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The theoretical calculations of ADME parameters molecular we
2024-12-30
The theoretical calculations of ADME parameters (molecular weight (MW), log P, topological polar surface are (tPSA), number of hydrogen donors (nON) and acceptors (nOHNH), and volume) and DLS are presented in along with the violations of Lipinski’s rule. According to these data, all compounds (–) c
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The acetylcholinesterase AChE inhibitor tacrine THA exerts n
2024-12-30
The acetylcholinesterase (AChE) inhibitor, tacrine (THA), exerts neuroprotective effects in time- and does-dependent manners against glutamate neurotoxicity (Takada-Takatori et al., 2006a, 2006b) and amyloid-β protein toxicity in PC12, a pheochromocytoma line (Wang et al., 2002; Xiao et al., 2000).
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Molecular docking simulations were carried out for ligands i
2024-12-30
Molecular docking simulations were carried out for ligands – in the ACE crystal structure (1O86) and DPP4 crystal structure (2G5P). Comparison of the binding mode of – () with enalaprilat (a) in ACE shows that the phenethyl group (–, enalaprilat) occupies the S1 pocket and the adjacent carboxylic Bi
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In conclusion we have designed and
2024-12-27
In conclusion, we have designed and synthesized a series of 4-phenyl-thiazole analogues as potent ATX inhibitors. Total twenty-five compounds were synthesized and evaluated for their inhibitory activity on ATX using FS-3 and human plasma assays. Compound was found to be the most potent derivative pr
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Pazopanib Autotaxin has been linked to
2024-12-27
Autotaxin has been linked to chemoresistance through its ability to inhibit apoptosis induced by paclitaxel in breast cancer Pazopanib [15] and LPA can inhibit cell death induced by cisplatin [40]. Autotaxin was included in the present study because it was identified as being over-expressed in pati
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However cancer and fibrotic diseases are
2024-12-27
However, cancer and fibrotic diseases are the most extensively studied disease states. ATX is connected to various cancers because it can stimulate chemokinesis and chemotaxis in melanoma cells. Upregulated ATX stephen ure has been reported in breast cancer,, prostate cancer, thyroid cancer, non-sma
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br Concluding remarks Autophagy ensures
2024-12-27
Concluding remarks Autophagy ensures cell homeostasis and survival through the continuous degradation/recycling of intracellular components. It can also represent a conserved, cell-intrinsic, defense mechanism against invading pathogens, including viruses. The autophagy process can be activated r
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Along with the improvement of the cadmium
2024-12-27
Along with the improvement of the cadmium transport from roots to aerial tissues, as is required for phytoremediation, over-expression of PtoHMA5 also led to the excessive accumulation of cadmium in leaves that was harmful to plant growth and physiological performance. Thus, detoxification of the he
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In our H K ATPase assay Fig and
2024-12-27
In our H+, K+-ATPase assay (Fig. 1 and Supplementary Fig. 1), myricetin (IC50 = 0.58μM) was more potent than acid-activated omeprazole (IC50 = 1.50μM). In contrast, in oral administration in mice (Fig. 3), omeprazole (20mg/kg) more effectively inhibited gastric Aurora B inhibitor secretion compared
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br Materials and methods br Results br Discussion CUs which
2024-12-27
Materials and methods Results Discussion CUs, which have been used as traditional medicine for thousands of years in East Asian countries, have the potential to be used for cancer chemoprevention and chemotherapy [17], [18], [19], [20]. CuB is one of the most promising agents as it is repor
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br ACL Regulation and Role in Lipid Metabolism ACL
2024-12-27
ACL Regulation and Role in Lipid Metabolism ACL is a ubiquitous enzyme at the nexus of nutrient catabolism and synthesis of cholesterol and fatty acids. In mammals, it is highly expressed in lipogenic tissues including adipose, liver, and lactating mammary glands [9]. In the presence of ATP and C
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Hypoxia induced replication arrest has been demonstrated in
2024-12-27
Hypoxia-induced replication arrest has been demonstrated in a variety of organisms in addition to mammals; including Zebrafish , , and (brine shrimp) which have been shown to survive for 4 years and longer in anoxic conditions . Despite this breadth of study, little is known about the mechanism of
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Co is an essential element for
2024-12-27
Co is an essential element for life in minute amounts [5]. The human adult contains about 1.1mg Co with the daily requirement of 0.1μg/day. Co is a component of vitamin B12. Co induces erythropoietin and blocks iodine uptake by the thyroid, controls the transfer of enzymes like homocysteine methylt
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APJ is mainly coupled to PTX sensitive
2024-12-27
APJ is mainly coupled to PTX-sensitive Gi/o proteins [33], and thus, it is associated with the inhibition of adenylyl cyclase and the activations of PI3K/Akt signaling and MAPKs signaling pathways [23], [54], [55], [56]. In a previous study, apelin stimulations of the PI3K/Akt and/or the MAPK pathwa
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Indications that HMGA proteins are involved in regulating th
2024-12-27
Indications that HMGA proteins are involved in regulating the structure and function of large chromatin domains come from the early work of Saitoh and Laemmli [143]. Employing immunolocalization techniques, these workers demonstrated that HMGA1 proteins are co-localized with both histone H1 and the
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