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br RING type E s and
2019-11-18
RING-type E3s and their substrates There is enormous diversity in substrate ubiquitination and its regulation, as the targets of RING-type E3s are incredibly varied. RING-type E3s are implicated as tumor suppressors, oncogenes, and mediators of endocytosis, and play critical roles in complex mult
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CDK lacks DNA binding domains and nuclear localization seque
2019-11-18
CDK6 lacks DNA-binding domains and nuclear localization sequences, and therefore will probably be transported to the nucleus by a ‘piggy-back’ mechanism and needs to contact its specific sites indirectly through DNA-binding proteins. Besides NF-κB p65, a further candidate transcription factor is PAX
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Three kinase inhibitors dasatinib type I imatinib type II
2019-11-18
Three kinase inhibitors dasatinib (type I), imatinib (type II) and nilotinib (type II), identified initially as inhibitors of tyrosine kinase BCR-ABL, were found to target DDRs in a chemical proteomic profiling study (Bantscheff et al., 2007, Hantschel et al., 2008). These tyrosine kinase inhibitors
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Experimentally measured DGAT activity was
2019-11-18
Experimentally measured DGAT activity was first reported by Weiss et al. (1960) and several different types of DGAT enzyme have since been described in plants [12,41,42]. As recently as 2011 there appeared to be just two DGAT enzymes both in plants and in other eukaryotes, namely DGAT1 and DGAT2 [43
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The phenolic hydroxyl group of ezetimibe tolerated various s
2019-11-18
The phenolic hydroxyl group of ezetimibe tolerated various structural modifications (disaccharide, carboxyalkyl and glucuronide) that retained inhibitory activity.13, 14, 15 We conjugated glycylglycine to phenolic hydroxyl group and synthesized ten 1H-pyrrole-2,5-dione derivatives 14a-j successfully
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In summary A is a potent orally
2019-11-18
In summary, A-216546 is a potent, orally available endothelin receptor antagonist with a high selectivity for the endothelin ETA receptor. The potency and bioavailability of A-216546 suggest that it will have important utility for preclinical evaluation of the pathophysiology of the endothelin syste
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A growing body of data indicates
2019-11-18
A growing body of data indicates that endothelial NOS (eNOS) is a rate-limiting enzyme for the synthesis of nitric oxide (NO), its downstream SANT-1 australia molecule. High pathological concentrations of NO produced from inducible NO synthase (iNOS) induce apoptosis, whereas a reduction in the con
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Acknowledgments We are grateful to Dr Jean Marie Bernassau
2019-11-18
Acknowledgments We are grateful to Dr. Jean-Marie Bernassau for his leadership in establishing our virtual screening platform and Dr. Julie Bick for protein purification. X-ray data collection for compound 4 was performed by Shamrock Structures at Southeast Regional Collaborative Access Team (SER-C
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With regard to the DGATs we have found that
2019-11-18
With regard to the DGATs, we have found that the majority of algal species encode at least one DGAT1, although it appears to be absent from Ostreococcus and Micromonas, as is the case for yeast, S. cerevisiae. More surprising is the presence of multiple DGAT2 genes in algae, with the exception of C.
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br Results br Discussion MSCs derived from the bone
2019-11-16
Results Discussion MSCs derived from the bone marrow and adipose tissue have been shown to promote the growth and metastatic ability of breast cancer and other human malignancies, but the mechanisms are incompletely understood (Barcellos-Hoff et al., 2013, Cuiffo et al., 2014, Del Pozo Martin
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The primary aim of this study was to
2019-11-16
The primary aim of this study was to evaluate DAPK methylation as a tumor marker which is not only detected in the primary tumor but also in the serum of patients. We used matched pre-operative serum samples to determine the correlation of tumor and serum results. Despite an equal methylation freque
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Ketoprofen br Materials and methods br
2019-11-16
Materials and methods Results The BUN and creatinine levels in the saline-treated CRF group were found to be significantly higher than those in the sham-operated control rats treated with either montelukast or saline (p major degradation product of lipid peroxidation in the renal, pulmonary, c
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Opiate withdrawal promotes the activation of the corticotrop
2019-11-16
Opiate withdrawal promotes the activation of the corticotropin-releasing factor (CRF) system, a major coordinator of neuroendocrine and behavioral responses to stressors. For instance, early (8–48 h) morphine withdrawal is associated with increased CRF mRNA expression in the central nucleus of the a
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Introduction Safety critical systems are defined as those sy
2019-11-16
Introduction Safety-critical systems are defined as those systems where failure could result in the loss of life or injury to people, damage to equipment or to the environment [9]. Safety standards, e.g., [41], [17], [18], [6], [38], expect appropriate safety analysis tasks to be integrated within
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We found that E and
2019-11-16
We found that E2 and GEN each has mostly similar effects on recruitment of the epigenetic modulators to the MB-COMT distal promoter (summarized in Table 2). These effects are associated with increased promoter methylation and gene suppression of COMT. It is noted that the array of epigenetic modulat
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