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Finally considering the encouraging inhibitory and selectivi
2020-10-26
Finally, considering the encouraging inhibitory and selectivity properties of compound and against isolated CK1δ, we have also acquired a very preliminary cytotoxicity profile on human ovarian carcinoma cell line (2008) and on its cisplatin-resistant clone (C13). Results showed that after 48h of e
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br Discussion This study characterized longitudinal changes
2020-10-26
Discussion This study characterized longitudinal changes of cholinesterase and PON1 enzyme activities in greenhouse workers over two periods of a crop season with different levels of pesticide exposure. Although study participants were not exposed to OP insecticides, because they worked under int
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We have previously reported the characterization of A
2020-10-26
We have previously reported the characterization of A-127722, a novel, non-peptide endothelin antagonist that displays very high affinity binding (K=69 pM) with a more than 1000-fold greater affinity for human endothelin ETA than ETB receptor. Although A-127722 is >1000-fold more selective for endot
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Another interesting finding regarding substrate selectivity
2020-10-26
Another interesting finding regarding substrate selectivity of iPLA2-VIA in whole cellular systems stems from the observation that some of the major species hydrolyzed by the enzyme contain a 16:1 fatty hsp90 inhibitor at the sn-2 position [57,119], raising the possibility that iPLA2-VIA may consti
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EDTA br Roles of DDR in epithelial cell differentiation br R
2020-10-26
Roles of DDR1 in epithelial cell differentiation Roles of DDR1 in cell migration, and invasion Dichotomous functions of DDR1 in disease progression Conclusions and perspectives The switch in EDTA from DDR1 to DDR2 during EMT is another important issue. The DDRs may exert distinct or red
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br Conclusions br Introduction The terms endocrine
2020-10-26
Conclusions Introduction The terms endocrine active and endocrine disruptive have been used to describe an ever-expanding list of naturally-occurring and synthetic compounds that interact with mammalian hormonal systems, and in particular, the reproductive system. These compounds have been ass
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br Acknowledgements The authors thank
2020-10-26
Acknowledgements The authors thank Drs. C. Klein, I. Canisso and A. Claes with assistance in obtaining tissues. Supported by the Albert G. Clay Endowment, University of Kentucky. Introduction Neoplastic cells often develop drug resistance during tumor progression or cancer treatment (Turner a
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An important role for the precursor molecule of the main
2020-10-26
An important role for the precursor molecule of the main EBI2 ligand, 25-OHC, in the inhibition of inflammation was recently shown. 25-OHC was demonstrated to inhibit inflammasome induction in mouse macrophages [28]. Inflammasome assemblies are the sites of caspase 1 activation and lead to the gener
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br Introduction O Methylguanine DNA methyltransferase
2020-10-26
Introduction O6-Methylguanine-DNA methyltransferase (MGMT) is a DNA-repair enzyme that specifically transfers alkyl adducts from the O6 position of guanine to the cysteine residue (Cys145) in its active site. In cancer cells, this ability of MGMT disrupts the cytotoxic actions of alkylating antic
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Due to the high attractiveness of E and E ligases
2020-10-26
Due to the high attractiveness of E2 and E3 ligases as drug targets, a number of drug discovery assays have been published, based on detection by fluorescence (Dudgeon et al., 2010, Krist et al., 2016, Zhang et al., 2004), FITC, Fluorescein isothiocyanate (Davydov et al., 2004, Huang et al., 2005,
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br Results The AR genotype frequencies are shown in
2020-10-26
Results The AR genotype frequencies are shown in Table 1. Alleles at the two loci are in linkage disequilibrium, as expected for such closely linked loci and consistent with previous findings (Kittles et al., 2001). The genotype frequency for the DBH 1021 polymorphism is similar to previous find
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Our results indicate a deregulation of DNA methylation machi
2020-10-26
Our results indicate a deregulation of DNA methylation machinery during seed development in apomixis. Since DRM2 is targeted loci through an RNA-directed DNA methylation (RdDM) pathway involving 24-nt siRNAs (Stroud et al., 2014, Law and Jacobsen, 2010) and differentially expressed between apomict a
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cmv br Materials and Methods br
2020-10-26
Materials and Methods Acknowledgements Introduction Collagen fibrillogenesis, the assembly of collagen fibers, is a critical process in the development, maturation, and repair of mammalian tissue. Alterations in the structure and amount of deposited collagen fibers can greatly alter the int
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In Hevea brasiliensis both the
2020-10-26
In Hevea brasiliensis, both the soluble PPase and the membrane-bound V-PPase are present in the latex; the soluble PPase is in the C-serum (cytosol) of the latex [6] and the V-PPase is on the tonoplast of the lutoid, a special vacuole in the laticifers of rubber trees [7]. The V-PPase on the lutoid
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The requisite extended benzyl alcohols and and final
2020-10-26
The requisite extended benzyl alcohols –, , and and final potential DFG-out binding hybrid inhibitors – and – were prepared as shown in , . Benzaldehyde was alkylated with -methoxybenzyl chloride and then reduced with sodium borohydride to give benzyl alcohol . Pyridine derivative was prepared by
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