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The assay performance was estimated using Z factors
2022-11-01

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 benzimidazole group seems to be a key feature for
2022-11-01

The benzimidazole group seems to be a key feature for the excellent anti-tumor activity of galeterone (159), which motivated the synthesis of new steroidal inhibitors containing N-heterocyclic groups structurally related to benzimidazole. Thus, several 1H- and 2H-indazole derivatives of dehydroepian
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A positive correlation between nasopharyngeal CCL and CCL co
2022-11-01

A positive correlation between nasopharyngeal CCL3 and CCL5 [16] concentrations and illness severity was shown in evaluating patients with RSV bronchiolitis [17]. CCL5 and CCL3 are important for monocyte and lymphocyte recruitment to the lung during RSV infection [7], [16], [18]. Despite the signifi
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4-IPP Based on its kinetic parameters and quaternary structu
2022-11-01

Based on its kinetic parameters and quaternary structure, R. pycnus arginase is a typical ureotelic L-arginase [2]. The Km value of the enzyme was lower than other arginases from other organisms (Table 2), including S. cerevisiae (15.7mM), B. anthracis (10mM), B. caldovelox (3.4mM), human liver (2.3
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OCT also is known as POU F plays
2022-10-31

OCT4 (also is known as POU5F1) plays an important role in embryonic stem cell self-renewal, development and reprogram somatic cell into pluripotent stem cell [[5], [6], [7]]. Recently, many studies also find OCT4 promotes the progression of many tumors. For example, Wnt/β-catenin promotes the expans
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br Materials and methods br Results The determination of the
2022-10-31

Materials and methods Results The determination of the intrinsic inhibitory potential of the oximes HI-6 and MMB-4 with human and guinea pig AChE revealed marked differences between both oximes (Table 1). MMB-4 had an only marginal effect on both AChE species, calculated IC50 of >1000μM, while
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Introduction Microdialysis is an in vivo technique
2022-10-31

Introduction Microdialysis is an in vivo-technique which allows continuous sampling of small molecular weight substances (such as neurotransmitters, metabolites and neuropeptides) from the extracellular space of different tissues or organs, e.g. brain, muscle or skin. While the implantation of the
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Introduction The lysosomal storage disorder
2022-10-31

Introduction The lysosomal storage disorder Gaucher disease (Mendelian Inheritance in Man, OMIM #230800) results from the recessively inherited deficiency of lysosomal glucocerebrosidase (GCase, EC 3.2.1.45), caused by mutations in the gene GBA1 (MIM# 606463) located on chromosome 1q21. The enzymat
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Finasteride has been shown to be a mechanism based
2022-10-31

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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closantel Regarding androgens it is known
2022-10-31

Regarding androgens, it is known that they are also essential for reproductive success (Walters et al., 2010). At the molecular level, their effects are produced mainly by dihydrotestosterone (DHT), arising from the conversion of testosterone by the enzyme 3-oxo-5-alpha-steroid-4-dehydrogenase (enco
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Considering the physicochemical stability results on Fig it
2022-10-31

Considering the physicochemical stability results on Fig. 5, it was observed that the particles are stable when they are stored at 4 °C for 30 days. After day 30, a significant increase was observed in particle size, but at the end of the 90 days the SLN particle size is still below 100 nm. Stabilit
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br Disclaimer br Conflicts of
2022-10-31

Disclaimer Conflicts of interest Role of the Sponsor Acknowledgements Funding/support: This project was supported by a grant from the Department of Surgery (R5129), Western University and by the Institute for Clinical Evaluative Sciences (ICES) Western site. ICES is funded by an annual g
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We conducted the largest drug screen to date in HPV
2022-10-31

We conducted the largest drug screen to date in HPV-positive cancers and identified Aurora kinase inhibitors as effective and understudied drugs in HNSCC and CESC. These drugs cause apoptosis and cell cycle arrest in vitro and decrease tumor size in vivo. This is the first published study to demonst
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ASK belongs to the family of MAPKKK ASK mediated
2022-10-31

ASK1 belongs to the family of MAPKKK. ASK1-mediated apoptosis is involved in the pathogenesis of several diseases such as I/R injury, infectious diseases and neurodegenerative disorders [33], [34], [35]. ASK1 can be activated through different mechanisms. One mechanism is that oxidative stress direc
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To further investigate the role of cholesterol
2022-10-31

To further investigate the role of cholesterol in the Rh2-induced cytotoxicity, we then focused on the U937 cell line, which is cholesterol auxotroph and considered as a valuable model to study the importance of cholesterol in membrane structure and function (Billheimer et al., 1987), and used the e
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