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At the end of experiments rats
2022-05-27

At the end of experiments rats were injected high dose of sodium pentobarbital (90mg/kg) and the rat’s head was cut and frozen in −20°C for 20min with the injecting tube in situ before section. The location of the tip of the injecting tube was verified and all the tips of the injecting tube were in
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Cys loop GABA receptors are well studied
2022-05-27

Cys-loop GABA receptors are well-studied targets for insecticides and also play an important role in nematode biology. These receptors are also targets for the anthelmintic piperizine (Accardi et al., 2012). The nematode GABA receptor most studied is the UNC-49 receptor which plays a role in muscle
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According to Laplace s law loss of
2022-05-27

According to Laplace’s law, loss of myogenic response would increase wall stress and tension in downstream vessels and subsequently induce endothelial dysfunction and arterial stiffness [36]. Indeed, we found that arteries from FPR-1 KO mice presented with a leftward shift in the stress-strain curve
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Based on this evidence future research
2022-05-27

Based on this evidence, future research should be directed towards the identification of actual receptor oligomeric states at the analyzed cellular surfaces. The macromolecular organization of these oligomeric receptors might establish informational hubs, which relay ligand/receptor interactions in
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First identified in as the second mammalian glutathione pero
2022-05-27

First identified in 1982 as the second mammalian glutathione peroxidase [23], we and Stockwell's group demonstrated in 2014 that the selenoperoxidase GPX4 is the key upstream regulator of ferroptosis [12], [13]. The role of GPX4 as the main regulator in the ferroptotic process is based on its unique
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The regulatory effects of NADPH oxidase on
2022-05-27

The regulatory effects of NADPH oxidase on ferroptosis might also relate to neuroinflammation. Although ferroptosis can trigger inflammatory responses in the brain, neuroinflammation, in turn, can also modify ferroptosis. It has been reported that inflammatory conditions such as those found in neuro
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The physicochemical properties of the
2022-05-27

The physicochemical properties of the prodrugs provided important clues for understanding a broad range of inhibitory activities in the cell assays (Table 2). Some physicochemical properties are useful in predicting drug absorption. Considering Lipinski’s rules and the polar surface area (PSA),l-ala
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Several classes of small molecule inhibitors of
2022-05-27

Several TNF-alpha, recombinant murine protein of small-molecule inhibitors of FBPase have been reported. These inhibitors can be structurally classified into two groups; non-phosphorus-based inhibitors and phosphorus-based inhibitors. In the former group, several chemotypes including anilinoquinazol
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Sumoylation is involved in regulating protein
2022-05-27

Sumoylation is involved in regulating protein-protein interactions, subcellular protein localization, protein stability, and transcriptional factor activity (reviewed in [29]). The small ubiquitin-like modifier (SUMO) protein is covalently attached to a lysine residue in a Ψ-K-X-D/E consensus sequen
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br Experimental procedures br Results br Discussion This
2022-05-27

Experimental procedures Results Discussion This study demonstrates that the genetic disruption or pharmacological inhibition of FAAH completely prevented all manifestations of pain symptoms in an NTG-induced migraine animal model. Thus, FAAH disruption or blockade abolished the activation o
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In patients with breast cancer ZRANB
2022-05-27

In patients with breast cancer, ZRANB1 gene amplification was found in a subset of cases, and ZRANB1 protein levels correlated with EZH2 protein levels and poor survival (both TNBC and non-TNBC). Moreover, unlike normal mammary epithelial cells, all human breast cancer cell lines examined (both TNBC
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Tyr phosphorylation of AnxA was first reported to be involve
2022-05-27

Tyr23 phosphorylation of AnxA2 was first reported to be involved in endocytosis, particularly in the internalisation of the insulin receptor [20]. Phosphorylated Tyr23 seems to be necessary for the stable association of AnxA2 with endosomes, and for their early-stage transport [14]. The role of AnxA
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We have expanded these studies by doing EEG
2022-05-27

We have expanded these studies by doing EEG recording in the ET-1 model. Using this technique, we demonstrated that activation of either the ETA NSC23766 or the ETB receptor induces electrical seizures. ET-1 induced electrical seizures occurred in the presence of either the ETA receptor antagonist o
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Classical drugs target the viral
2022-05-27

Classical drugs target the viral Tivozanib reverse transcriptase (RT), protease and integrase (IN) [[4], [5], [6]]. Raltegravir (ISENTRESS/MK-0518) is the prototypical integrase strand transfer inhibitor (INSTI) leading to an extremely strong reduction in viral load [7] and it has been approved for
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Multi targeting agents are of major
2022-05-27

Multi-targeting agents are of major interest in modern drug design and discovery. Design of such compounds can be applied to H3R antagonists for the purpose of achieving optimum efficiency as performed for some preclinical candidates such as recently for contilisant (Bautista-Aguilera et al., 2017;
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