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AdipoRon acts on the anti
2024-04-17
AdipoRon acts on the anti-diabetic effects of adiponectin, exhibiting its effect through the activation of AMPK and PPARα pathways via AdipoR1 and AdipoR2, respectively [23]. AdipoR activation is a promising treatment for diabetes, nonalcoholic fatty liver disease, and cardiovascular disease, demons
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A previous study reported that the
2024-04-17
A previous study reported that the serotonergic mechanism was involved in the psychological stress-induced alteration in synaptic plasticity in the rat hippocampal CA1 field (Matsumoto et al., 2004). Sumitaka Inoue et al. (Inoue et al., 2014) reported that pretreatment with a 5-HT1A receptor partial
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7-Ethoxyresorufin In previous research we determined
2024-04-17
In previous research, we determined that blocking mAC during heparin-induced capacitation result in sperm having a lesser oxygen consumption, suggesting that cAMP produced by this enzyme would be linked to mitochondrial activity and, therefore, with the regulation of sperm metabolism (Fernández and
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Despite functional studies demonstrating the role of HT in
2024-04-17
Despite functional studies demonstrating the role of 5-HT in ureteral contractility, the source of endogenous 5-HT in the ureter is unclear. Since 5-HT-containing enterochromaffin cells, which are present in the gastrointestinal tract, could not be found in the ureter (Nocito et al., 2007, Ripoche,
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Another interesting interaction concerns NMDA preconditionin
2024-04-17
Another interesting interaction concerns NMDA preconditioning to protect against glutamate neurotoxicity. It has been shown that an A1R antagonist prevented neuroprotection evoked by NMDA preconditioning against glutamate-induced cellular damage in cerebellar granule cells. In this study, the functi
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We further analyzed selected hit compounds for
2024-04-17
We further analyzed selected hit compounds for their ability to inhibit human AdK in intact cells. Human 1321N1 astrocytoma daminozide were utilized which were found to express AdK. The whole cell assay was performed using a 96-well format. The standard AdK inhibitor 5-iodotubercidin was employed a
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(+)-Aphidicolin australia br Introduction Myasthenia gravis
2024-04-17
Introduction Myasthenia gravis (MG) is an autoimmune disease characterised by failure of transmission at the neuromuscular junction (NMJ). In 80–85% of myasthenia gravis patients, the disease is mediated by antibodies to the nicotinic (+)-Aphidicolin australia receptor (AChR; (Lindstrom et al.,
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Toxicity is the main reason for
2024-04-17
Toxicity is the main reason for the failure at all stages of the new drug development process. The major part of safety-related attrition occurs at preclinical phases while predicting preclinical safety liabilities earlier in the drug development process. This strategy enables the design and/or sele
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br AD and COX LOX pharmacology Early studies on
2024-04-16
AD and COX/5-LOX pharmacology Early studies on the role of cyclooxygenases in AD were inspired by epidemiological data suggesting that COX inhibitors such as nonsteroidal anti-inflammatory drugs (NSAIDs) could be beneficial in AD patients (Lucca et al., 1994, McGeer et al., 1990). This line of re
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A previous study reported that the serotonergic mechanism wa
2024-04-16
A previous study reported that the serotonergic mechanism was involved in the psychological stress-induced alteration in synaptic plasticity in the rat hippocampal CA1 field (Matsumoto et al., 2004). Sumitaka Inoue et al. (Inoue et al., 2014) reported that pretreatment with a 5-HT1A receptor partial
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br Introduction The principal pathways of adrenal and gonada
2024-04-16
Introduction The principal pathways of adrenal and gonadal steroidogenesis have been known for over 50 years (reviewed by Miller and Auchus, 2011). Cholesterol is first converted to pregnenolone via three reactions, 20-hydroxylation, 22-hydroxylation and scission of the 20,22 carbon–carbon bond,
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Over the past decade extensive
2024-04-16
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 Disclaimer Statement br Acknowledgments br Introduction M
2024-04-16
Disclaimer Statement Acknowledgments Introduction Metabolic changes are a common feature of cancerous tissues. Mutations in oncogenes and tumor suppressor genes cause alterations to multiple intracellular signaling pathways that rewire tumor cell metabolism and re-engineer it to allow enhan
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Treatment of all of the GYN cancer cells in
2024-04-16
Treatment of all of the GYN cancer SKF 83566 hydrobromide in this study with ATRi not only reduced phosphorylation of Chk1 at Ser345 following genotoxic stress, but also phosphorylation of ATM. Loss of phospho-ATM following ATRi treatment is not likely due to non-specific targeting of ATM by ETP-464
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Introduction the DNA damage response important implications
2024-04-16
Introduction: the DNA damage response — important implications for tumour development and treatment Cells are invariably challenged by tens of thousands of lesions inflicted on their DNA everyday (Lindhal, 1993). This DNA damage can be caused exogenously by exposure to different types of radiation
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