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Acetylcholinesterase AChE activity and expression level can
2024-10-11

Acetylcholinesterase (AChE) activity and expression level can be down regulated by TCDD in neuronal cells [3], [6]. Thus AChE could be considered as a target of the neuronal toxicity of dioxin. AChE has several types of transcripts by alternative splicing in the 3′ region of primary transcripts [7],
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MLN8237 The first suggestions that the cleaved
2024-10-11

The first suggestions that the cleaved intracellular domain of APP, AICD, might transit to the nucleus and hence selectively regulate gene transcription arose from analogies with the Notch receptor signalling system where similar intra-membrane proteolysis occurs [84], [85] and it was later confirme
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Anti LT therapy by LO inhibition has
2024-10-11

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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Thalidomide MafB a member of the Maf protein family is
2024-10-11

MafB, a member of the Maf protein family, is essential for terminal differentiation of macrophages (Kelly et al., 2000). The phagocytic activity of polystyrene beads was found to be enhanced in Thalidomide with exogenous expression of MafB (Tillmanns et al., 2007). However, in alveolar macrophages
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Here we report discovery of highly selective
2024-10-11

Here we report discovery of highly selective pan-Aurora kinase inhibitors through phenotypic screening. The co-crystal structure of cpi-613 australia bound in the ATP binding site of Aurora A is described, and provides insight into the possible structural basis for the selectivity of the interacti
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Introduction Preeclampsia a serious hypertensive disorder th
2024-10-10

Introduction Preeclampsia, a serious hypertensive disorder that can occur during pregnancy, is a pregnancy-related disease characterized by the onset of perindopril erbumine synthesis and proteinuria after the 20 t h week of gestation, and it occurs in about 5% of all pregnancies [1]. If left untr
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Plasma apelin levels predict the major cardiovascular
2024-10-10

Plasma apelin levels predict the major cardiovascular event after percutaneous coronary intervention in patients with ST elevation myocardial infarction (STEMI), and adverse events are higher in patients with lower plasma apelin levels [75]. Apelin and its receptor are markedly upregulated in the he
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Detailed analysis of the dose
2024-10-10

Detailed analysis of the dose dependence of Aβ effects revealed that at low amounts, Aβ can also act as a positive regulator of presynaptic activity, enhancing the neurotransmitter release probability and increasing the neuronal excitability [2]. The facilitator effects of low Aβ dose on excitatory
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br Conclusion We have identified
2024-10-10

Conclusion We have identified three non-competitive inhibitors of the human and porcine APN with Ki values in the μM range, by combining virtual screening and kinetic assays. Molecular docking simulations suggest these novel inhibitors block APN activity by an alternative mechanism to Zn coordina
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br Role of OCT in histamine
2024-10-10

Role of OCT3 in histamine clearance Histamine is a powerful neuromodulator, as well as a regulator of immune processes and vascular tone in the central nervous system (Gross, 1981; Haas et al., 2008; Jutel et al., 2006). In contrast to 5-HT and the catecholamines, a high-affinity transporter for
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Plant material and growth conditions Arabidopsis thaliana ec
2024-10-09

Plant material and growth conditions. Arabidopsis thaliana ecotype Columbia was grown on a mixture of soil, vermiculite, and perlite (4:2:1) with a 16h light/8h dark tak tak in a temperature-controlled growth room (22°C), unless indicated otherwise. Molecular cloning and plant transformation. The c
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NSAIDs induce gastrointestinal toxicity and evoke asthma
2024-10-09

NSAIDs induce gastrointestinal toxicity and evoke aspirin solubility by decreasing the production of gastroprotective prostanoids and by redirecting the COX substrate AA into LT biosynthesis, thereby causing vasoconstriction in gastric mucosa and airways (Celotti and Laufer, 2001; Koeberle and Werz
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In fact serotonin is a major modulator of dopaminergic DA
2024-10-09

In fact, serotonin is a major modulator of dopaminergic (DA) neuronal activity through the 5-HT2C receptor. Studies have shown that the selective 5-HT2C receptor agonist Ro60-0175 blocks the burst-firing of mesolimbic DA neurons, which project from the ventral tegmental area (VTA) to the nucleus acc
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The class C receptors also share a common agonist
2024-10-09

The class C receptors also share a common agonist-binding mode. In all cases, an agonist induces VFT closure by forming intermolecular bonds with surface residues in both the LB1 and LB2 domains (Geng et al., 2013, Geng et al., 2016, Kunishima et al., 2000, Muto et al., 2007, Nuemket et al., 2017, T
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Calcineurin has been established to
2024-10-09

Calcineurin has been established to be a ubiquitous Ca2+-activated serine phosphatase in the nervous system (Pyrzynska et al., 2001). It has been reported that the activation of calcineurin protects aromatase from autophagy-mediated protein degradation, implying that calcineurin-dependent dephosphor
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