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The discovery of acetylsalicylic acid aspirin in paved
2024-01-04
The discovery of acetylsalicylic Bufalin (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 safet
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Based on these findings the time point for manipulating auto
2024-01-04
Based on these findings, the time point for manipulating autophagy may also determine its role, whereby autophagy induction performed before ischemia could play a protective role but have an opposite effect once ischemia/reperfusion has occurred. This hypothesis is further supported by the protectiv
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The combination of Aurora kinase inhibitors with standard ch
2024-01-04
The combination of Aurora kinase inhibitors with standard chemotherapeutics or radiotherapeutics are currently in progress, such as AZD1152 plus radiotherapy in various solid cancer models. In addition, Azzariti et al. found that AZD1152-HQPA enhanced oxaliplatin and gemcitabine effectiveness in the
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The acidification of endocytic compartments is closely relat
2024-01-04
The acidification of endocytic compartments is closely related to endocytic activity, although the mechanism linking acidification and membrane dynamics is largely unknown. In a recent RNA interference (RNAi)-based screen, V-ATPase depletion blocked the formation of clathrin-coated vesicles, an effe
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Molecular docking quantitative structure activity relationsh
2024-01-03
Molecular docking, quantitative structure–activity relationship (QSAR) and high-throughput virtual screening (HTVS) studies have a very widespread use in computer-assisted drug design.25, 26, 27, 28 Suvannang et al. used the published X-ray crystallographic data to examine known aromatase inhibitors
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The approach of enzymatically converting an
2024-01-03
The approach of enzymatically converting an analyte and detecting it by the resulting small pH changes near the reduced graphene oxide (rGO) surface has successfully been pursued in case of urea (Piccinini et al., 2017). Furthermore, this work reported that electrostatic layer-by-layer (LbL) assembl
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br Materials and methods br
2024-01-03
Materials and methods Results Discussion The current treatment modalities for colorectal cancer are hampered by various issues such as high acquired resistance, long-term complication with potential of cancer recurrence, severe side-effects and poor therapeutic index [50], [51], [52]. Compl
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The electrokinetic remediation technique is carried out with
2024-01-03
The electrokinetic remediation technique is carried out with a low-level direct current, and the pollutants in soil can be transported and removed by the electric field [19]. This works well even in soil with low permeability via electro-osmotic flow and electro-migration [20]. The electrokinetic pr
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Another hypothesis is angiogenesis inhibition Angiogenesis i
2024-01-03
Another hypothesis is angiogenesis inhibition. Angiogenesis is a process that involves the growth, migration and differentiation of endothelial TRAM 39 to form new blood vessels. Angiogenesis favorably influences tumor growth and also influences tumor invasion of vessels, resulting in tumor metasta
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The association of male gender with
2024-01-03
The association of male gender with increased atherosclerosis has stimulated interest in the role of androgen signalling in this condition. Androgens act (Fig. 2) by direct activation of androgen receptor (AR), a nuclear receptor that acts as a ligand-regulated transcription factor (Gao et al., 2005
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Phosphatase Inhibitor Cocktail 3 (100X in DMSO) At the organ
2024-01-03
At the organismal level, skeletal muscle, lung and adipose tissues mediate net de novo synthesis and release of glutamine, whereas net glutamine catabolism occurs in the kidney [7]. The liver exhibits net glutamine consumption coupled to urea production in the post-absorptive state, and net glutamin
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Proteinase K Alectinib is a second generation ALK antagonist
2024-01-03
Alectinib is a second generation ALK antagonist that is built upon a 9-ethyl-6, 6-dimethyl-11-oxo benzo[b]carbazole scaffold (Fig. 5C) [58]. This drug is effective against the ALK L1196M gatekeeper mutation along with C1156Y and F1174L mutations [7]. The 11-oxo group of the drug forms a Proteinase K
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Finasteride has been shown to be
2024-01-02
Finasteride has been shown to be a mechanism-based inhibitor of 5AR-2 [9]. Finasteride acts as an alternate substrate for 5AR-2 and is initially bound in an extremely stable enzyme-bound NADP-dihydrofinasteride adduct which is ultimately processed to dihydrofinasteride. The NADP-dihydrofinasteride a
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AR is expressed in cell
2024-01-02
AR is expressed in cell-specific human ovarian follicles at all stages of follicular development [25]. Administration of androgens in animals demonstrated initiation of follicular recruitment, stimulation of early stages of follicular growth, and increase in the number of growing follicles [26,27].
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The aldehyde reductase AKR A and aldose reductase AKR B
2024-01-02
The aldehyde reductase (AKR1A1) and aldose reductase (AKR1B1) belong to aldo-ketoreductase (AKR) superfamily catalyzing the reduction of corresponding aldehydes and ketones involved. Both the closely related enzymes AKR1A1 and AKR1B1 have 65% structural similarity and differ only at the active site.
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