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Enlarging the ligand binding pocket by
2020-10-22

Enlarging the ligand-binding pocket by reduction of the size of the residue F435 switched DES to an agonist indicating that F435 is involved in mediating the antagonistic effect of DES (Fig. 7E) [13]. The conformation of the smaller side chain of L435 was either not altered by DES or was too small t
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ATP binding cassette transporters such as ABCA and ABCG are
2020-10-22

ATP-binding cassette transporters such as ABCA1 and ABCG1 are expressed on cell membranes to transport cholesterol from Oxaprozin to HDL. These transporters help to improve RCT and reduce atherosclerosis. ABCA1 and ABCG1 gene expression are primarily induced by the stimulation of liver X receptor/r
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Lidocaine A set of small molecule LigI
2020-10-22

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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Methylation of histone tails is important in
2020-10-22

Methylation of histone tails is important in regulating 9508 structure and transcription. Methylation occurs at arginine and at mono-, di- or tri-methylated lysine residues. The reversibility of histone methylation was recently revealed by the identification of two histone demethylases, LSD1 and JH
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The aniline R group was extensively explored and a
2020-10-22

The aniline R2 group was extensively explored and a large variety of substitution was tolerated at several positions on the aryl ring (). Notably, substitution at the 3-position often gave increased potency. Increasing lipophilic bulk at this position gave increasing potency within an ether series (
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The effect of NAT deletion on mitochondrial function
2020-10-22

The effect of NAT1 deletion on mitochondrial function in MDA-MB-231 Nutlin 3 has been reported elsewhere (Carlisle et al., 2018). However, unlike the data presented here, increases in reserve capacity and glycolytic reserve were seen. The reasons for this variance between our study and that of Carl
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The androgen receptor AR is a steroid hormone receptor that
2020-10-21

The androgen receptor (AR) is a steroid hormone receptor that plays a crucial role in the normal development of male reproductive tissues, and its high expression and/or relaxation of its regulation are strongly implicated in prostate cancer (PCa) [11]. Androgen binding induces conformational change
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COMT expression protein level and
2020-10-21

COMT expression, protein level and activity are down regulated by E2. Using estrogen receptor (ER) positive MCF-7 cells, Xie et al. demonstrated an E2 dose dependent (1, 10 and 100 nM) decrease in S-COMT 1.3 kb mRNA that was maximum after 48 h (Xie et al., 1999). A similar decrease was not observed
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These data indicate that in the context of the N
2020-10-21

These data indicate that, in the context of the N-terminal 42 amino acids of p53, threonine 18 is a substrate for phosphorylation by CK1 as mediated by prior phosphorylation of serine 15. To determine whether this is a property of full length p53, GST-p53 fusion proteins comprising the full length p
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There have been two reports of
2020-10-21

There have been two reports of tumor shrinkage in response to dasatinib treatment in lung SCC patients harboring the DDR2 kinase domain S768R mutation., In the first case described by Hammerman et al. a combination of erlotinib (an epithelial growth factor receptor inhibitor) and dasatinib was admin
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Ranolazine br Conclusion In conclusion our
2020-10-21

Conclusion In conclusion, our findings do not suggest that HT is an important determinant of future AD risk and are in line with a recent Cochrane review stating that HT is not indicated for preventing dementia or cognitive decline in postmenopausal women [13]. Contributors Conflict of inte
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br Material and Methods br
2020-10-21

Material and Methods Results and Discussion Conclusions Two chemical coupling agents, BTDE and CDI, were used to activate the free hydroxyl groups of plant cellulose powder and OPH from Flavobacterium ATCC 27551 immobilized on modified carriers by covalent linkages. The highest immobilizati
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Sulforaphane is one of the few parasites that can
2020-10-21

is one of the few parasites that can be encysted and excysted and we tested the localization and role of HA-tagged gEno in both differentiations, using a recently developed integrated vector that introduces a C-terminal triple HA tag under the selection marker puromycin . The localization of HA-tagg
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On the other hand the
2020-10-21

On the other hand, the interaction of the Kaempferia parviflora extract with CYP3A was uncompetitive with a low Vmax value. In the in vivo study, the Kaempferia parviflora extract did not interfere with CYP3A activity throughout the entire duration of treatment. This is fortunate as CYP3A isoforms a
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The importance of EBI for B cell function was
2020-10-21

The importance of EBI2 for B cell function was first suggested by the dramatic upregulation of this receptor in EBV-transformed B cells 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 of EBI2 in
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