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We recently described the benzoxazin one analogue of
2019-07-19
We recently described the 1,3-benzoxazin-4-one analogue of LY294002 and showed it to have pan-PI3K and DNA-PK activity [2]. We have also reported on the activity of other family members, such as 3 which causes sensitization of lung cancer and colon cancer cells to radiation [11] and 4 (LTUSI122) as
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In the present work we ask
2019-07-19
In the present work, we ask whether rNMP incorporation is an evolutionarily conserved property of DNA synthesis in Archaea. For this purpose, we used the best characterized hyperthermophilic anaerobe, Pyrococcus abyssi GE5 [47]. This strain duplicates its genome as fast as Bacteria, supported by euk
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Classical DHFR inhibitors such as methotrexate MTX bind tigh
2019-07-19
Classical DHFR inhibitors such as methotrexate (MTX) bind tightly to the enzyme and possess adequate clinical pharmacokinetics. MTX bind to the DHFR binding site through the formation of hydrogen bonds with Asn64, Lys68, Arg28, Arg70, Val115 and Ile7 amino Berberine hydrochloride residues as well a
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The compounds were ranked based on the Glide XP Score
2019-07-19
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 Materials and methods br Results br
2019-07-19
Materials and methods Results Discussion In the present study, as a trial to evaluate the marine ciliate E. crassus for further studies, its susceptibilities to B[a]P and β-NF were measured. Acute toxicity of B[a]P in aquatic organisms has been extensively studied, but not enough data is av
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The ribosomal synthesis of D proteins
2019-07-18
The ribosomal synthesis of D-proteins is not currently feasible; the best effort undertaken so far was limited to the translational incorporation of two D-amino acids into the nascent protein chain by means of modified ribosomes (Dedkova et al., 2006). We therefore apply solid-phase peptide synthesi
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Anti-Inflammatory Peptide 1 A range of therapies exists for
2019-07-18
A range of therapies exists for the treatment of inflammation-driven diseases, which can be summarized as non-steroidal anti-inflammatory drugs (NSAIDs), corticoids and steroidal-related drugs (Ward et al., 2008). Despite of these notable successes, there are still major unmet medical needs in the t
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A surprising second functional effect was found in culture e
2019-07-18
A surprising second functional effect was found in culture experiments. Inclusion of LTD4 reduced the frequency of Fas receptor (CD95) expression. Once again, this effect, although modest, was reversed by a cysLT1 receptor antagonist. The biologic significance of this effect or its mechanism remaine
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br Materials and methods br Results br Discussion In
2019-07-18
Materials and methods Results Discussion In the present study, as a trial to evaluate the marine ciliate E. crassus for further studies, its susceptibilities to B[a]P and β-NF were measured. Acute toxicity of B[a]P in aquatic organisms has been extensively studied, but not enough data is av
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During DNA replication p protein
2019-07-18
During DNA replication p21 protein binds PCNA, in its role as processivity factor, to stop replication when there is DNA damage, and apparently p21 also binds PCNA when this is in complex with Cyc/CDKs [11]. In plants, KRPs (functional analogs of p21), inhibit kinase activity in CycD/CDKs complexes
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Acknowledgments br Prostaglandin D PGD
2019-07-18
Acknowledgments Prostaglandin D (PGD) plays a key role in mediating allergic reactions such as those seen in asthma, allergic rhinitis, atopic dermatitis and allergic conjunctivitis. PGD is the major cyclooxygenase product formed and secreted by activated mast cells and its levels in bronchoalveo
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Acidic substituents showed moderate biochemical activity
2019-07-18
Acidic substituents () showed moderate biochemical activity, but these compounds showed reduced cellular potency. Additional compounds bearing a carboxylic NSC 319726 were also prepared and tested (data not shown). All of acidic compounds showed low cellular potency regardless of their biochemical
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Completion of h of education was significant in virtually al
2019-07-18
Completion of 150 h of education was significant in virtually all prior studies of the 150-h requirement (Allen and Woodland, 2006, Boone et al., 2006 and others). While the 150-h requirement applies to licensure, students are often permitted (as in California) to sit for the CPA exam with fewer tot
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The present study was the first to
2019-07-18
The present study was the first to examine how COMT genotype and estradiol are associated with (+)-MK 801 where functioning in healthy postmenopausal women. We hypothesized that with decreased circulating estradiol after menopause, the COMT genotype relationship to cognition would remain and perhap
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To further verify the effect
2019-07-18
To further verify the effect of BBR on ACAT2 protein expression, we have conducted an in vitro permeability assay using Caco-2 monolayer. This assay has long been used to predict the in vivo Heparin sodium and bioavailability of a compound. It was observed that the amount of cholesterol esters in t
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