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Application of the broad acting HTR antagonist methiothepin
2022-12-01
Application of the broad-acting 5-HTR antagonist methiothepin (Bard et al., 1996, Hoyer et al., 1994, Peroutka, 1990) converted the TBS-induced response of both thalamocortical and intracortical A1 synapses from LTP to LTD, an effect that was mimicked by the selective 5-HT2R antagonist ketanserin (L
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br Autophagy in cancer br Phytochemicals as
2022-12-01
Autophagy in cancer Phytochemicals as a valuable source of autophagy modulation agents Epidemiological studies demonstrated that there is a strong association between diet and human cancer mortality so that daily consumption of phytochemicals declines the incidence of different types of cancer
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Zhang et al screened three thousand compounds library
2022-12-01
Zhang et al. screened three thousand compounds library and found two active 3,5,6-substituted indolin-2-one molecules. Further, they designed various derivatives of this scaffold and among them compound 23 from the series was found active with 1.8 μM on Aurora-B kinase luminescent assay [53]. Jeff
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Loss of expression or functional activity of cell
2022-12-01
Loss of expression or functional activity of cell adhesion is intricately related to advanced stages of tumour progression and invasiveness. Martin-Belmonte and Perez-Moreno recently mentioned that the deregulation of adhesion can alter tumourgenesis in the early stage. We have shown for the first t
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In this paper we described
2022-12-01
In this paper, we described synthesis, biological evaluation and docking study of 3-aroyl-1-(4-sulfamoylphenyl)thiourea derivatives 4a–o as 15-lipoxygenase inhibitors. Results and discussion Conclusion We designed and synthesized a novel of thiourea derivatives containing phenylsulfonamide mo
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We also showed that steatosis
2022-12-01
We also showed that steatosis induced an additional increase of ASK1 activation that was associated to the exacerbation of hepatocyte and liver damage and was unrelated to ER stress. Indeed, several settings, also different to ER stress, can induce ASK1 activation and many of them involve oxidative
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There is limited information regarding hyperargininemia inci
2022-12-01
There is limited information regarding hyperargininemia incidence or prevalence. Reports of incidence vary by an order of magnitude: 0.5 to 5.0 per million [5], [6]. A relatively large U.S. study estimated 1.1 cases per million births [7], but it used an indirect methodology that introduces uncertai
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Regardless of the initial treatment most patients
2022-12-01
Regardless of the initial treatment, most patients with advanced NSCLC experience relapse and disease progression [15]. A subpopulation of immediate concern and clinical need is patients who have advanced NSCLC that is especially aggressive, which is usually defined as disease that rapidly progresse
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Polycyclic aromatic hydrocarbons PAHs are abundant environme
2022-11-30
Polycyclic aromatic hydrocarbons (PAHs) are abundant environmental contaminants that are produced by the incomplete combustion of organic matter, combustion engines, residential heating, azd4547 synthesis burning, and industrial activities (Gelboin, 1980; Phillips, 1999, Phillips, 2002). Some PAHs
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Our initial approach to identify hits was two pronged
2022-11-30
Our initial approach to identify hits was two-pronged and included a high-throughput screening (HTS) campaign of the OSI kl compound name library as well as a virtual screening (VS) campaign, utilizing a publically available crystal structure of ACK1 (PDB code: ). A tolerance for protein flexibilit
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The finding of the apelin
2022-11-25
The finding of the apelin/APJ axis represents an impressive event in cardiovascular studies. As a result of various experimental and clinical studies conducted in vivo and in vitro, it has been indicated that apelin/APJ is a crucial mediator of cardiovascular homeostasis, which takes part in the pat
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br Under normal physiological conditions
2022-11-24
Under normal physiological conditions, the agonist binds to AT1R on the surface of the plasma membrane and activates the receptor, mediating downstream signaling. Then, activated AT1R is phosphorylated by protein kinase C (PKC) [13] or G protein coupled receptor kinases (GPKs, such as GRK2 [13], G
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BV6 mg APP is a member of a conserved protein
2022-11-24
APP is a member of a conserved protein family that also includes amyloid precursor-like proteins 1 and 2 (APLP1, APLP2).8, 9, 10 The proteins in this family are type I single-pass transmembrane BV6 mg with receptor-like structural features but not entirely clear cellular functions.11, 12, 13, 14 The
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br Introduction Breast cancer is
2022-11-24
Introduction Breast cancer is the most frequently occurring cancer in women, and despite the development of new therapies there has been little decline in the mortality rate over the past decade (Siegel et al., 2015). This is partly due to the genetic diversity of breast cancers, such that there
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HT modulates cortical and hippocampal pyramidal cell
2022-11-18
5-HT modulates cortical and hippocampal pyramidal cell function in a very complex manner, since most 5-HT receptor subtypes (excitatory as well as inhibitory) are expressed on pyramidal MS023 as well as GABAergic interneurons that exert inhibitory control over pyramidal cells (Leiser et al., 2015,
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