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We found that several anticancer
2024-12-16

We found that several anticancer drugs inhibit 5-HT3 phorbol synthesis current in vitro. Several studies have suggested that 5-HT3 receptor antagonists have anti-mitogenic and apoptotic effects on colorectal and breast cancer cell lines (Ataee et al., 2010, Hejazi et al., 2015). Irinotecan is used f
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We further analyzed selected hit compounds
2024-12-16

We further analyzed selected hit compounds for their ability to inhibit human AdK in intact cells. Human 1321N1 astrocytoma 7389 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 as a po
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During the year study period of
2024-12-13

During the 4-year study period, 19.9% of men in the dutasteride group developed prostate cancer as compared to 25.1% in the placebo group, which represents an absolute risk FRAX486 of 5.1% for men taking dutasteride (Pe weighed against the prospect of undesirable sexual side effects and decreased qu
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The current antifungal pipeline contains several categories
2024-12-13

The current antifungal pipeline contains several categories of compounds at different stages of development [1], [9], [10], [96]. In Table 1 we summarize the most promising antifungal molecules that are in preclinical and in clinical development. Several compounds in the pipeline are derivatives of
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This development notwithstanding the chemotherapeutic treatm
2024-12-12

This development notwithstanding, the chemotherapeutic treatment for leukemia has stagnated over the last 40 years [35]. Main treatment options necessitate aggressive chemotherapy to target leukemic cells [36], [37], [38], [39]. Several limitations of current treatment options include the use of ant
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The AHR potentially enhances IDO expression possibly via
2024-12-12

The AHR potentially enhances IDO-expression, possibly via crosstalk with several inflammatory signaling pathways (shown by now for IL6 and ‘signal transducer and activator of transcription’ (STAT) 3, and for NFκB, toll like receptor-pathways) [56,59,60]. IDO metabolizes Trp to kynurenines, which are
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Among all the compounds the novel L derivative d showed
2024-12-12

Among all the compounds, the novel L-748,337 derivative (23d) showed the potent human β3-AR antagonist activity and high lipolysis inhibitory activity in vitro. The CUDC-907 australia 23d displayed 23-fold more potent β3-AR antagonist activity (EC50 = 0.5117 nM) than that of L-748,337 (EC50 = 11.91
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br Methods br Results br Discussion Adiponectin is
2024-12-12

Methods Results Discussion Adiponectin is naturally expressed and secreted exclusively from adipocytes, and adiponectin levels and its isoforms in circulation have recently been reported to highly associate with human coronary artery disease (CAD) [46], [47], [48], [49], these studies clear
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br Experiment br Results and discussion br
2024-12-12

Experiment Results and discussion Conclusion Introduction Tuberculosis (TB) is a chronic specific bacterial infection caused by bacteria of the Mycobacterium tuberculosis [1]. TB remains one of the deadliest diseases in the world. It is the second leading infectious cause of death after
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iso 1 Changes in actin microfilaments are mediated by
2024-12-12

Changes in iso 1 microfilaments are mediated by changes in extracellular matrix, mechanical stimulation or growth factors intracellular signaling. We observed significant changes in a number of intracellular signaling pathways associated with changes in actin dynamics during hMSCs differentiation.
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The nAChR has been considered an interesting potential
2024-12-12

The α7 nAChR has been considered an interesting potential target for numerous therapeutic indications over the last two decades, with GTS-21 one of the first candidates proposed for Alzheimer's disease [2], [3], [23]. Unfortunately, although many α7-selective agonists have been developed [21], none
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Additionally regulation of GPCR heteromerization by
2024-12-12

Additionally, regulation of GPCR heteromerization by specific ligands may depend not only on the affinity of ligands for receptors, but also on presence of different interacting proteins co-localizing with the receptors in the specific cell, which may induce some conformational changes and contribut
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Given the profound expression of HT A and
2024-12-12

Given the profound Ferrostatin-1 of 5-HT1A and 5-HT2A in the hippocampal CA1 region, and their potential to complex with mGluRs, the objective of this study was to examine if sleep deprivation alters the expression of 5-HT1A and 5-HT2A receptors and determine whether potential changes are reversibl
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The role of DHT in early teleost
2024-12-12

The role of DHT in early teleost embryogenesis is not entirely clear or established, however additional studies that treat fish embryos to DHT or to specific srd5a inhibitors at critical stages of development (i.e. prior to sex differentiation) will shed light on the early functions of this androgen
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An AXL decoy receptor with enhanced GAS
2024-12-12

An AXL decoy receptor with enhanced GAS6-binding properties, MYD1, was engineered as a therapeutic tool to disrupt GAS6/AXL signaling in vivo (Kariolis et al., 2014). MYD1 was shown to block metastasis of human ovarian cancer Calmidazolium chloride and a murine breast cancer cell line in grafting as
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