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HT modulates cortical and hippocampal pyramidal cell
2025-03-01

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 Macitentan as well as GABAergic interneurons that exert inhibitory control over pyramidal cells (Leiser et al., 2
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Introduction Adenosine monophosphate cAMP is a general purpo
2025-03-01

Introduction Adenosine 3′,5′-monophosphate (cAMP) is a general-purpose signaling molecule present in most branches of life. Intracellular cAMP levels control diverse cellular functions. In bacteria, cAMP regulates metabolism by activation of the catabolite activator protein (CAP), also known as cAM
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Since pyrrolopyrimidine dithiolanes and both displayed parti
2025-03-01

Since pyrrolopyrimidine dithiolanes and both displayed particularly excellent levels of ACK1 inhibition, these analogs were viewed as potential candidates for further investigation in tumor xenograft experiments. While in vitro metabolic studies indicated that pyrrolidine was predicted to be signifi
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PRT 4165 Application of the broad acting HTR antagonist
2025-02-28

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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Pompe disease is accompanied by
2025-02-28

Pompe disease is accompanied by the deficiency of the lysosomal α-1,4-glucosidase that makes the Chemotactic peptide unable to hydrolyze glycogen to glucose, thereby resulting in the accumulation of glycogen in lysosomes, especially in skeletal muscles and cardiac tissues. This accumulation results
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Inactivation of the proton pump comes with luminal alkaliniz
2025-02-28

Inactivation of the proton pump comes with luminal alkalinization of the targeted vesicles such as lysosomes (Fig. 2b). Lysosome pH can also be raised stoichiometrically by addition of a membrane-permeable weak ryanodine such as methylamine or chloroquine which accumulates in its protonated, non-me
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Human leukemic blasts from both
2025-02-28

Human leukemic blasts from both AML and ALL patients demonstrated 5-, 12-, and 15-LOX expression [54]; however, using quantitative PCR, 5-LOX was much more prevalent than 15-LOX. When 15-HETE, 12-HETE, and LTB4 were tested for a direct effect on leukemic blasts, none induced apoptosis [54]. In contr
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Introduction Lipoxygenases LOXs are key enzymes that catalyz
2025-02-28

Introduction Lipoxygenases (LOXs) are key enzymes that catalyze the polyunsaturated fatty acids (PUFAs) such as arachidic wdr5 (AA), linoleic acid (LA) and others unsaturated fatty acids (Brash, 1999). LOXs are expressed in immune, neural, epithelial, tumor cells and other cells (Claesson, 2009). B
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Introduction Initially postulated to represent the main sour
2025-02-28

Introduction Initially postulated to represent the main source of ATP production in eukaryotic cells, mitochondria are recently recognized to perform manifold essential functions beyond energy production, impacting most areas of cell biology and medicine [1]. Mitochondrial metabolism is both the ba
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Heparin br Results br Discussion br STAR
2025-02-28

Results Discussion STAR★Methods Author Contributions Acknowledgments We thank Angela Walker for assistance with the manuscript; Junlin Liu, Xiangxiang Gu, Na Chen, Lu Xue, and the BV Core Facility of iHuman Institute for their support; scientists and colleagues at Amgen Inc., Zhulun W
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Z-VEID-FMK The rescue of the behavioral deficit was associat
2025-02-28

The rescue of the behavioral deficit was associated with a significant reduction in the levels of both soluble and insoluble Aβ peptides and their deposition in the Z-VEID-FMK of the same animals. In search for the mechanism behind the reduced amyloidosis, we assessed APP metabolism. Confirming pre
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In AD and possibly other forms of
2025-02-28

In AD, and possibly other forms of dementia, it has been suggested that tau mislocalization to dendritic spines anticipates neurodegeneration [48]. Accumulation of hyperphosphorylated tau in dendritic spies would cause a derangement of synaptic function, thereby impairing excitatory synaptic transmi
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During the course of our ACK inhibitor program
2025-02-27

During the course of our ACK1 inhibitor program, a high-throughput screening (HTS) campaign of our internal sample collection was conducted. A series of -aryl pyrimidine-5-carboxamides of the general structure () was identified. Earlier studies of the structure–activity relationship (SAR) of identif
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In order to investigate their effects
2025-02-27

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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indacaterol Qualitative inspection of the single channel tra
2025-02-27

Qualitative inspection of the single-channel traces presented in both Figures 3 and 4 shows that within bursts of activity, βAnc-containing AChRs display a marked reduction in open probability. To quantify these differences in single-channel behavior, we performed dwell-time analysis under high-reso
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