% inhibi
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Using our infection assays we also explored
2023-08-28
Using our infection assays, we also explored whether low-pH compartments were required for the entry of ZIKVs in mammalian cells. Lysosomotropic agents such as ammonium chloride, chloroquine and Bafilomycin A1, strongly inhibited the ability of ZIKVs to enter mammalian cells. Our results are in agre
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br Research perspective In vitro and in vivo studies have
2023-08-28
Research perspective In vitro and in vivo studies have demonstrated that increased LPA/ATX signaling contributes to cancer initiation and progression. Recent findings on the role of non-tumoral ATX in cancer progression and metastasis highlighted a new functional contribution for the microenviron
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Five alternatively spliced isoforms of ATX have been describ
2023-08-28
Five alternatively-spliced isoforms of ATX have been described and all are catalytically active [16], [17]. The original ATX described in 1992 is termed ATXα, whereas the most abundant isoform is ATXβ and is the same isoform responsible for plasma lysoPLD activity [18]. Full length ATX is synthesize
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br The future of cancer therapeutics with Aurora kinase inhi
2023-08-28
The future of cancer therapeutics with Aurora kinase inhibitors Involvement of Aurora kinases in deregulating multiple tumor suppressor and oncogenic pathways together with the preclinical findings on the efficacy of Aurora kinase inhibitors in attenuating growth of tumor mtor pathway suggests th
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Here we report discovery of highly selective pan
2023-08-28
Here we report discovery of highly selective pan-Aurora kinase inhibitors through phenotypic screening. The co-crystal structure of Ramelteon bound in the ATP binding site of Aurora A is described, and provides insight into the possible structural basis for the selectivity of the interaction. To
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br Introduction Hepatocellular carcinoma HCC
2023-08-28
Introduction Hepatocellular carcinoma (HCC) is the third-leading cause of cancer-related death worldwide and accounts for 70–85% of all liver cancer diagnoses [1]. In East and South-East Asia, the occurrence of HCC and the related number of fatalities have gradually increased in recent decades [2
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br Materials and methods br Results br Discussion We
2023-08-28
Materials and methods Results Discussion We have in this study used semi-nested degenerative PCR to identify the lipoxygenases expressed in the lung tissue from M. fascicularis and report on the identification of 5- and 12/15-LO transcripts from this tissue. Although we did not find transcr
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The fact that Yoda can activate
2023-08-28
The fact that Yoda1 can activate Piezo1 in the absence of other cellular components other than a cell membrane [2], suggests that it may directly interact with and activate Piezo1. However, this does not preclude Yoda1 from interacting and activating non-Piezo channels, particularly in endothelial c
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The only psychostimulant treatment option
2023-08-28
The only psychostimulant treatment option in Turkey is methylphenidate (Çetin et al., 2015). It is broken down by carboxylase enzyme (CES1) (Sun et al., 2004). From the point of pharmacokinetics, it may be suggested that CES1 gene polymorphisms may be the key responsible factors in patients resistan
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Despite these efforts to prevent oxidative metabolic degrada
2023-08-26
Despite these efforts to prevent oxidative metabolic degradation, and showed only marginal improvements in metabolic stability and still exhibited high plasma clearances as shown in . High molecular weight as well as relative high log values could be contributing factors to the poor PK profiles of a
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Finasteride has been shown to be a
2023-08-26
Finasteride has been shown to be a mechanism-based inhibitor of 5AR-2 [9]. Finasteride acts as an alternate substrate for 5AR-2 and is initially bound in an extremely stable enzyme-bound NADP-dihydrofinasteride adduct which is ultimately processed to dihydrofinasteride. The NADP-dihydrofinasteride a
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We have previously shown that the antinociceptive effect of
2023-08-26
We have previously shown that the antinociceptive effect of tramadol, an analgesic that, like paracetamol is able to increase serotonin levels within CNS, is potentiated or antagonized respectively by a 5-HT1A/B nonspecific CHIR-124 blockade or activation (Rojas-Corrales et al., 2000). Moreover, it
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