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We further analyzed selected hit compounds for their
2023-12-22

We further analyzed selected hit compounds for their ability to inhibit human AdK in intact cells. Human 1321N1 astrocytoma Fusidic Acid sodium salt synthesis were utilized which were found to express AdK. The whole cell assay was performed using a 96-well format. The standard AdK inhibitor 5-iodotu
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Many metalloenzyme inhibitors consist of two
2023-12-22

Many metalloenzyme inhibitors consist of two chemical components: the MBG, the portion of the inhibitor designed to bind to the metal, and the scaffold, the portion of the inhibitor recognized by the amino BCA Protein Quantitation Kit residues that form the substrate-binding site of the metalloenzy
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br The embryological and physiological
2023-12-22

The embryological and physiological roles of ATX ATX is a vital enzyme that is needed for early embryological development. ATX knockout (KO) (ENPP2−/−) embryos die in utero on average at day 9.5 with vascular and neural tube defects [30], [73], [74], [75]. In these mice, malformations in the alla
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PF also a dual Aurora A and Aurora
2023-12-22

PF-03814735, also a dual Aurora-A and Aurora-B inhibitor, was administered in a phase I dose escalation study in a 3-weekly Entrectinib for 5 or 10 consecutive days [69], [70]. To date 25 patients have been included in 7 dose levels (5–100mg/day for 5 days). Using the 5-day schedule the MTD was def
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Evidences have suggested that impairment of CK
2023-12-22

Evidences have suggested that impairment of CK activity contributes to inhibition of Na+, K+-ATPase and H+-ATPase activities during infectious diseases, since these ATPases are dependent of ATP, as observed by Baldissera et al. [31] in fish experimentally infected by Aeromonas caviae. We observed th
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In addition to drawing attention to
2023-12-22

In addition to drawing attention to Ser454 of ACL as a phosphosite that is regulated by both BDK and PPM1K, our phospho-proteomics screen identified several additional sites in other proteins. For example, Ser25, Ser29, and Ser79 of the lipogenic enzyme acetyl-coA carboxylase 1 (ACC1) were found to
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We further conducted stratified analyses to
2023-12-21

We further conducted stratified analyses to observe changes in enzyme levels across the periods by subgroups. Fig. 1 shows the changes in GPx levels by subgroups of age, sex, and smoking status. In all participants, GPx levels decreased when air pollution levels declined but increased after the Olym
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br MADS box proteins in plants a flourishing
2023-12-21

MADS box proteins in plants, a flourishing family In contrast to animals, homeotic genes in plants do not code for homeodomain-containing proteins, but rather, in almost all cases, for MADS domain proteins. The sequencing of the genome of Arabidopsis thaliana revealed more than 100 putative MADS
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As patients with type diabetes are known to
2023-12-21

As patients with type 2 diabetes are known to be hyperinsulinemic per se, this relationship between insulin/IGF1 receptor and AR may point towards a causal role of insulin in AR upregulation. Indeed, this is supported by several previous observations. Beyond the already mentioned AR activation by in
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br Introduction AMP activated protein kinase AMPK has been f
2023-12-21

Introduction AMP-activated protein kinase (AMPK) has been found to be a key character against cardiovascular diseases and cellular stress. When activated by certain stress, AMPK regulates sugars and fatty acids that are good or detrimental to the heart. For example, targeting AMPK phosphorylation
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br Experimental methods br Acknowledgments br Introduction L
2023-12-21

Experimental methods Acknowledgments Introduction Long-term potentiation (LTP) and long-term depression (LTD) at excitatory synapses are thought to underlie experience-dependent learning and memory. These synaptic plasticity mechanisms are best characterized at hippocampal CA1 synapses, whe
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Introduction Lipoxygenases LOXs are key enzymes that catalyz
2023-12-21

Introduction Lipoxygenases (LOXs) are key enzymes that catalyze the polyunsaturated fatty acids (PUFAs) such as arachidic c-myc inhibitor (AA), linoleic acid (LA) and others unsaturated fatty acids (Brash, 1999). LOXs are expressed in immune, neural, epithelial, tumor cells and other cells (Claess
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br Results and discussion br
2023-12-21

Results and discussion Conclusion The tyrosine kinase ALK represents one of the most successful molecular targets for the development of precise medicine to treat stratified subgroups of cancer patients. Three generations of ALK inhibitors have been awarded the FDA's approval or are being exte
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br ABCA and cancer drug response
2023-12-21

ABCA2 and cancer drug response Overall, the expression of ABC transporters has been linked with multidrug resistance phenotypes through the efflux of drugs via ATP-dependent transport. For example, 13 distinct transporters (ABCA2, ABCB1, ABCB4, ABCB11, ABCC1–6 ABCC10, ABCC11 and ABCG2) have been
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Here we have used transcriptome
2023-12-21

Here, we have used transcriptome analysis of primary neonatal rat cardiomyocytes treated with either the ETR agonist endothelin-1 or the α1-AR agonist phenylephrine to assess differences in their respective signalling networks, and further probed these differences using a panel of fluorescent resona
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