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To study the role of DNA PK
2019-11-30
To study the role of DNA–PK in the response to replication arrest, we used the DNA replication inhibitor aphidicolin (APH). APH, a mycotoxin isolated from Cephalosporium aphidicola, inhibits DNA replication by interacting with the replicating DNA polymerase α (pol α). APH specifically inhibits the a
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Since the initial identification of DNA ligase inhibitors by
2019-11-30
Since the initial identification of DNA ligase inhibitors by a structure-based approach [[18], [26]], there have been several reports describing LigI inhibitors using computer modelling and derivatives of the original DNA ligase inhibitors [[49], [50], [51]]. While these studies have shown that the
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Within the X CX PX RX motif of several prokaryotic
2019-11-29
Within the X1CX3PX5RX7 motif of several prokaryotic FGE substrates, the residues of X3, X5, and X7 are variably found as mixtures of alanine, glycine, threonine, or serine residues [26], [27]. The docked model of our identified HCTPRRP motif revealed that position X1 (H1) and position X7 (P7) were n
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Besides EGFR other tyrosine kinase receptors are
2019-11-29
Besides EGFR, other tyrosine kinase receptors are currently gaining attention as potential therapeutic targets. Included among these is the fibroblast growth factor receptor (FGFR) family, which is involved in the progression of a variety of cancers.7, 8, 9, 10, 11 In lung cancer, fibroblast growth
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Cancer patients may develop cachexia
2019-11-29
Cancer patients may develop cachexia, a deleterious wasting syndrome that is associated with muscle atrophy and has an impact on the well-being of patients and on the response to the treatment. Indeed, cachexia is a devastating and often irreversible syndrome observed in up to 80% of cancer patients
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br Introduction The stroma associated with breast cancer met
2019-11-29
Introduction The stroma associated with breast cancer metastasis consists of extracellular matrix (ECM) proteins, including fibrillar collagens, and a cellular component comprised of mesenchymal stem/multipotent stromal Licofelone (MSCs), vessels, and cells of the immune system (Pein and Oskarss
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br Results br Discussion Thus the biochemical
2019-11-29
Results Discussion Thus, the biochemical and structural studies of six Maf proteins from different organisms have revealed two subfamilies of new enzymes with the metal-dependent nucleoside triphosphate pyrophosphatase activity against both canonical and noncanonical pyrimidine nucleotides (Yh
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Contrary to genetic aberrations epigenetic methylation marke
2019-11-29
Contrary to genetic aberrations epigenetic methylation markers with broad coverage of OvCa subtypes were detected in primary tumors [21]. Ibanez de Caceres et al. [22] identified hypermethylation of BRCA1, APC, p16, p14, DAPK or RASSF1A in 50 of 50 primary tumors. Moreover the methylation pattern w
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br Chemistry The test compounds listed in Table
2019-11-29
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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br Methods br Results br Discussion I R induces oxidative
2019-11-29
Methods Results Discussion I/R induces oxidative stress and increases the intracellular levels of ROS, resulting in tissue damage [31]. ROS is generated by mitochondrial electron transport chain, nicotinamide ataluren dinucleotide phosphate (NADPH) oxidase complex, xanthine oxidase and NOS
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Itch also known as astrophin
2019-11-29
Itch, also known as astrophin-1 interacting protein-4 (AIP4), is a HECT domain-E3 ligase. It was discovered in 1998 in mouse coat color genetic studies which displayed the disruption caused by the Itch gene inducing a lethal autoimmune inflammatory condition. The substrates of Itch are transmembrane
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Although our knowledge of the biochemical and biological fun
2019-11-29
Although our knowledge of the biochemical and biological functions of E3 ubiquitin ligases has increased in B-cell malignancies, a deeper characterization of cell-context dependent substrate regulation and biological relevance is needed. The recent approval of a general proteasome inhibitor, VELCADE
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These data from developing brain are in
2019-11-29
These data from developing CTX0294885 are in contrast to noradrenergic receptor regulation in the adult brain. In adult animals, a persistent increase in the α2-AR high affinity state is elicited as a result of DSP-4 lesion or reserpinization, as measured by [3H]clonidine binding to membrane prepar
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Defensins are one major class of antimicrobial cationic pept
2019-11-28
Defensins are one major class of antimicrobial, cationic peptides that are released from Pseudo-UTP and imbedded in the mucus layer on mucosal surfaces [45]. They can be categorized into two major families; α- and β-defensins. In humans there are two α-defensin members, defensin 5 (HD5) and defensi
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As previously stated the most unexpected finding from this
2019-11-28
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 understa
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