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QSAR based on the D structures of ligands plays an
2021-06-16
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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The authors gratefully acknowledge financial support from
2021-06-16
The authors gratefully acknowledge financial support from the State of São Paulo Research Foundation (FAPESP, Fundação de Amparo à Pesquisa do Estado de São Paulo), grants 2013/07600-3 and 2013/25658-9, and the National Council for Scientific and Technological Development (CNPq, Conselho Nacional de
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Data from our in vitro studies using
2021-06-16
Data from our in vitro studies using BEAS-2B cells showed a biphasic response of cells to NNK. The initial phase of decrease in CRM1 expression in NNK-exposed cells was observed in our previous study. In this study, we further showed that p-p53 (Thr55) expression was also decreased during this initi
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EPAC activation in VSMCs and ECs
2021-06-15
EPAC activation in VSMCs and ECs reverses several processes involved in the development of in-stent restenosis. Of particular relevance is the ability of EPAC1 to induce SOCS3 gene expression, as SOCS3 exerts multiple protective effects in both cell types, while immunohistochemical studies have show
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Previously we have described increased
2021-06-15
Previously, we have described increased expression of both cytokine and chemokine mRNA (e.g. MCP-5 and fractalkine) in the left ventricle of male EP4-KO mice with dilated cardiomyopathy [2]. Takayama et al. [31] have shown that PGE2 potently inhibits cytokine/chemokine secretion (MCP-1, interleukin
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br Materials and methods br Results and discussion
2021-06-15
Materials and methods Results and discussion Conclusions Acknowledgements This work was supported financially by the LIAONING S&T Project (No. 20180550107) and Basic Scientific Research Funds of DLNU (0918110143). Introduction Since 1970s, numerous artificial mimetic enzymes have bee
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Adding more pieces to the puzzle using a human to
2021-06-15
Adding more pieces to the puzzle, using a human-to-animal crossover study, blood taken from healthy volunteers that underwent exercise was used as a dialysate to perfuse a rabbit heart in a Langendorff model of MI [62]. Unprecedentedly, dialysate of plasma from exercised humans reduced infarct size
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The hepatic cytochrome P CYP superfamily is essential for
2021-06-15
The hepatic cytochrome P450 (CYP450) superfamily is essential for metabolising foreign chemicals, fatty acids, vitamins, hormones and other compounds and consists of 18 subfamilies (Uno et al., 2012). The number of discovered CYP genes is increasing as a result of intense work with CYP450 gene struc
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A structural explanation for how RBR RING s
2021-06-15
A structural explanation for how RBR RING1s handle their bound E2~Ubs differently from canonical RINGs has not been readily apparent. Only a few residue positions are strongly conserved in RING and RING1 domains, most of which are zinc-coordinating Cys and histidine residues. A key position in canon
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Because macrophages clear the injured tissue
2021-06-15
Because macrophages clear the injured tissue of dead KU55933 australia and matrix debris, macrophage infiltration is essential for normal tissue repair. In cardiac remodeling by MI, however, macrophages infiltrate excessively into not only the infarct area and marginal area of MI. Infiltrated macro
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BTB06584 In this review focusing on biocatalyst formate
2021-06-15
In this review, focusing on biocatalyst “formate dehydrogenase FDH” catalyzing both of the formic BTB06584 oxidation to CO2 and the CO2 reduction to formic acid, representative examples of properties, types, structure of active-site of FDH and, reaction mechanism of formic acid oxidation and CO2 re
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One possible explanation for differences in the binding
2021-06-15
One possible explanation for differences in the binding ability of monomeric versus dimeric forms of DDR2 ECD to collagen could be that the monomeric form only binds to the primary GVMGFO site, whereas dimeric (and oligomeric) DDR2 ECD binds to additional sites on the collagen triple-helical molecul
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Sodium Aescinate In summary our findings show that
2021-06-15
In summary, our findings show that LPS can activate CysLT2R on microglial Sodium Aescinate to induce microglial inflammation and microglia-dependent neuronal death. Furthermore, pharmacological inhibition or knocking down of CysLT2R expression protects neurons against neurotoxicity via suppression
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br Materials and methods br Results and
2021-06-15
Materials and methods Results and discussion Acknowledgements This study was supported by the Open Project Program of the Key Laboratory of Mariculture & Enhancement of Zhejiang Province (No. 2016KF003), the Key Project of Zhejiang Province (No. 2016C02055-7), and the International Science
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Considering the protumoral functions of TAMs new therapies
2021-06-15
Considering the protumoral functions of TAMs, new therapies against TAMs have recently gained interest. Such treatments, particularly inhibitors of the colony stimulating factor 1 receptor (CSF-1R), are currently evaluated in several clinical trials [19]. CSF-1R inhibitors may also be of interest in
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