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bwx Despite the fact that the precise
2019-08-17

Despite the fact that the precise relevance of Ube2E self-ubiquitination in vivo is still elusive, findings of Sarkari et al. do establish Ube2E1 ubiquitination in bwx [36]. In vivo self-ubiquitination of Ube2E1 is further supported by the high-throughput study aimed to identify all ubiquitinated p
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QSAR based on the D structures of ligands plays an
2019-08-16

QSAR based on the 3D structures of ligands plays an important role in the ligand-based drug discovery and design [12]. Comparative molecular field analysis, CoMFA [11], and comparative molecular similarity index analysis, CoMSIA [12] are among the most popular QSAR models. They focus on changes in 3
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There is literature precedence for the
2019-08-16

There is literature precedence for the metabolic activation of the methylene carbons adjacent to the ring oxygen(s) of dioxanes and benzopyrans resulting in ring-opened electrophilic carbonyl species. Based on the potential for this metabolic pathway being operative with , a steric block approach wa
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Several highly selective COX inhibitors
2019-08-16

Several highly selective COX-2 inhibitors (coxibs) have been reported and marketed [6], including celecoxib [7] and etoricoxib [8] (Fig. 1). Even though these drugs produce less ulceration than conventional NSAIDs, coxibs still produce significant gastric and cardiovascular side effects due to the d
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E is encoded by the largest
2019-08-16

E1 is encoded by the largest and most conserved open-reading frame (ORF) of the PV genome. The protein ranges in size from 600 to 650 amino acids, depending on the PV type. Overall, the protein can be divided into three functional segments: an N-terminal regulatory region that is essential for optim
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Haj Yahya et al applied native chemical ligation for the
2019-08-16

Haj-Yahya et al. [52] applied native chemical ligation for the construction of diubiquitin probes. They attached a cysteine residue to the lysine side chain of the proximal ubiquitin and ligated the distal module using the C-terminal thioester of ubiquitin. Elimination of the sulfur Luciferase Repor
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br Conclusion From the series of synthesized N
2019-08-16

Conclusion From the series of synthesized N-methylated and N-benzylated pyrimidinediones, it may be concluded that the presence of electron rich species with pyrimidinediones is vital for enhancing binding with target, although, incorporation of steric bulky group must be taken into consideration
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Experiments on the rat model of
2019-08-16

Experiments on the rat model of E. coli pyelonephritis, performed to investigate the relationship between the acute inflammatory processes and the permanent kidney damage (Brooks et al., 1974), have demonstrated a positive correlation between the degree of free radical-mediated renal injury and the
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br P Y receptor structure br Pharmacology Several
2019-08-15

P2Y receptor structure Pharmacology Several subtype selective compounds have been developed in recent years (Jacobson and Müller, 2016; Rafehi and Müller, 2018). These compounds are helpful tools for analyzing the roles of P2Y receptor subtypes in physiology and pathophysiology. The present ar
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br Materials and methods br Results br Discussion We initial
2019-08-15

Materials and methods Results Discussion We initially found that ISL, a natural product with a linear scaffold (2-propenone), is able to inhibit CK2 (IC50 = 17.3 μM). Then we have investigated the inhibitory potential of a novel series of compounds with linear scaffolds by combining fragmen
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Our previous work has demonstrated that two glutamate
2019-08-15

Our previous work has demonstrated that two glutamate residues (Glu-305 and Glu-331 in murine and human TPP II) in the active site are important for exopeptidase activity in mTPP II [17]. At least one of these, Glu-331, seems to form a salt bridge to the N-terminal amino group of the substrate, posi
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br Acknowledgements We would like to thank Dr Ron Mason
2019-08-15

Acknowledgements We would like to thank Dr Ron Mason (NIEHS, Research Triangle Park, NC) for helpful discussion regarding the analysis of CCl4 metabolism, to Dr Karla Thrall and Dr Rick Corley (Battelle) for helpful discussions regarding study design and data interpretation, and to Jim Merdink an
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Homologous recombination HR has important roles in
2019-08-15

Homologous recombination (HR) has important roles in the repair of stalled or collapsed DNA replication forks, as well as of DNA double-strand breaks. Among the factors required for HR in human angiotensin ii are RAD51, BRCA1, and BRCA2 (Davies et al., 2001, Sung and Klein, 2006, Xia et al., 2001).
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br Introduction The stroma associated with breast
2019-08-15

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 Embelin powder (MSCs), vessels, and cells of the immune system (Pein and Osk
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Anaesthetized mice of one eNOS KO strain showed a paradoxica
2019-08-14

Anaesthetized mice of one eNOS-KO strain showed a paradoxical decrease in blood pressure (BP) in response to i.p. administration of the NOS-inhibitor L-NA suggesting a role for non-endothelial isoforms of NOS in maintaining BP [1]. Alternatively, diminution in the activity of the renin-angiotensin s
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