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C PHNO has been described as
2020-09-14
[11C]-(+)-PHNO has been described as a full agonist at both D2 and D3 receptors [54,55]. [11C]-(+)-PHNO was initially developed as a PET radiotracer for imaging the high affinity state of the D2 receptor (i.e., highD2) as a means of measuring synaptic dopamine changes in response to pharmacologic ch
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A An optimized BEI SEIscore based
2020-09-14
(A) An “optimized BEI-SEIscore” based on the trends, emerged from the statistical analysis of several optimization studies in pharmaceutical industry (Abad-Zapatero, 2007, Abad-Zapatero and Blasi, 2011). This type of optimized scores has been used in many previous studies. Ki=1nM at 300° K, compare
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Funding sources This study was funded by European
2020-09-14
Funding sources This study was funded by European Community’s Seventh Framework Programme under grant agreement No. 305662 (Project: Community-based scheduled screening and treatment of malaria in pregnancy for improved maternal and infant health: a cluster-randomized trial ‘COSMIC’). Acknowledg
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br MCADD review br Funding None br Introduction
2020-09-14
MCADD review Funding None. Introduction Bacteroides species are obligate anaerobes, Gram-negative, and non-spore-forming bacteria and 21 species of this genus are found particularly in the oral cavity and gastrointestinal tract in vertebrates [1,2]. B. fragilis is the most common annexin v
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Aspergillus nigerA niger is another filamentous fungus
2020-09-14
Aspergillus nigerA. niger is another filamentous fungus, in which alternative dehydrogenases have been described. Filamentous fungi are a very important group of microorganisms that are used in industry (O’Donnell et al. 2011). Biotechnological production processes using these organisms are often hi
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artesunate br Materials and methods br Results Metabolic
2020-09-14
Materials and methods Results Metabolic stability of compounds was studied by incubation with pooled human liver microsomes. Piperine was the metabolically most stable compound, with a t1/2 of 141min (Fig. 2, and Table 1). SCT-29 and LAU 397 showed t1/2 of approx. 45min, whereas a t1/2 of only
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br Conclusion CSF R may contribute to limitation of targeted
2020-09-14
Conclusion CSF-1R may contribute to limitation of targeted therapies by providing EGFR-bypassing signals that support proliferation. Multi-kinase inhibitors such as cabozantinib are available, and agents targeting CSF-1R are in clinical trials, however, at present, as inhibitors of tumor-associat
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To simulate the inhibition of the enzyme by organophosphorus
2020-09-11
To simulate the inhibition of the enzyme by organophosphorus, carbamate insecticides or nerve agents, a reversible cholinesterase inhibitor physostigmine was used for most experiments for safety reasons. However, the results of the measurements were verified using the soman organophosphate, which is
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ClC is not only a chloride ion channel but also
2020-09-11
ClC-3 is not only a chloride ion channel but also a regulatory protein involved in the regulation of multiple signaling pathways. The PI3K/AKT/mTOR signaling pathway plays a crucial role in regulating cell growth, migration, invasion, and distant metastasis [13,14]. Although abnormal PI3K/AKT/mTOR a
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Dose response analysis Fig can be performed on cells in
2020-09-11
Dose response analysis (Fig. 2) can be performed on KU55933 in culture, in tissue, in animals or even in patients. Many different responses can be measured, including mRNA levels, reporter gene activity, gene product (e.g. enzyme) activity or even physiological functions such as inhibition of ovulat
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In the present study we examined whether the gene for
2020-09-11
In the present study we examined whether the gene for estrogen receptor alpha, Esr1, plays a role in the expression of maternal memory in female rats. The approach utilized a newly developed rat Esr1 knockout (KO) rat model (Rumi et al., 2014) to evaluate whether deletion of the Esr1 DIDS affected t
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br Chemistry The test compounds listed in
2020-09-11
Chemistry The test compounds listed in Table 1, Table 2, Table 3, Table 4, Table 5, were synthesized as outlined in Scheme 1, Scheme 2, Scheme 3, Scheme 4, Scheme 5. Synthesis of 2–5 is described in Scheme 1. N-Sulfonylation of the aniline 26 with benzenesulfonyl chloride afforded the sulfonamide
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In our current work we have undertaken liquid phase combinat
2020-09-10
In our current work, we have undertaken liquid phase combinatorial synthesis methods for the synthesis of 1,2,5-trisubstituted benzimidazole derivatives as hDHODH inhibitors. Synthesised Cyanine 5-dUTP were also screened by molecular docking studies over the reported hDHODH structure. The synthesis
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br Acknowledgments This work was funded by the EU
2020-09-10
Acknowledgments This work was funded by the EU ERDF and the Spanish Ministry of Economy and Competitiveness (MINECO) under Project TIN2013-41576-R, and the Spanish Ministry of Education, Culture and Sport (MECD) under a FPU grant (AP2010-3259), and the Andalusian Regional Government (Spain) under
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We have previously reported that CK is
2020-09-10
We have previously reported that CK2 is downregulated in senescent human lung fibroblast IMR-90 cells, aged rat tissues, and aging nematodes [17,18]. CK2 downregulation induces cellular senescence via the PI3K-AKT-mTOR-reactive oxygen species-p53-p21Cip1/WAF1 pathway in human cells [[19], [20], [21
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