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Also important in binding of E
2020-10-14
Also important in binding of E2 to the ER is the hydroxyl on the D ring, which has a stabilizing contact with His-524 in ERα (Fig. 7) and with His-475 in ERβ (Fig. S1) [8,9,36,37]. The spatial relationship of the functional groups on the A and D rings on E2 has been used to develop chemicals contai
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br Materials and methods br Results br Discussion
2020-10-14
Materials and methods Results Discussion This study demonstrates that various progestogens combined with E2 had different effects on breast cell growth. These effects had an inverse correlation with the changes of the PRA/PRB ratio. E2\'s antiapoptotic effects on MCF-7 DPQ may be related to
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br Introduction Concrete is one of the most commonly
2020-10-14
Introduction Concrete is one of the most commonly used materials in the construction industry and its raw material is available throughout the world. Concrete is derived from ordinary Portland cement and is used for the construction and development of infrastructures. Research shows that demand f
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Grapiprant is a selective antagonist for
2020-10-14
Grapiprant () is a selective antagonist for prostaglandin E (PGE) receptor subtype 4 (EP4) identified as a clinical candidate for the treatment of inflammatory pain associated with osteoarthritis (OA). It is currently under development for use in humans and dogs. The projected dosing regimen of grap
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br Materials and methods br Results br Discussion COX mediat
2020-10-13
Materials and methods Results Discussion COX-2-mediated production of PGE2 is involved in cell growth and metastasis of many cancers. Previous studies indicated that COX-2 was overexpressed in many cancer tissues and that PGE2 increased cancer cell growth, a process that could be suppressed
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br PFL AE as a
2020-10-13
PFL-AE as a model for the GRE–AEs Most of the GRE–AEs have proven difficult to study due to instability, difficulty in overexpression, lability of the iron-sulfur cluster, or other reasons. PFL-AE is the exception, and after the initial discovery of the iron–sulfur cluster in this enzyme [60], co
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Mifepristone The role of ETB clearing receptors has been stu
2020-10-13
The role of ETB clearing receptors has been studied in detail in endothelial cell–specific ETB knock-out mice. In these animals, clearance of an intravenous Mifepristone of labeled ET-1 was reduced significantly compared with wild-type controls. Importantly, functioning ETB were retained on all oth
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TRAF and TRAF were initially identified as
2020-10-13
TRAF1 and TRAF2 were initially identified as tumor necrosis factor receptor 2 (TNRF2)-associated components, TRAF4 was overexpressed in breast carcinoma cells, whereas TRAF3, TRAF5 and TRAF6 were discovered by their interaction with specific domains in the cytoplasmic tails of trans-membrane recepto
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Acknowledgments We are grateful to Dr Jean Marie Bernassau f
2020-10-13
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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br Results and discussion br Conclusion Analogues of triazol
2020-10-13
Results and discussion Conclusion Analogues of 1,2,4-triazole and 1,3,4-oxadiazole have been designed, synthesized and characterized. To avoid late stage failure, it is important to study the preliminary pharmacokinetic parameters. The results of pharmacokinetic data suggested that, all molecu
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br Acknowledgements Thanks are due to Science
2020-10-13
Acknowledgements Thanks are due to Science and Technology Development Fund – Egypt for the Research Support Technology Development Grant (RSTDG) no. 12626. Our deep thanks and gratitude is also extended to National Cancer Institute (NCI), Bethesda, Maryland, USA for performing the anticancer eval
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br Molecular modeling simulation study Molecular modeling st
2020-10-13
Molecular modeling simulation study Molecular modeling study was performed through docking of the test compounds into the binding site of hDHFR enzyme using Discovery Studio 2.5 software. Computational docking is an algorithm designed to determine the suitable position and the orientation of the
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br Introduction Biocatalysis can be used to synthesize chira
2020-10-13
Introduction Biocatalysis can be used to synthesize chiral building blocks, such as monomers for polymer materials, and precursors for pharmaceuticals [[1], [2], [3], [4]]. Enzymes are very suitable for catalyzing reactions with high enantioselectivity to obtain chiral products. For instance, alc
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In the context of food allergy it
2020-10-13
In the context of food allergy it is hypothesized that intestinal barrier dysfunction might contribute to both antigen sensitization and the IgE/mast cell mediated effector phase of allergic disease, however no concluding data has been published to date [5]. An understanding of the mechanism of prim
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In LPS treated BV cells we found that the upregulated
2020-10-13
In LPS-treated BV-2 cells, we found that the upregulated CysLT2R was translocated into the nucleus. The nuclear localization of CysLT2Rs in microglia has not been reported previously. It is known that CysLT1Rs in endothelial matrix metalloproteinase translocated to the nucleus in a ligand-independen
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