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It has been reported that HT R
2024-08-16
It has been reported that 5-HT2R involves in type 2 diabetes mellitus and 5-HT-induced IR [22,23]. The present study also demonstrated that it is 5-HT2R rather than other 5-HT receptors, including 5-HT1BR and 5-HT7R, in the liver that mediates HFD-induced abnormality of hepatic lipid metabolism, and
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Ro 08-2750 australia Several mechanisms have been suggested
2024-08-15
Several mechanisms have been suggested to account for the causal association of ICAM-1 induction and leukocyte adhesion with DR, including oxidative stress [16], NF-κB [17], PKC [18], and bioactive lipids [19]. Our previous studies highlighted the role of bioactive lipid metabolites derived from 12/
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Two critical determinants of receptor
2024-08-15
Two critical determinants of receptor trafficking are found within the GABAB1 cytoplasmic tail: the di-leucine internalization signal (EKSRLL) (Margeta-Mitrovic et al., 2000, Restituito et al., 2005) and the ER retention signal (RSRR) (Calver et al., 2001, Margeta-Mitrovic et al., 2000, Pagano et al
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Therefore the rational design of target compounds is
2024-08-15
Therefore, the rational design of target compounds is based on the hybrid of attractive phenotypic bis-indole (5, Fig. 1) and sulfonamide moieties, in which the indole core might anticipate in hydrophobic interaction, and the functionality of sulfonamide group may involve in H-bonding with the site
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Introduction Antimicrobial resistance is a growing health th
2024-08-15
Introduction Antimicrobial resistance is a growing health threat worldwide that has been associated with incorrect prescription and overuse of prostaglandin agonist synthesis [1]. Considering that physicians play a central role in antibiotic usage, a better understanding of their prescribing behav
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The electrokinetic remediation technique is carried
2024-08-15
The electrokinetic remediation technique is carried out with a low-level direct current, and the pollutants in soil can be transported and removed by the electric field [19]. This works well even in soil with low permeability via electro-osmotic flow and electro-migration [20]. The electrokinetic pr
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AMPK is a cellular energy sensor
2024-08-15
AMPK is a cellular energy sensor that is phosphorylated in response to high intracellular ADP levels to increase GLUT4 translocation into the cell, and subsequently, increase intracellular glucose levels to provide substrate to replenish ATP levels [25]. In metabolic syndrome, sequestration of plasm
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aphidicolin Based upon these findings the S
2024-08-15
Based upon these findings, the 12S-lipoxygenase seems to increase membrane excitability by specifically inhibiting M-type K+ channels. The 12S-lipoxygenase is expressed in many parts of mammalian aphidicolin including the cerebrum, cerebellum, hypothalamus, basal ganglia, hippocampus, olfactory bul
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Inflammatory factors released by activated cells during
2024-08-15
Inflammatory factors released by activated cells during AD are very important for the disease progression. Not only several inflammatory cytokines, such as IL-1β, IL-18, and IL-33, but also anti-inflammatory ones, as IL-10 and IL-13, are upregulated in the brain of AD patients (Morimoto et al., 2011
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In the presence of detrimental conditions such as inflammati
2024-08-14
In the presence of detrimental conditions, such as inflammation, hypoxia, ischemia trauma or neoplastic milieu, the extracellular levels of adenosine increase massively, reaching micromolar range [51,52]. In these pathological contexts, adenosine accumulation stems from increased extracellular depho
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fusidic acid The theoretical calculations of ADME
2024-08-14
The theoretical calculations of ADME parameters (molecular weight (MW), log P, topological polar surface are (tPSA), number of hydrogen donors (nON) and acceptors (nOHNH), and volume) and DLS are presented in along with the violations of Lipinski’s rule. According to these data, all compounds (–) c
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The first rationally designed dual mPGES
2024-08-14
The first rationally designed dual mPGES-1/5-LO inhibitor was reported in 2008 and represents a structural derivative of pirinixic Hexa His tag - a synthetic agonist of PPARα with lipid-lowering properties (Koeberle et al., 2008b). Further α-alkyl- and α-aryl-substituted derivatives have been synth
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br Materials and methods All animal experiments
2024-08-14
Materials and methods All animal experiments were performed using the recommendations of the Guide for the Care and Use of Laboratory Animals (National Research Council, 2011) and approved by the University of Colorado—Denver Institutional Animal Care and Use Committee. Adult male Sprague—Dawley
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atrial natriuretic peptide receptor In summary the role of
2024-08-14
In summary, the role of 5-HT and different types of 5-HTRs in gating plasticity induction in neocortical circuits remains unclear, with variable and seemingly contradictory effects reported for LTP induction in cortical sensory fields (e.g., V1, enhanced LTP: Inaba et al., 2009, Kojic et al., 1997,
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In this paper we describe the formation of
2024-08-14
In this paper, we describe the formation of a structure-based pharmacophore which lead to the discovery of several hydrophobic, yet non-lipid inhibitors of ATX. These compounds docked within the same volume occupied by the initial non-lipid inhibitors of ATX used to build the pharmacophore. Violatio
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