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In light of the overall loss
2020-09-18
In light of the overall loss of activity and selectivity observed with this series of arylchromenone-4-ones bearing small -alkoxy substituents, we were pleased to identify a potent and relatively selective inhibitor , exhibiting IC values of 0.008μM and 0.07μM for DNA-PK and PI3Kα, respectively. The
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Furthermore Survivin is a member of the inhibitor of
2020-09-18
Furthermore, Survivin is a member of the inhibitor of apoptosis family. IR induces a rapid nuclear accumulation of survivin and subsequent phosphorylation of the protein in the nucleus. Co-immunoprecipitation and immunofluorescence co-localization analyses revealed an interaction among survivin, Ku7
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br Methods for assessing TLS While
2020-09-18
Methods for assessing TLS While the precise quantification of restricted DNA synthesis events is possible (e.g. unscheduled DNA synthesis (UDS) reveals NER), so far, it is impossible to identify TLS stretches of only a few nucleotides within the background of bulk DNA replication of normal DNA. N
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br Structural and biochemical features of pol X family
2020-09-18
Structural and biochemical features of pol X family polymerases The X-family DNA polymerase (polX) is specialized in DNA repair. This family is composed of four different DNA polymerases: pol β, pol λ, pol μ and TdT. Only three members of the polX family possess an N-terminal BRCT (BRCA1 carboxy-
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br Conclusions In this paper we describe the recombinant
2020-09-18
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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Beyond phosphorylation cancer cells may alter pyrimidine bio
2020-09-18
Beyond phosphorylation, cancer XCT790 may alter pyrimidine biosynthesis through the activation of the proto-oncogenic transcription factor MYC. MYC is a master regulator of many different pathways and has significant influence on the expression of nucleotide metabolism genes. Previous studies have s
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In this context we initiated a program to
2020-09-18
In this context, we initiated a program to develop new antiviral chemotypes towards a host factor implicated in dopamine antagonist drugs replication: the host (human) dihydrofolate reductase (DHFR) [21]. We recently identified this enzyme as the molecular target of 1-aryl-4,6-diamino-1,2-dihydrotr
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CGK733 Interaction between neutrophils and ECs represents th
2020-09-18
Interaction between neutrophils and ECs represents the first step of the cellular phase of the inflammatory response, and provide the best condition for the transfer of the PMNL-derived LTA4 to the ECs, leading to the transcellular formation of cysteinyl-LTs. It is intriguing therefore to think that
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Several highly potent CysLT receptor antagonists with large
2020-09-18
Several highly potent CysLT1 receptor antagonists with large structural (-)-p-Bromotetramisole Oxalate have been developed. Beyond antagonists with structures analogous to cysteinyl leukotrienes, other subclasses comprise: (a) hydroxyacetophenones, (b) indoles and indazoles, (c) quinolines, benzoth
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Since its inception ADEPT approach has been
2020-09-17
Since its inception, ADEPT approach has been widely reported by many groups using a variety of enzymes and prodrugs (see reviews) [12], [14]. Both mammalian and non-mammalian enzymes have been utilised. Of the mammalian variety, human β-glucuronidase in combination with many prodrugs [17], [18] and
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The use of AACSB accreditation as an indicator
2020-09-17
The use of AACSB accreditation as an indicator of expected performance on the CPA exam has been examined by prior studies (e.g. Barilla et al., 2008, Boone et al., 2006, Grant et al., 2002, Howell and Heshizer, 2006, Lindsay and Campbell, 2003, Marts et al., 1998). While these studies are based on d
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br The LSCP model and its
2020-09-17
The LSCP model and its properties In this section, we first introduce the LSCP model in Section 2.1. Some examples of the model are presented in Section 2.2 and basic properties of the model are presented in Section 2.3. Finally, Section 2.4 introduces finite dimensional approximations necessary
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PF-4708671 br Functional significance Defects of the lysyl h
2020-09-17
Functional significance Defects of the lysyl hydroxylases LH1, LH2, and LH3 impair collagen secretion and stability in the extracellular matrix, and cause rare connective tissue disorders such as Ehlers-Danlos type-VI [27], Bruck syndrome [28], and skeletal dysplasia [29], respectively. Elucidati
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UVRAG is a mammalian ortholog of yeast
2020-09-17
UVRAG is a mammalian ortholog of yeast Vps38 and a promoter of autophagy [51,60,61]. It forms distinct complexes with BECN1 (mammalian ortholog of yeast Vps30/Atg6) and the class III phosphatidylinositol 3-kinase (whose catalytic subunit [PIK3C3] is the mammalian ortholog of yeast Vps34) and contrib
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Enlarging the ligand binding pocket by reduction
2020-09-17
Enlarging the ligand-binding pocket by reduction of the size of the residue F435 switched DES to an agonist indicating that F435 is involved in mediating the antagonistic effect of DES (Fig. 7E) [13]. The conformation of the smaller side chain of L435 was either not altered by DES or was too small t
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