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br Acknowledgments br Introduction Angiotensin II AngII is a
2024-03-22

Acknowledgments Introduction Angiotensin II (AngII) is among the most potent vasoactive substances produced in humans. Its effects are numerous, from vasoconstriction to control of fluid and electrolytes balances. Many of the physiological and pathological effects of AngII are mediated by the
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There is a growing body of evidence showing that
2024-03-22

There is a growing body of evidence showing that pentobarbital causes memory disorders [3], [4], [5]. Our results that a single injection of pentobarbital into bilateral hippocampus significantly impaired hippocampus-dependent spatial memory retrieval (Fig. 1) add support to that evidence. Previous
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Cell surface metalloproteases coordinate signaling
2024-03-22

Cell surface metalloproteases coordinate signaling during development, tissue homeostasis, and disease. A disintegrin and metalloprotease 17 (ADAM17) is a well-characterized member among ADAM family, which mediates the cleavage of various cell surface proteins (Black, 2002, Black et al., 1997, Dello
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The excellent potencies selectivities and improved PK associ
2024-03-21

The excellent potencies, selectivities and improved PK associated with the piperazine class triggered more extensive off-target screenings of the highlighted compounds. A screen of more than 100 enzymes, receptors, and ion channels resulted in activity at the norepinephrine transporter (NET). This
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Based on the observation that
2024-03-21

Based on the observation that antipsychotic drugs increase 5-HT1A–D2 heteromerization level (Łukasiewicz et al., 2016), we set out to compare the effect of paroxetine to that of risperidone. Paroxetine, a potent SSRI, is very effective in the treatment of depression and anxiety disorders, e.g., gene
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In order to investigate their effects in
2024-03-21

In order to investigate their effects in vitro, therefore, we first used TE671 cells, which have provided a useful source of human AChR for in vitro and radioimmunoassay studies. We found no marked effect of either MuSK-MG or SNMG sera on AChR numbers or on AChR subunit expression. This appears to c
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On the basis of the above information we
2024-03-21

On the basis of the above information, we designed a new series of benzothiazole–piperazine derivatives (–) that have the aforementioned structural requirements (). Benzothiazole is an important ring system in the drug discovery studies of AD. There are several benzothiazole compounds that show pote
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Acetylcholinesterase AChE activity and expression level can
2024-03-21

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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A similar circuit between pyramidal neurons
2024-03-21

A similar circuit between pyramidal neurons and SST interneurons is also prevalent in layers 2/3 of the cortex. The synapses onto SST interneurons, however, are functionally weak, raising questions about their computational power. In the first set of experiments, Urban-Ciecko et al. (2018) show that
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Previously several genes such as cytokine
2024-03-21

Previously, several genes such as cytokine (Lyu and Park, 2007), cell motility-associated genes (Schotterl et al., 2017), transforming growth factor-β (TGF-β), TGF-β receptor II which is a cell surface receptor with serine/threonine kinase activity (Jiang et al., 2014, Schotterl et al., 2017), cell
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Endoplasmic reticulum ER stress resulting from
2024-03-21

Endoplasmic reticulum (ER) stress resulting from accumulation of misfolded proteins in ER lumen stimulates a chain of adaptive responses termed as the unfolded protein response (UPR). Glucose related protein (GRP78/BiP), key ER chaperone essential for the activation of the ER-transmembrane signaling
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Over the past decade extensive research has been directed
2024-03-21

Over the past decade, extensive research has been directed toward the discovery of Aurora-selective small-molecule inhibitors. As a result, a handful of Aurora inhibitors has been identified. Among them, 1 (VX-680) and 2 (SNS-314) have entered human clinical trials as pan-Aurora kinase inhibitors (F
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br Crystal structure ACLY protein is a homotetramer of
2024-03-21

Crystal structure ACLY protein is a homotetramer of four identical subunits [9]. Each polypeptide chain contains 1101 amino-acid residues [10]. The crystal structure of full-length ACLY protein is yet unresolved. However, Sun et al. recently succeeded in crystallizing chymotrypsin-truncated human
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br Author contributions br Conflicts of interest
2024-03-21

Author contributions Conflicts of interest The authors declare no competing financial interests. Acknowledgement This work was supported by grants from the Deutsche Forschungsgemeinschaft (Sonderforschungsbereich/Transregio 166–Project C1 and grant CA 1014/1-1 to D.C.) and the IZKF Würzbur
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Expression subcellular localization transcriptional activity
2024-03-21

Expression, subcellular localization, transcriptional activity and protein stability of Foxo are regulated by proteins such as STAT3, PKB, JNK and AMPK (Sun et al., 2017; Zhang et al., 2011). STAT3 is a member of the signal transducer and activator of transcription (STAT) protein family that plays c
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