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The compounds were ranked based on the Glide XP
2021-06-07
The compounds were ranked based on the Glide XP Score, as shown in . All 15 compounds were subject to a radiometric assay previously used in our lab to evaluate their ability to inhibit DHFR steady-state activity in recombinant TS-DHFR (A). Compound demonstrated greater than 50% inhibition of DHFR
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DDR distribution in healthy fibrotic and inflamed tissues Wh
2021-06-07
DDR1 distribution in healthy, fibrotic and inflamed tissues Whereas we can easily mine publicly available databases to infer DDR1 expression profile in different tissues (as reported in Fig. 1), fine comprehension of DDR1 biology has been hampered by the absence of a commercially available specific
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conotoxin Several RNA BPs like the ELAV protein family membe
2021-06-07
Several RNA-BPs, like the ELAV protein family member HuR, tristetraprolin (TTP) or the KH-type splicing regulatory protein (KSRP) have been shown to interact with these AREs and thereby lead to stabilization or destabilization of the mRNA [5]. Control of nucleocytoplasmic mRNA export is also very i
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The notion that a small subset of inducible cellular transcr
2021-06-07
The notion that a small subset of inducible cellular transcripts, encoding immunological important factors, is translocated across the nuclear envelope by the karyopherin CRM1 is gaining support from various recent studies. For example, experimental evidence has been provided demonstrating that the
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br Involvement of p MAPK
2021-06-07
Involvement of p38 MAPK pathway The NF-κB signal transduction cascade is a major stress response signaling pathway for the COX-2 gene expression. In mice and humans, the COX-2 promoter has SB 265610 for many transcription factors, including NF-κB in the 5′ region of the COX-2 gene [11], and the
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3902 receptor Introduction The COMT gene is located on chrom
2021-06-07
Introduction The COMT gene is located on chromosomal band 22q11.2, extends over 28 kb, contains six exons, and encodes for catechol-O-methyl-transferase (Weinshilboum and Raymond, 1977; Grossman et al., 1992; Lundström et al., 1995; Bearden et al., 2005). This enzyme plays a major role in regulatio
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In order to validate the ATP competitive mode of inhibition
2021-06-07
In order to validate the ATP competitive mode of inhibition, compound 12 was selected as a representative inhibitor of this series, and the IC50 values were determined at eight different concentrations of compound 12 ranging from 0.001 to 100 μM, and repeated four times using different ATP concentra
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Perturbations in cell cycle are known to induce apoptosis Ou
2021-06-07
Perturbations in kn to nm australia are known to induce apoptosis. Our results show that a fraction of the DT40YB-1b+/− cells, in addition to becoming tetraploids, undergo apoptotic cell death. Similar observations linking polyploidy and apoptosis have been made in the past [23], [30], [31], [32],
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EPAC activation in VSMCs and ECs reverses several
2021-06-05
EPAC activation in VSMCs and ECs reverses several processes involved in the development of in-stent restenosis. Of particular relevance is the ability of EPAC1 to induce SOCS3 gene expression, as SOCS3 exerts multiple protective effects in both cell types, while immunohistochemical studies have show
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In vitro studies suggest that cPLA does not show
2021-06-05
In vitro studies suggest that cPLA2α does not show clear preference for the headgroup present at the sn-3 position, although a slight preference for zwitterionic phospholipids such as PC and PE has recently been pointed out [24]. In this regard, mass spectrometry analyses of glycerophospholipid hydr
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br Material and methods br Results br
2021-06-05
Material and methods Results Discussion The results show for the first time that DDRs may be involved in the pathogenic mechanisms of neurodegenerative diseases. We found that DDR1 and DDR2 levels are up-regulated in post-mortem AD and PD brains, suggesting that these receptors play a role
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In this report we describe
2021-06-05
In this report we describe studies of the effects of peroxisome proliferator-activated receptor γ (PPARγ) and acyl-CoA synthetase (ACSL1) on palmitate-induced ER stress in the human cardiomyocyte-like cell line AC16 [22], which was derived from adult ventricular heart tissue. PPARγ is a nuclear rece
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MJ33 lithium salt synthesis Despite the important agronomic
2021-06-05
Despite the important agronomic traits regulated by SUMO, most research studies on SUMOylation have been mainly limited to model plants, such as Arabidopsis and rice (Wang et al., 2011), due to the lack of molecular tools specific to other economically relevant plants. On the other hand, plants harb
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The Wnt signaling pathway has been demonstrated to be respon
2021-06-05
The Wnt signaling pathway has been demonstrated to be responsible for a variety of biological processes. The three best-characterized Wnt signaling pathways are the canonical Wnt pathway, the noncanonical planar cell polarity pathway, and the noncanonical Wnt/calcium pathway. The canonical Wnt/β-cat
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More recently Boskovic et al have visually corroborated
2021-06-05
More recently, Boskovic et al. (2003) have visually corroborated that purified DNA-PKcs can bind short DNA fragments by using single particle EM. DNA biotinylated at the 5′ end was labelled by coupling to commercial streptavidin–gold particles (Fig. 4D). When analysed in the microscope, DNA-PKcs mo
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