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With a favorable spectrum of
2021-07-02
With a favorable spectrum of CRTh2 dependent in vitro and in vivo efficacy demonstrated, the off-target activity of compound 18 was investigated, first against a panel of prostanoid receptors and related eicosanoid targets (Table 8), where no significant activities at 10μM concentration were found i
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p Kip is a critical
2021-07-02
p27Kip1 is a critical component of the cell cycle machinery [15]. As an inhibitor of cyclin E-Cdk2, p27Kip1 plays a pivotal role in controlling cell proliferation, S-phase entry, and G1-phase exit during development and tumorigenesis [16]. p27Kip1 is predominantly regulated via posttranslational mod
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br Acknowledgements We thank Jeus Perez Clausell from the De
2021-07-02
Acknowledgements We thank Jeus Perez-Clausell from the Department of Cell Biology, School of Biology, University of Barcelona, Felipe Casanueva's group from the Department of Molecular Endocrinology and Carlos Diéguez's group from the Department of Physiology, School of Medicine, University of Sa
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The regression also revealed a significant
2021-07-02
The regression also revealed a significant association between admission selectivity (SELECT) and exam pass rate (PASS%) (p prostaglandin receptor serve as an indicator of a student’s ability to learn and their aptitude for academic success. These same qualities likely enable more selective schools
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In the last and the most challenging part three mixtures
2021-07-02
In the last and the most challenging part, three mixtures were selected to evaluate the reliability of the presented correlation and the CPA model. For Athabasca bitumen, Amani et al. [25] measured the experimental data at very high temperatures compared to the thermal recovery range up to 644 K (ne
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Interestingly Carver Johnson and Kim investigated a
2021-07-02
Interestingly, Carver, Johnson, and Kim (2016) investigated a polymorphism in the OPRM1 μ-opioid receptor gene for its role in sensitivity to social contexts. The G allele of this polymorphism was associated with higher levels of sensitivity. The authors found significant interactions, e.g. the nega
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Recently pharmacological studies have revealed
2021-07-02
Recently, pharmacological studies have revealed that natural compounds achieve increasing attention due to its high therapeutic effectiveness and low adverse effect, compared with the chemically synthesized compounds. Emodin is a kind of natural anthraquinone derivative enriched in traditional Chine
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Radicicol The inhibition of CYP activity by NOR
2021-07-02
The inhibition of CYP11β activity by NOR was 11- and 2.5-fold higher than those reported for the antifungal agents ketoconazole (IC50: 4.4μM) and clotrimozole (IC50: 1.0μM) (Fernandes and Porte, 2013). Furthermore, NOR was able to inhibit P450 aromatase activity in carp ovaries, although at a rather
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Another potential source of variable affinities is inherent
2021-07-02
Another potential source of variable affinities is inherent in the method of RBA determination. While several reports simply use relative IC50 values as RBAs [11], [12], [13], [14], [15], these are only an approximate measure of relative affinity since IC50 varies due to experimental and biological
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Our previous high throughput screening HTS campaign using au
2021-07-02
Our previous high-throughput screening (HTS) campaign using automated, robust, and sensitive fluorescence based NAD/NADH Quantitation Colorimetric Kit synthesis assay [10], [11] led to the identification of several EPAC specific inhibitors (ESIs), and was subsequently followed by extensive hit-to-le
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The endothelin receptor type B EDNRB belongs to
2021-07-02
The endothelin receptor type B (EDNRB) belongs to the family of G protein-coupled receptors, which functions as a vital regulatory factor in signal transduction in cells, locating on human chromosome 13q22.3 (Ayala-Valdovinos et al., 2016; Bregar et al., 2018; Morimoto et al., 2018; Widowati et al.,
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In terms of its protease activity
2021-07-02
In terms of its protease activity, MME has a broad range of substrates being able to target glucagon, bradykinin, GLP1, and several other BG45 of circulating small molecules [25]. MME has been shown to target free insulin B-chain [32], although whether MME could target and degrade the insulin recep
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Molecular modelling studies were performed on
2021-06-29
Molecular modelling studies were performed on the hDHFR inhibitors identified (1, 11, 13, 14, 16, 25 and 32) to explore the structural basis of the interaction between the mentioned compounds and the human enzyme. The docking studies were performed using the X-ray crystallographic structure of the h
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Industrial fermentation aims to produce valuable products fr
2021-06-29
Industrial fermentation aims to produce valuable products from cheap feedstocks by utilizing diverse microbial functions through aerobic or anaerobic fermentation [[8], [9], [10]]. During anaerobic fermentation, the reducing power is mostly directed to product synthesis rather than being oxidized, r
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The goal of this paper is to
2021-06-29
The goal of this Dihydroartemisinin paper is to investigate the penalized empirical likelihood method for the Cox model, as a competitor to the penalized partial likelihood. Since empirical likelihood (EL) was proposed by Owen, 1988, Owen, 2001, empirical likelihood methods have been investigated w
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