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Further analysis sought to understand the mechanism
2024-09-10

Further analysis sought to understand the mechanism associated with the autotaxin-mediated increase of miR-489-3p in circulation. Based upon sequence complementarity, DIANA TarBase predicted miR-489-3p targets MAPK2K1, or MEK1, an oncogene widely dysregulated in cancer (Fig. 4A). To test this relati
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bax inhibitor br Crystal structure ACLY protein is a homotet
2024-09-10

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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The apoptosis promoting Bcl family includes BH only
2024-09-10

The apoptosis-promoting Bcl-2 family includes BH3-only proteins (e.g., Bim, Bid and Bad) and multiple-domain proteins (e.g., Bax and Bak). At the time of apoptosis stimulation (e.g., DNA damage), only the BH3-only protein is activated, directly or indirectly promoting Bax/Bak oligomerization, changi
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br In vivo visualization of aromatase with
2024-09-10

In vivo visualization of aromatase with positron emission tomography (PET) Positron emission tomography (PET) utilizes the high Phosphatase Inhibitor Cocktail 2 (100X in ddH2O) photons formed during the annihilation of positrons to detect the changes in the amount and localization of injected rad
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Due to its unique histological
2024-09-10

Due to its unique histological architecture and blood supply, the lung is one of the most susceptible organs under uncontrolled systemic inflammatory circumstance [16]. Several studies have reported the anti-inflammatory benefits of metformin in acute lung injury induced by lipopolysaccharide (LPS),
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In a recent issue of Minokoshi and colleagues have added
2024-09-10

In a recent issue of , Minokoshi and colleagues have added more light to our understanding of the role of hypothalamic AMPK in the regulation of energy balance. Previous seminal work from the same group suggested that AMPK in the PVH might be involved in the modulation of feeding . Here, they show
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Various compounds have been designed to inhibit aldose reduc
2024-09-10

Various compounds have been designed to inhibit aldose reductase (AR) [12]. These compounds can be classified into two main categories, the first category comprises those containing a carboxylic FRAX486 sale moiety, for example, 3-thiazolidineacetic acid derivative, which has been reported to be a p
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Despite functional studies demonstrating the role of HT in
2024-09-09

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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A highly attenuated B pertussis strain
2024-09-09

A highly attenuated B. pertussis strain, named BPZE1, has recently been described [10]. It produces enzymatically inactive pertussis toxin (PT), no dermonecrotic toxin and only trace amounts of tracheal cytotoxin. Markedly reduced lung pathology was observed in mice intranasally (i.n.) infected with
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br Materials and methods br Results br
2024-09-09

Materials and methods Results Discussion This study demonstrates that treatment with a selective adenosine kinase inhibitor ABT-702, thereby enhancing extracellular adenosine, can provide partial protection from age-related hearing loss in C57BL/6J mice. Chronic treatment with ABT-702, comm
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br Colabeling evidence for ACh and GABA cotransmission
2024-09-09

Colabeling evidence for ACh and GABA cotransmission Though functional demonstrations of ACh/GABA cotransmission remain largely limited to the retina and our recent analyses of cortex (Lee et al., 2010, Saunders et al., 2015a, Saunders et al., 2015b), evidence suggestive of ACh/GABA cotransmission
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The discovery of acetylsalicylic acid aspirin in
2024-09-09

The discovery of acetylsalicylic Gallein (aspirin) in 1897 paved the way for the development of classical NSAIDs as first-line therapeutics for anti-inflammatory, anti-pyretic and analgesic therapy. Large efforts have been made in the following decades to improve the efficacy and in particular safe
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Drug resistance development often involves structurally
2024-09-09

Drug resistance development often involves structurally un-related drugs and, specifically both conventional and targeted agents. IGROV-1/Pt1 DMPO synthesis are characterized by resistance to cisplatin and reduced sensitivity to inhibitors of EGF-R and MEK, the up-stream activator of ERK1/2, associ
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Having taken a step back from affinity
2024-09-09

Having taken a step back from affinity to gain better exposure and solubility, we started work to replace the unstable oxazolinone, and address the selectivity over the hERG channel. Keeping in mind the binding mode of the series from crystal structures, triazole was identified as another mildly aci
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Introduction Initially postulated to represent the main sour
2024-09-09

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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