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br Conclusion The role of DNA PK
2019-11-28
Conclusion The role of DNA-PK target in DNA DSB repair renders this tcY-NH2 kinase of great medicinal interest in cancer chemotherapy especially the cancer types of linked to DNA defects. Due to the absence of 3D DNA-PK target structure, different ligand-based methods were applied for design of
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We have previously disclosed the
2019-11-28
We have previously disclosed the discovery of a 7-azaindole-3-acetic 99 8 CRTh2 antagonist chemotype 1 from HTS and its subsequent optimization to give 2 as a potent and orally bioavailable inhibitor of eosinophil shape change (SC) in human whole blood. Subsequent to disclosure of that work, others
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VEGF inhibition causes vascular regression and
2019-11-28
VEGF inhibition causes vascular regression and tissue hypoxia in tumor tissues and their surrounding healthy adipose tissues. In this regard, tumors in steatotic livers and adjacent to adipose tissues would experience more hypoxia than non-adipose tumors. Indeed, our present experimental results sup
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br Materials and methods br Results
2019-11-27
Materials and methods Results Discussion PYR-41 inhibits UBE1 activity that catalyses an initial step in the ubiquitination reaction. In the present study, we examined the role of this enzyme in sperm-egg fusion by inhibiting UBE1 enzymatic activity in eggs. Our results suggest that PYR-41
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CDK lacks DNA binding domains and nuclear
2019-11-27
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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Preparation of the pyridyl ether analogs was accomplished by
2019-11-27
Preparation of the 2-pyridyl ether analogs (–) was accomplished by alkylation of alcohol with 2-bromopyridines in the presence of NaH to afford the desired pyridyl ether analogs in low to moderate yield. Preparation of the 3-pyridyl analog was carried out by conversion of alcohol to the tosylate,
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Placental insufficiency is regarded as the
2019-11-27
Placental insufficiency is regarded as the main etiology for FGR. Placental development is highly unique in eutherians and is regulated by numerous factors. For example, the novel retrotransposon-derived gene retrotransposon-like 1 (RTL1) was recently shown to play a key role in placental developmen
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LP a levels are lowered by
2019-11-27
LP(a) levels are lowered by combined oral hormone therapy [80], [81], [82], [83], [84], whereas for most studies using transdermal HRT little or no changes have been observed [85], [86], [87]. Oral versus transdermal administration In general most markers are influenced in a similar way by oral
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Baicalein trihydroxyflavone was first isolated from the root
2019-11-27
Baicalein (5,6,7- trihydroxyflavone) was first isolated from the roots of Scutellaria baicalensis Georgi (Lamiaceae family), a medicinal plant with diverse therapeutic implications; antibacterial, antiviral, and anti-inflammatory properties. It has been found that baicalein benefits neuroinflammati
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KN-93 Phosphate Only a few studies have examined
2019-11-27
Only a few studies have examined the effect of prostanoids on cardiac fibroblasts. Therefore, this study examines the effect of PGE2 on cardiac fibroblast proliferation and tests the hypothesis that PGE2 causes cardiac fibroblast proliferation via alterations of KN-93 Phosphate regulatory molecules
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The importance of EBI for B cell function
2019-11-27
The importance of EBI2 for B cell function was first suggested by the dramatic upregulation of this receptor in EBV-transformed Paxilline receptor and further inferred from its regulation in activated and GC B cells (Birkenbach et al., 1993, Glynne et al., 2000, Shaffer et al., 2000). An involvement
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To ascertain separation of the distinct enzymatic activities
2019-11-27
To ascertain separation of the distinct enzymatic activities found in this protein preparation following separation on the HAP column, a rigorous quantitative analysis was conducted on the nickel–agarose elution and HAP FT pools of protein. For these analyses, each pool of protein was dialyzed in th
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Collectively the results presented here provide new insights
2019-11-27
Collectively, the results presented here provide new insights into ligand binding, clustering, spatial distribution, and phosphorylation of DDR1b and DDR2 in response to soluble collagen I. As depicted in the cartoon of Scheme 1, we postulate a model in which the spatial distribution and assembly of
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A set of small molecule LigI inhibitors were identified
2019-11-26
A set of small molecule LigI inhibitors were identified through an in silico structure-based screen, using the atomic resolution structure of LigI complexed with nicked DNA [[18], [26]]. This screen yielded inhibitors that were selective for LigI (L82), inhibited both LigI and LigIII (L67) and inhib
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br Materials and methods br Results
2019-11-26
Materials and methods Results Discussion In this study we characterized in more detail the interrelationship between the expression levels of the B. malayi Bm-cpl-3 and Bm-cpl-6 cysteine proteases and the fitness of Wolbachia, and consequently that of the parasite. Our present in vitro data
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