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Most of the identified aldose reductase inhibitors possess u
2025-03-03
Most of the identified aldose reductase inhibitors possess undesirable effects like poor pharmacokinetic properties, hypersensitivity and Steven-Johnson Syndrome [1]. However, the main side effect is the lack of selectivity relative to aldehyde reductase (ALR1, EC 1.1.1.2). ALR1 plays the important
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br Glioblastoma GBM is the highest grade glioma Grade IV
2025-03-03
Glioblastoma GBM is the highest-grade glioma (Grade IV) according to WHO classification and belongs to the most malignant form of ECL detection reagent tumor. It is an incurable disease despite the use of aggressive treatments that include surgery and radiotherapy, usually in combination with ch
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Interestingly hypoxia and an enhanced Warburg effect ultimat
2025-03-03
Interestingly, hypoxia and an enhanced Warburg effect ultimately lead to increased lactate production. The accumulation of lactate results in an acidic tumor microenvironment, which induces local inflammation. Lactate also promotes the polarization of macrophages that express immunosuppressive argin
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br Introduction Psychostimulant abuse and
2025-03-03
Introduction Psychostimulant abuse and addiction remain a societal problem in the United States. The latest statistics from the National Survey on Drug Use and Health indicate that slightly less than one million people over the age of 12 report having a cocaine use disorder (NSDUH, 2016). Additio
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Involvement of Adiponectin in the regulation of imatinib res
2025-03-03
Involvement of Adiponectin in the regulation of imatinib resistance in human CML cells has not been hitherto examined. Therefore, in this study, we first established imatinib-resistant K562 CML cells, and then evaluated the effect of Adiponectin in reversing imatinib resistance. The data presented h
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The assay performance was estimated using Z factors
2025-03-03
The assay performance was estimated using Z′-factors (plotted in Fig. 2A) according to Zhang et al. calculated for each plate comparing positive (in the absence of an inhibitor) and negative controls (in the presence of an AdK inhibitor). The mean Z′-factor±SD was determined to be 0.7±0.1, indicativ
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The first suggestions that the cleaved intracellular domain
2025-03-03
The first suggestions that the cleaved intracellular domain of APP, AICD, might transit to the nucleus and hence selectively regulate gene transcription arose from analogies with the Notch receptor signalling system where similar intra-membrane proteolysis occurs [84], [85] and it was later confirme
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While the direct effects of ARI
2025-03-03
While the direct effects of 5-ARI lead to a dramatic CHC in serum DHT levels, other laboratory values are also affected by 5-ARI use. Serum testosterone elevations are known to occur with both finasteride and dutasteride use, but values will typically remain within the normal laboratory range [18].
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Fig A shows a schematic
2025-03-03
Fig. 2A shows a schematic representation of histological results according to the Franklin and Paxinos Mouse Brain Atlas (2001). The black circles represent the sites of drug infusion that were on-target within the amygdala. Gray circles represent the animals that had infusion locations outside the
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br ARIs in the prevention of prostate
2025-03-03
5ARIs in the prevention of prostate cancer Prostate cancer continues to be a leading cause of male deaths worldwide. In 2009, it was estimated there would be 192,280 new cases of prostate cancer with a predicted 27,360 deaths [25]. Because androgens, and specifically DHT, play a large role in bot
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br Acknowledgements This work was supported by
2025-03-03
Acknowledgements This work was supported by the FedEx Institute of Technology at The University of Memphis (to DLB and ALP), NSF REU CHE 1156738 (to ALP in support of RSS), and NIHCA921060 (to GT). This material is based upon work supported by the National Science Foundation under Grant No. CHE-1
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Benzoic acid metabolite Various cardiovascular diseases show
2025-03-03
Various cardiovascular diseases show a high occurrence of autophagosomes. Whereas basal autophagy is required for the proper functioning of cardiomyocytes [82], the deletion of Atg5 gene in myocardium shows a high risk of cardiomyopathy [83]. Hamacher et al. observed that an upregulation of Bnip3,
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Here we report discovery of highly
2025-03-03
Here we report discovery of highly selective pan-Aurora kinase inhibitors through phenotypic screening. The co-crystal structure of methosulfate bound in the ATP binding site of Aurora A is described, and provides insight into the possible structural basis for the selectivity of the interaction.
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Based on the extracellular domain structures
2025-03-01
Based on the extracellular domain structures, we can infer that the dimer arrangement of GABAB receptor will undergo substantial changes upon receptor activation (Geng et al., 2013). First, agonist-stimulated closure of GABAB1 VFT would cause an upward rotation of its LB2 domain, coupled with an inw
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Thus a majority of known chemical
2025-03-01
Thus, a majority of known chemical and physico-chemical methods of metallic ions assay has a number of disadvantages, such as a low sensitivity and selectivity, high costs and complexity of the equipment. Therefore, the development of simple cost-effective sensitive methods of quantitative analysis