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The compounds were ranked based on the Glide XP
2019-12-26

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 General Characteristics of the
2019-12-26

General Characteristics of the Type II Dehydrogenases Alternative NAD(P)H dehydrogenases conduct the reaction of the rotenone-insensitive oxidation of cytosolic and mitochondrial matrix NADH and/or NADPH (Fig. 1) (Melo et al., 2004, Rasmusson et al., 2004, Rasmusson et al., 2008). They catalyze t
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Plant uptake of P from OA could also be affected
2019-12-26

Plant uptake of P from OA could also be affected by arbuscular mycorrhizal fungi (AMF). Approximately 80% of terrestrial plant species form symbiotic associations with AMF (Smith and Read, 2010) which can enhance plant P uptake (Facelli and Facelli, 2002, Pearson and Jakobsen, 1993, Tibbett, 2000).
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Despite the sources of error discussed above
2019-12-26

Despite the sources of error discussed above, several trends have emerged and much valuable data are available regarding binding affinities of progestogens for different steroid receptors. All the progestogens bind to the PR with a high affinity, typically in the nanomolar range. For example the syn
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In brief while previous studies have evaluated the
2019-12-26

In brief, while previous studies have evaluated the individual roles of VDR and ER signaling pathways in breast cancer, in the present study we performed an in silico approach for comparative evaluation of these pathways. Considering the complex interaction networks in the context of cancer, such co
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br Introduction Our understanding of how
2019-12-26

Introduction Our understanding of how ligands interact with G protein coupled receptors is evolving, particularly the recognition that some have the ability to preferentially activate a subset of intracellular signalling cascades – so called pathway biased ligands [1]. Additionally, it is now acc
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The development of novel approaches to study GPCR mediated
2019-12-26

The development of novel approaches to study GPCR-mediated transactivation in live MM-102 is important, and this study describes a unique BRET-based quantification of Grb2 recruitment to the EGFR as a direct readout of GPCR-mediated transactivation. We have previously used the recruitment of Grb2 t
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In addition to EGFR other
2019-12-26

In addition to EGFR, other receptor tyrosine kinases (RTKs) also play roles in the tumor progression under hypoxia, especially hepatocyte growth factor receptor (cMet) (Le et al., 2012). Our data suggested that unlike EGFR, hypoxia had no apparent effect on cMet papain inhibitor (data not shown), su
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A structural explanation for how RBR RING s
2019-12-26

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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CFSs are recognized as a driver of genome instability
2019-12-26

CFSs are recognized as a driver of genome instability in human cells and are hotspots for deletions or translocations in cancers (Richards, 2001). The generally accepted model for their expression is that the CFS locus shows a delay in chromatin condensation in early mitosis caused by the persistenc
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In children only the genotype
2019-12-26

In children, only the 6/7 genotype was associated with spina bifida, increasing the risk about 4 times relative to the DHFR 3/3 and 6/6 genotypes. However, the 95%CIs are broad and only few spina bifida patients have the DHFR 6/7 genotype. The effect of the 6/7 genotype on spina bifida risk is there
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br Materials and methods br Results br Discussion In
2019-12-26

Materials and methods Results Discussion In this study, we developed a new CysLT1 and CysLT2 receptors-mediated Cy5 amine (non-sulfonated) guinea pig model for screening both CysLT2 receptor and CysLT1/2 receptor antagonists. Unlike human CysLT2 receptors, which are equally stimulated by bo
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br Introduction Benzanthrone BNZ is
2019-12-26

Introduction Benzanthrone (BNZ) is a dye intermediate used in the synthesis of number of polycyclic vat and disperse dyes. It has been detected as an environmental pollutant in urban ambient air particulates, originating from furnace effluents, municipal refuge, wood and coal combustion and autom
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The activity of chromenones bearing heteroaryl groups at the
2019-12-24

The activity of chromenones bearing heteroaryl groups at the 8-position is summarised in . Replacement of the 8-phenyl substituent of by a thiophen-2-yl group ( and ) did not improve DNA-PK inhibitory activity, although the 4-phenylthiophen-2-yl derivative (), together with the bithiophene analogue
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The mutation in Caucasian people of European heritage is qui
2019-12-24

The Δ32 mutation in Caucasian people of European heritage is quite common but extremely rare in Asian and African countries (Huang et al., 1996). We recently reported the presence of this mutation from India (Husain et al., 1998a) and established the complete inheritance pattern (Husain et al., 1998
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