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Having taken a step back from affinity to gain better
2023-11-17
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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On the contrary evidence also suggests that autophagy plays
2023-11-17
On the contrary, evidence also suggests that autophagy plays a striking protective role in cancer cells. Highly burgeoning cancer mln0128 require cellular building blocks for their metabolism and energy production. At this stage of cancer development, autophagy acts as a friend providing all the ess
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Tenatoprazole The first description of autophagy as
2023-11-17
The first description of autophagy as a tumour suppression process arises from the observation that the initial step regulatory gene, Atg6/BECN1, was monoallelically lost in 40% to 75% of human prostate, breast, and ovarian cancers [31]. However, while BECN1 heterozygous mutant mice develop, with lo
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ATP citrate lyase ACLY is a cytosolic enzyme that catalyzes
2023-11-16
ATP citrate lyase (ACLY) is a cytosolic enzyme that catalyzes the generation of acetyl-CoA from citrate [15]. Acetyl-CoA is the building block for the biosynthesis of fatty acids and cholesterol, and also serves as a substrate of the acetylation reaction of various molecules, including histones and
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We subsequently performed immunohistochemistry on sections o
2023-11-16
We subsequently performed immunohistochemistry on sections obtained from mice at 16 weeks after surgery. Type II collagen expression was detected in all articular cartilage zones, but was weak in the upper zone in the vehicle-treated group. MMP-13 and type X collagen expression were increased in the
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Despite the absence of disulfide bonds in its linear structu
2023-11-16
Despite the absence of disulfide bonds in its linear structure, KT43C displays antifungal and antibacterial activity. Disulfide bonds are determinants of defensins' integrity and have been reported to increase the antimicrobial activity (Jenssen et al., 2006). However, some linear derivatives of AMP
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The basis for the protonation of chitosan
2023-11-16
The basis for the protonation of chitosan is the alkaline primary amino group, which is also the reason for the special properties of chitosan (Guibal, Van Vooren, Dempsey, & Roussy, 2006; Tamer et al., 2017; Yang et al., 2014). Our previous work (Meng et al., 2012) and several other reports (Yan et
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Aberrant lipid levels are associated with various disorders
2023-11-16
Aberrant lipid levels are associated with various disorders, including vascular diseases and diabetes. Furthermore, important events support the idea that lipids, especially cholesterol and its derivatives, have a fundamental role in the physiopathology of AD. The csf1r is rich in cholesterol, and i
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BMH-21 In order to get a better understanding of
2023-11-16
In order to get a better understanding of this synergy, we tested the effect of preliminary incubation of BMH-21 with non-stimulating concentrations of gonadotropins or FSK before subsequent stimulation by FSK or gonadotropins alone, also at sub-stimulating concentrations. We observed that human LH
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br Conclusions The present data suggest
2023-11-16
Conclusions The present data suggest that homeostatic balance of the cortical/hippocampal adenosinergic tone is necessary for normal working memory function and any deviation appears to impair performance – either as a consequence of A2AR under-activation when adenosine levels are reduced or due
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Our published data showed that in mouse heart the protein
2023-11-16
Our published data showed that, in mouse heart, the protein level of WDR1 was highest during the embryonic stage, but became progressively decreased to a constant level from birth to adulthood (Yuan et al., 2014), indicating an important role of WDR1 in embryonic heart development. However, functio
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G actin has a molecular weight
2023-11-16
G-actin has a molecular weight of 42 kD and dimensions about 55 × 55 × 35 Å3. It consists of 375 amino acids arranged into two individual domains (Alberts et al., 2014). A central cleft bisects the protein into two aforementioned domains which surround a deep cleft containing ATP or ADP and a tightl
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We have expressed the ECDs of the
2023-11-16
We have expressed the ECDs of the human α1, β1, γ and ɛ AChR subunits in the past using the methylotropic yeast Pichia pastoris as soluble glycosylated proteins [15], [16]. Further work with the γ subunit ECD revealed a marked improvement of the solubility and yield following the mutation of hydroph
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Owing to efficient catalytic character high
2023-11-16
Owing to efficient catalytic character, high electrolyte accessible area, easy fabrication and many other interesting properties, metal oxide nanoparticles are extensively used in a variety of electro-analytical processes [14]. Metal oxide nanoparticles immobilized over a conductive and large area s
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Pyrimidine is the important pharmacology core in
2023-11-15
Pyrimidine is the important pharmacology core in many Aurora inhibitors, such as VX-680, ENMD-2076, CYC-116 and ENMD-2076 [12]. To identify additional effective Aurora inhibitors, we designed a series of 2,4-diaminopyrimidine compounds, our modeling studies suggested that the Methoxyresorufin core a
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