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QSAR based on the D
2019-09-30
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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IL is not expressed in tissues
2019-09-30
IL-8 is not expressed in tissues constitutively because of its strong chemoattractant, proinflammatory, and angiogenic activities. Rather, it is an inducible factor, produced by a variety of cell types, including leukocytes, fibroblasts, endothelial and epithelial cells, in response to proinflammato
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Today many strategies have been
2019-09-30
Today, many strategies have been developed to enhance CXCR-4 receptor 9-AC on the cell surface, either by modifying the cell culture medium or by modifying the CXCR-4 gene in BMSCs to stimulate stem cell recruitment (Jiang et al., 2012, Liu et al., 2014b). For instance, the pre-conditioning of sub-c
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The most important cytotoxic lesion formed by the
2019-09-30
The most important cytotoxic lesion formed by the nitrogen mustards is generally considered to be the DNA–DNA interstrand cross-link 12, 13. DNA–DNA interstrand cross-links are thought to exert their cytotoxic effects by inhibiting DNA duplex strand separation, progression of the ApexPrep DNA Plasmi
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A further quandary concerning rediscoveries arises
2019-09-30
A further quandary concerning rediscoveries arises in habitats modified and frequented by humans, where rediscovered species may occur through accidental or deliberate introductions (Metcalf et al., 2007) rather than having persisted despite adverse conditions. Confusion regarding origin could evoke
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Adding MPA or NETA we found no impact
2019-09-29
Adding MPA or NETA we found no impact on the estradiol-induced downregulation of serum-stimulated endothelin synthesis in vitro [40]. Progesterone was also able to inhibit the angiotensin II-induced increase in endothelin production [41]. Several clinical studies on the effect of oral or transdermal
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To study the effect of DDR
2019-09-29
To study the effect of DDR inhibition by imatinib, nilotinib and dasatinib in a cellular environment we generated DDR1 and DDR2 expressing HEK293 cell lines by stable transfection. Of the five DDR1 splice variants we focused on the 1b variant whose over-expression has been associated with pulmonary
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br Competing interests br Acknowledgments
2019-09-29
Competing interests Acknowledgments This work was supported by grants from Fujian Fujian Provincial Natural Science Foundation (2016J01612). Introduction Cancer is still one of the most serious diseases in the world. According to the World Health Organization (WHO), cancer is the second mo
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Structure similarity searches were conducted using the stand
2019-09-29
Structure similarity searches were conducted using the standalone version of the DALI program with the query structures scanned against a local current version of the PDB that has all chains as separate entries (Holm and Sander, 1995). The structural hits for each query were collected, even if the D
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br Results br Discussion In
2019-09-29
Results Discussion In this paper we present insights into the observed specificities of inhibitors targeting the ubiquitin-activating and related E1 rilpivirine clinical via crystal structures of the specific NEDD8-E1 inhibitor MLN4924, the dual NEDD8/Ub E1 inhibitor ABPA3, and the selective U
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In recent years there has been
2019-09-29
In recent years there has been a dramatic increase in identification and optimization of potent CRTh2 antagonists which may not only inhibit the recruitment and activation of Th2 cells but also accelerate apoptosis and clearance of these cells from inflamed tissue, thereby promoting the resolution
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Although PGD was initially considered to
2019-09-29
Although PGD was initially considered to elicit its biological actions through a classical PGD receptor (DP1), later findings suggested that several PGD-mediated actions of eosinophils arise via DP2,, which is also known as CRTH2 (chemoattractant receptor-homologous molecule expressed on Th2 cells)
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The physiological role of the UCNs
2019-09-29
The physiological role of the UCNs in the regulation of the HPA axis is still under debate (Fekete and Zorrilla, 2007, Suda et al., 2004). UCN 1 was proved to increase the plasma ACTH and corticosterone levels in rats (Bagosi et al., 2014, Vaughan et al., 1995), whereas UCN 2 and UCN 3 were shown to
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The majority of pro inflammatory cytokines
2019-09-29
The majority of pro-inflammatory cytokines are regulated by NFκB, and recently, it has been found that p38 MAPK partly regulates NFκB-driven gene 5-Azacytidine by increasing the association of the basal transcriptional factor, TATA-binding protein, with the C terminus of p65 subunit of NFκB and inc
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The two SNPs rs rs presented above are part
2019-09-29
The two SNPs rs4818-rs4680 presented above are part of the haploblock (rs6269, rs4633, rs4818, rs4680) presenting the 3 major haplotypes which influence the enzymatic activity of COMT. This activity is inversely related to the sensitivity of pain in a chronic pain syndrome; so the haplotype (GCGG) h
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