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Secondly as pointed out by Sulentic and Kaminski in
2025-02-28
Secondly, as pointed out by Sulentic and Kaminski in their recent paper [90], most of the AhR literature to date has focused on mouse AhR. Although both mouse and human AhR are interchangeable in many in vitro systems, the in vivo ligand binding affinity is drastically different between the two AhRs
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In addition to the above mentioned
2025-02-27
In addition to the above-mentioned synaptic mechanisms, the serotonergic system also has a critical role in the antidepressant effects of mGlu2/3 receptor antagonists. Indeed, we previously reported that mGlu2/3 receptor antagonists increased the firing rate of serotonin neurons in the dorsal raphe
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A high throughput small molecule ACK biochemical inhibition
2025-02-27
A high-throughput small molecule ACK1 biochemical inhibition screen was performed in-house and led to the identification of 1μM inhibitor furanopyrimidine (). Further binding studies found LKB1 to be both ATP-competitive and reversible. Early structure-activity relationship (SAR) work was performed
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ACK has been clearly implicated in cancer progression in rec
2025-02-27
ACK1 has been clearly implicated in cancer progression in recent years. A strong correlation between ACK1 gene copy number, protein level and activity have been demonstrated in tumors of different tissue types (Mahajan et al., 2007; van der Horst et al., 2005; Wang et al., 2006). Our western blot an
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Ryoichi et al modified potent clinical candidate VX with cya
2025-02-27
Ryoichi et al. modified potent clinical candidate VX-680 (6) with 3-cyano-6-(5-methyl-3-pyrazolamino)pyridine as Aurora kinase inhibitor. Substituted cyano pyridine derivative (7) inhibited proliferation of HCT-116 cells with an IC50 value of 115 nM. It showed tumor inhibition in mice model at a dos
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br Introduction In addition to ATP production an
2025-02-27
Introduction In addition to ATP production, an important role of mitochondria in the pancreatic beta cell is anaplerosis, which is the net synthesis of citric ICG001 cycle intermediates that are exported to the cytosol where they are converted to numerous other metabolites that stimulate and/or s
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br In vivo visualization of aromatase with positron
2025-02-27
In vivo visualization of aromatase with positron emission tomography (PET) Positron emission tomography (PET) utilizes the high DMPO photons formed during the annihilation of positrons to detect the changes in the amount and localization of injected radiopharmaceuticals in the living body (recen
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ML133 HCl Chlorogenic acid an abundant polyphenol found in c
2025-02-27
Chlorogenic ML133 HCl (7), an abundant polyphenol found in coffee and the human diet, has various biological activities including antioxidant and anticancer effects [54]. Jiang et al. reported that compound 7 had a selective cytotoxic activity on human oral tumor cells (HSG, HSC-2) as compared with
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Apoptosis a major process of programmed
2025-02-27
Apoptosis, a major process of programmed cell death, and in response to many chemopreventive agents (Jeyamohan et al., 2016). In general, two major signaling pathways control apoptosis, namely, a pathway mediated by cell death receptor and a pathway mediated by mitochondrion, and possible drug targe
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Most clinically approved antiangiogenic drugs are aimed at b
2025-02-27
Most clinically approved antiangiogenic drugs are aimed at blocking the action of vascular endothelial growth factor, or VEGF, which is accepted to be the most important tumor-derived angiogenic factor, stimulating proliferation and migration of endothelial cells, as well as branching of vessels (Fe
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In the present study a
2025-02-27
In the present study, a splice acceptor site mutation (c.1769-1G > C) was identified in AR gene from patients with CAIS. The c.1769-1G > C mutation results in replacement of the normal sequence (CAG/G) with a new sequence (CAC/G) at the splice acceptor site of intron 2. In the splice acceptor site r
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dub inhibitor In a recent issue of Minokoshi and colleagues
2025-02-26
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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Introduction Aldose reductase ALR is the first
2025-02-26
Introduction Aldose reductase (ALR2) is the first enzyme of the polyol pathway that catalyzes the reduction of glucose to sorbitol utilizing NADPH as a cofactor. The intracellular accumulation of sorbitol, due to increased aldose reductase activity at high blood glucose levels, such as those occurr
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In this study Rb increased the phosphorylation of p
2025-02-26
In this study, Rb1 increased the phosphorylation of p38 MAPK and Akt and macrophage phagocytosis of bacteria in mouse lung cells, consistent with the in vitro results. A recent study showed that Rb1 diminished the severity of lung injury in rats exposed to LPS. Rb1 inhibited the LPS-induced increase
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The obtained results indicate that even
2025-02-26
The obtained results indicate that even when the impairment of the same forms of memory are present, amnesia can develop in different ways. Impairment of memory reconsolidation in the conditioned food aversion model through both the serotonin receptor antagonist and the antagonist of NMDA glutamate