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br Acknowledgment br Introduction Pesticides are largely
2020-03-31
Acknowledgment Introduction Pesticides are largely used in agriculture to enhance food production and, to a lesser extent, to control unwanted pests and disease vectors in public health. However, these compounds are often associated with toxicity in non-target species including humans. Occupat
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br Allosteric inhibitors In general candidate
2020-03-31
Allosteric inhibitors In general, candidate drugs that bind to a GPCR at a site that is distinct (allosteric site) from the binding site of the endogenous agonist (orthosteric site) are attracting increasing attention 39, 42, 58. Allosteric modulators display saturability of their effect, probe d
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br Clinical studies br Practical implications
2020-03-31
Clinical studies Practical implications for young women Conclusion Research on the oncogenic mechanism of hormones has advanced dramatically in the latter years. The finding that progestogens are more powerful determinants of risk than estrogens in breast cancer has been added to advances i
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br In addition to the classic nuclear genomic
2020-03-31
In addition to the classic nuclear genomic action, estrogens have been found to induce rapid effects occurring within minutes following administration. These effects are mediated through a subpopulation of estrogen receptors associated with the plasma membrane, a process usually termed “membrane-i
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br Diverse functions of ERK
2020-03-31
Diverse functions of ERK pathway Same as the other MAPK cascades, the ERK pathway is activated by several extracellular stimuli and different internal routes. ERK vitally tunes the function of various substrates in all cellular components; the nucleus, cytoplasm, membranes and the cytoskeleton. E
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The present study was set to characterise the
2020-03-31
The present study was set to characterise the DNMT gene orthologs and describe the expression patterns of these genes during seed development in natural diploid apomict B. divaricarpa and diploid sexual B. stricta. Material and methods Results The B. stricta genome v1.2, was sequenced and ass
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While the mechanism of DHODH inhibition induced differentiat
2020-03-31
While the mechanism of DHODH inhibition-induced differentiation is not fully understood, this phenomenon may be caused by pyrimidine depletion. Pyrazofurin, an inhibitor of OMP decarboxylase, was able to induce differentiation and suggests pyrimidine depletion as a potential mechanism (Sykes et al.,
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It is not precisely known which of the
2020-03-31
It is not precisely known which of the intramolecular interactions created by the SH2 domain, the SH3–SH2 linker and the SH2–kinase linker are essential for the catalytic activity of Csk or how these interactions regulate Csk activity. Thus far it has been shown that site-directed mutagenesis of SH
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Next our exploration shifted to modifications at the lateral
2020-03-30
Next, our exploration shifted to modifications at the lateral chain of the benzoquinone nucleus (SAR 2). Considering that the CK2 inhibitory activity is favoured by the presence of the -Ph-4-NO2 (SAR 1), the subsequent analogues were investigated with this moiety retained. The influence of the side
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In the next experiments using a Cell Stress
2020-03-30
In the next experiments, using a Cell Stress Array kit we assessed the effect of mixture of progestogens on the expression of 26 proteins. One group of proteins including PON3, Phospho-p38a, SIRT2, SOD2, HIF-1 alpha, HIF-2alpha and p27 were upregulated upon progestogen treatment. HIF-1 functions as
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br Structure and function of EPAC isoforms EPACs are
2020-03-30
Structure and function of EPAC isoforms EPACs are guanine nucleotide exchange factors (GEFs) for the Ras-like GTPases Rap1 and Rap2 [9]. There are two mammalian EPAC isoforms, EPAC1 and EPAC2 1, 2 (Figure 1). Whereas EPAC1 displays a wide tissue distribution, the expression of EPAC2 is more restr
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Nimodipine administration also inhibited the eIF ATF singnal
2020-03-30
Nimodipine administration also inhibited the eIF2α/ATF4 singnaling which is a crucial evolutionarily conserved adaptive pathway during cellular stresses including hypoxia and ischemia (Evans et al., 2016; Manwani and McCullough, 2013). While, the eIF2a/ATF4 pathway, activated by different forms of s
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DGK type I http www apexbt com media
2020-03-30
DGKη1 (type II DGK) has a separated catalytic domain [10], [13], whereas the domains of DGKα, ε and ζ are not split [1], [2], [3], [4], [5]. Therefore, the structural difference may cause the distinct affinity for DG among these isozymes. Because other type II DGKs (η2, δ1, δ2 and κ) also have the s
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Confidence with which data of
2020-03-30
Confidence with which data of animal safety/toxicity studies can be translated to human depends upon the knowledge that whether humans would be exposed to similar chemical entities (parent and its metabolites) as the animals exposed during toxicity studies. In this regard, in vitro qualitative evalu
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As previously stated the most unexpected finding from this
2020-03-30
As previously stated, the most unexpected finding from this series of compounds was the identification of a dimethyl isoxazole side chain that gave dramatically improved binding over the parent compounds. Holding this piece of the molecule constant, a series of analogs were made to further understan
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