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br Materials and methods br Results br Discussion
2019-12-06
Materials and methods Results Discussion Cisplatin, as one member of a class of platinum-containing anti-cancer drugs, which displays a great deal of clinical activity on a wide variety of solid tumors. In addition, cisplatin often used in combination with other chemotherapy drugs to treat
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PKA signalling in the nucleus was thought
2019-12-06
PKA signalling in the nucleus was thought to be due to the translocation of the catalytic subunit upon activation from the sphingosine 1-phosphate receptor modulator to the nucleus via diffusion [72]. However, a new understanding has emerged, as both the regulatory and catalytic subunits have been
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Multiple protein species are known to
2019-12-06
Multiple protein species are known to naturally exist for the transmembrane receptors DDR1 and DDR2. Five splice variants have been characterized for DDR1 (“a” through “e”). The d and e isoforms lack the intracellular kinase domain of DDR1. The splicing of DDR1 to various extents has been reported i
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In principle in vitro techniques
2019-12-06
In principle, in vitro techniques for assessing enzyme induction might include the use of cultured hepatocytes, precision-cut liver slices, immortalized mglur lines (such as those derived from hepatomas) and reporter gene constructs (where appropriate cells are transfected with recombinant DNA enco
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To assess whether the described cooperation between
2019-12-06
To assess whether the described cooperation between the EGFR and FGFR receptors was relevant at the clinical level, we determined the effect on progression-free survival of FGFR1 expression in patients with adenocarcinoma who were receiving erlotinib or gefitinib. As we had observed EGFR-FGFR1 coope
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One step in pyrimidine biosynthesis is conversion
2019-12-06
One step in pyrimidine biosynthesis is conversion of l-dihydroorotate (DHO) to orotate (ORO), under action of the enzyme dihydroorotate dehydrogenase (DHODH, EC 1.3.99.11), which contains a flavine (FMN) as redox cofactor [1]. In this transformation, electrons resulting from DHO oxidation are transf
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Oxybutynin synthesis br Materials and methods br
2019-12-06
Materials and methods Results Discussion DDR2 played a role in cell motile behavior, but the relationship between motility and collagen activation of DDR2 tyrosine kinase was unclear. Studies with smooth muscle cells from DDR1−/− mice demonstrated a defect in cell attachment to collagen and
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br Cysteine proteases as molecular
2019-12-06
Cysteine proteases as molecular targets for trypanosomatid diseases Approaches relying on a molecular target, such as SBDD and target-based screening, have supported outstanding scientific developments in current pharmaceutical R&D. By integrating experimental and computational methods, these str
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The CysLT receptor antagonist BayCysLT RA significantly
2019-12-06
The CysLT2 receptor antagonist BayCysLT2RA significantly suppressed multiple antigen challenge-induced infiltration of eosinophils and mononuclear Iloperidone into the lung, indicating that CysLT2 receptor activation is involved in leukocyte migration. In contrast to the present finding, Barret et
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More recently Boskovic et al have
2019-12-05
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 mol
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We recently described the benzoxazin one analogue
2019-12-05
We recently described the 1,3-benzoxazin-4-one analogue of LY294002 and showed it to have pan-PI3K and DNA-PK activity [2]. We have also reported on the activity of other family members, such as 3 which causes sensitization of lung cancer and colon cancer cells to radiation [11] and 4 (LTUSI122) as
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br Conclusions In this paper
2019-12-05
Conclusions In this paper we describe the recombinant expression and characterization of ParI, a C5-DNA-MTase from P. arcticus 273–4. To our knowledge, this is the first characterization of an orphan C5-DNA-MTase from a psychrophilic bacterium. The C5-DNA-MTase could not be expressed in regular E
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Although several genomic technologies including the
2019-12-05
Although several genomic technologies, including the generation of ERRγ-specific knockout mice, have revealed that ERRγ plays a pivotal role in cellular bioenergetics [1], its involvement in other metabolic pathways has been appreciated only recently. Therefore, we highlight recent findings on the r
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Considering these reports and with the aim of further
2019-12-05
Considering these reports, and with the aim of further investigating the mechanism by which the cAMP-Epac/PKA pathway activates eNOS, we have performed imaging experiments evaluating the effect of drugs that increase cAMP or modify its signalling pathways (PKA or Epac activators and inhibitors) on b
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To provide a brief critical
2019-12-05
To provide a brief critical evaluation of this technology and an outlook, we note that performance of SMEPT is critically dependent on each of the components making up this platform, namely the substrate, the enzyme, and the prodrug. With regards to the latter, SMEPT is built on the experience and s
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