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The compounds were ranked based on the Glide
2020-06-24

The compounds were ranked based on the Glide XP Score, as shown in . All 15 compounds were subject to a radiometric assay previously used in our lab to evaluate their ability to inhibit DHFR steady-state activity in recombinant TS-DHFR (A). Compound demonstrated greater than 50% inhibition of DHFR
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br Conclusions Overexpression of DDR might contribute to tum
2020-06-24

Conclusions Overexpression of DDR2 might contribute to tumor progression in lung SQCC, and the T681I mutation we found in this work is an inactivating mutation. There is a possibility that not only activating mutation but also overexpression of DDR2 might be a molecular target for treatment of lu
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The crystal structure of the B
2020-06-24

The crystal structure of the B. subtilis Maf (BSU28050) was published in 2000, and, to date, it represents the only experimental work with a purified Maf protein (Minasov et al., 2000). The structure revealed a structural fold similar to that found in ITPases and YjjX proteins, which are nucleotide
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Several single nucleotide polymorphisms SNPs in humans affec
2020-06-24

Several single nucleotide polymorphisms (SNPs) in humans affect CYP3A expression and activity (Lamba et al., 2002). The CYP3A4 SNP rs2740574 (also referred to as CYP3A4*1B, by The Human Cytochrome P450 (CYP) Allele Nomenclature Database, http://www.cypalleles.ki.se/) is a change in the promoter regi
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Introduction Cholesterol plays a pivotal role as
2020-06-23

Introduction Cholesterol plays a pivotal role as a constituent of biological membranes and as a precursor for vitamins, hormones and bile acids. Accordingly, its production, distribution, and elimination must be tightly regulated at the cellular and organismal level. Accordingly, dysregulated chole
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Overall the DDR kinase domain has a typical kinase domain
2020-06-23

Overall, the DDR1 kinase domain has a typical kinase domain structure and adequate sequence and/or structure similarity with other kinase domains, as shown in Fig. 2, which allow homology modeling of the active and inactive conformations. In addition to conformational changes to the activation loop
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eletriptan br Materials and methods br
2020-06-23

Materials and methods Results Discussion Recently it has been found that prostaglandins play an important role in modulating the host immune system [1,3,22,23], and some parasites produce these eicosanoid mediators to survive into their hosts [6,[10], [11], [12],24,25]. The discovery that p
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Materials and methods br Results br
2020-06-23

Materials and methods Results Discussion Microbial production of trans-4Hyp, an added-value amino K02288 receptor for pharmaceuticals, offers significant advantages over conventional chemical extraction in economic and environmental aspects. However the low titer and productivity with the ex
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br Results and discussion br Conclusion In this investigatio
2020-06-23

Results and discussion Conclusion In this investigation, pharmacophore models of CK1 inhibitors were developed using a pharmacophore modeling protocol proposed by us. The optimal pharmacophore hypothesis, Hypo2, was adopted to retrieve potential CK1 inhibitors from the commercial chemical data
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Regarding their reported beneficial properties on
2020-06-23

Regarding their reported beneficial properties on the digestive tract, the aim of this study was to evaluate the effect of water extracts of three Hypericum sps., HP, HA, HU and some of the main phenolic compounds (Ch, R and Q) on DNA protection against oxidative and alkylating DNA damage induced by
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br Enzymes repairing alkylated DNA br Induction of the Ada
2020-06-23

Enzymes repairing alkylated DNA Induction of the Ada regulon Methylated Ada is a strong activator for ada and alkA promoters. Although much weaker than the methylated form, unmethylated Ada acts alone as an activator for ada and alkA promoters. In contrast, the unmethylated protein present in
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NF B is a family of protein mediators that
2020-06-23

NF-κB is a family of protein mediators that regulate various innate and adaptive immune responses [29,30]. The NF-κB family consists of the following five proteins: c-Rel (Rel); p65 (RelA); RelB; p50(NF-κB1); and p52(NF-κB2). It has been confirmed that NF-κB is activated by TNF family cytokines, suc
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myosin inhibitor Another critical finding in this study
2020-06-23

Another critical finding in this study is that the level of αSyn oligomers in the SN of σ1R−/− mice was progressively increased with age, whereas the levels of αSyn monomers and αSyn messenger RNA (data not shown) were not altered compared to WT mice. A number of studies reported that soluble αSyn m
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Another critical finding in this study
2020-06-23

Another critical finding in this study is that the level of αSyn oligomers in the SN of σ1R−/− mice was progressively increased with age, whereas the levels of αSyn monomers and αSyn messenger RNA (data not shown) were not altered compared to WT mice. A number of studies reported that soluble αSyn m
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This work was supported by grants from the
2020-06-23

This work was supported by grants from the Institute of Cancer Research (ICR) and Biotechnology and Biological Sciences Research Council (BB/I014276/1 and BB/M013782/1). Main Text In 2006, Warburg et al. described an apparently distinct connective-tissue disorder characterized by blepharophimosi
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