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Given the powerful and ubiquitous
2024-07-19
Given the powerful and ubiquitous nature of adenosine action within the CNS, basal levels of extracellular adenosine are carefully regulated and are estimated to be in the region of 30–300 nM (Fredholm et al., 2001). The two main pathways for the control of extracellular adenosine involve phosphoryl
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We have expressed the ECDs of the human and
2024-07-19
We have expressed the ECDs of the human α1, β1, γ and ɛ AChR subunits in the past using the methylotropic yeast Pichia pastoris as soluble glycosylated proteins [15], [16]. Further work with the γ subunit ECD revealed a marked improvement of the solubility and yield following the mutation of hydroph
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The first suggestions that the
2024-07-19
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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In an insightful essay Heryanto writes that language is a
2024-07-19
In an insightful essay, Heryanto (1990, 40) writes that language is “a phenomenon expressing the particular history of a society” that did not exist in many parts of the world. “Language is not a universal category or cultural activity. Though it may sound odd, not all people have a language in the
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tranylcypromine br Free entry equilibrium At stage of
2024-07-19
Free entry equilibrium At stage 2 of the game, n ≥ 2 firms simultaneously decide whether or not to enter the industry. Market entry involves a sunk fixed cost f > 0, which we assume cannot be subtracted from the tax base. Our assumption reflects that deductions of market entry costs are often inc
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Finasteride has been shown to be a
2024-07-19
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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In this paper we describe the formation
2024-07-19
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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Aurora A or B selective and pan aurora inhibitors have
2024-07-19
Aurora -A or -B selective and pan-aurora inhibitors have demonstrated different preclinical and clinical therapeutic efficacies [2,[19], [20], [21], [22], [23]]. For example, clinical trials for a pan-Aurora inhibitor VX-680 (developed by Vertex) were halted at phase II for toxicity reasons (one cas
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Calcineurin has been established to be a ubiquitous Ca activ
2024-07-19
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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The proinflammatory cytokines and chemokines including IL TN
2024-07-18
The proinflammatory cytokines and chemokines, including IL-1β, TNF-α and MCP-1, mediate acute and chronic inflammation and play a role in the development of hypertension [2, [51], [52], [53]], cardiovascular diseases [4, 54] and renal injury [55, 56] in animal models and humans. Concerning the possi
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The association of male gender
2024-07-18
The association of male gender with increased atherosclerosis has stimulated interest in the role of androgen signalling in this condition. Androgens act (Fig. 2) by direct activation of androgen receptor (AR), a nuclear receptor that acts as a ligand-regulated transcription factor (Gao et al., 2005
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The expanding catalog of glutamate receptor auxiliary subuni
2024-07-18
The expanding catalog of glutamate receptor auxiliary subunits and associated transmembrane proteins underscores the importance and complexity of the receptor complexes. Whereas the interactions described here specifically control AMPARs, distinct auxiliary subunits, Neto-1/2, modulate neuronal kain
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br Serine glycine and one carbon metabolism Altered serine
2024-07-18
Serine/glycine and one-carbon metabolism Altered serine metabolism in tumors was noted nearly half a century ago, and elevated flux through the de novo serine synthesis pathway (SSP) is a common phenomenon in cancer Tanshinone IIA---sulfonic sodium [43]. The SSP branches from glycolysis at the po
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Several enzymes in serine and
2024-07-18
Several enzymes in serine and glycine metabolism have been proposed as biomarkers for cancer stage and prognosis. Phosphoglycerate dehydrogenase (PHGDH), phosphoserine phosphatase (PSPH), and serine hydroxymethyltransferase (SHMT) levels are high in TNBC and low in luminal-A breast cancers (Kim et a
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In our previous study adiponectin system genes
2024-07-18
In our previous study, adiponectin system (genes and proteins) expression in the porcine endometrium and myometrium was observed on Days 2 to 3, 10 to 12, 14 to 16, and 17 to 19 of the estrous cycle [23]. Adiponectin receptors expression (mRNA) in the porcine endometrium was described by Lord et al.
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