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The inhibition of FAS by C produces an accumulation of
2019-12-17
The inhibition of FAS by C75 produces an accumulation of malonyl-CoA which is difficult to reconcile with the activation of CPT1 reported by others [2], [16], [17], [18]. To unravel this paradox the mechanism of action of C75 needs to be examined. We recently demonstrated that C75 is converted in vi
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br Conclusions In the present study decreased AChE
2019-12-17
Conclusions In the present study, decreased AChE and increased BuChE and BeChE activities were observed in greenhouse workers relative to control subjects; however, these changes cannot be related to OP exposure but likely to pesticide-induced oxidative stress or a mild inflammatory state. The in
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The present study sought to determine if chlorodifluoroaceto
2019-12-17
The present study sought to determine if chlorodifluoroacetophenones, such as 3 and 4, were amenable to a radiolabelling methodology to generate potential 18F imaging agents with high cholinesterase affinity. A number of procedures have been reported for the synthesis of trifluoromethyl ketones, inc
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Identification of the drug to be
2019-12-17
Identification of the drug to be used as first-step antihypertensive treatment has always been, and remains, a matter of debate. The decision wihich drug (or drug combination) to choose as first-line therapy depend on many variables such as coexisting metabolic disorders, obesity, presence of subcli
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Binding affinity was measured by
2019-12-17
Binding affinity was measured by a scintillation proximity binding assay using [H]4-OHT (ERRγ) or [H]estradiol (ERα/β) as radioligand. In all cases, the ERβ affinity was not significantly different from ERα. Compounds were compared to , which showed high affinity for both receptors and moderate (six
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In the present study we investigated the
2019-12-17
In the present study, we investigated the role of EP1R after ICH and its mechanism of action. We hypothesized that EP1R activation aggravates ICH injury but that its blockade reduces injury through the Src kinases and the MMP-9 signaling pathway. To test this hypothesis, we examined the effects of s
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br Oxidoreductase like MEM for prodrug activation br
2019-12-17
Oxidoreductase-like MEM for prodrug activation Future outlook Although MEM-mediated prodrug activation has been performed by different MEMs and prodrugs, and their effectiveness have been proved in vivo, only a few types of MEMs or prodrugs have been explored in prodrug activation until now [2
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The ubiquitin like modifier NEDD
2019-12-17
The ubiquitin-like modifier NEDD8 (NEURAL PRECURSOR CELL EXPRESSED, DEVELOPMENTALLY DOWN-REGULATED 8) uses similar enzymatic machineries for NEDD8 conjugation as ubiquitin (Figure 1) [11, 12, 13, 14]. In plants as well as in other eukaryotes, the number of E3 ligases for NEDD8 and the number of know
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VX-702 mg After incorporation of random nucleotides
2019-12-17
After incorporation of random VX-702 mg by TdT during heavy-chain rearrangements, both TdT and pol λ may perform in trans polymerase activity (in unknown proportions), whereas synthesis of the complementary strand can only be achieved by pol λ using its gap-filling activity, which TdT lacks because
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br Results and discussion In the
2019-12-17
Results and discussion In the present study, we used a set of compounds (Fig. 2) consisting of ATP (a), dATP (b), an ATP analog containing β,γ-nonhydrolyzable hypophosphate P-P bond (c), and three pairs of P-diastereoisomers of α-thio-ATP analogs (d,e,f) containing a sulfur Rucaparib free base i
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The reaction of chitosan with
2019-12-16
The reaction of chitosan with DVS should take place primarily through a nucleophilic attack of the vinyl sulfone groups to the amino groups in chitosan [39,50], although its hydroxyl groups can also be involved, as it happens when using agarose [35]. These reactions create very stable secondary amin
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Metal ions are known not
2019-12-16
Metal ions are known not to be necessary for catalytic activity of serine proteinases. Nevertheless, Co2+ and Ca2+ ions were found to stabilize glutamyl endopeptidase molecule [1], [7], [19]. In our previous study, we have described significant stimulating effect of Ca2+, Mg2+, and Co2+ on biosynthe
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br RING type E s
2019-12-16
RING-type E3s and their substrates There is enormous diversity in substrate ubiquitination and its regulation, as the targets of RING-type E3s are incredibly varied. RING-type E3s are implicated as tumor suppressors, oncogenes, and mediators of endocytosis, and play critical roles in complex mult
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Given the widespread occurrence of oncogene
2019-12-16
Given the widespread occurrence of oncogene-induced RS and the increasing clinical interest in small molecule inhibitors that further exacerbate RS in human cancers (such as ATR inhibitors), our findings point to a protective role for RAD52 in the maintenance of cancer cell viability. As such, RAD52
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br Materials and methods br Results br Discussion
2019-12-16
Materials and methods Results Discussion Structural analysis of dnmt3 sequences of different ploidy fish cloned in this study showed high similarities to zebrafish sequences, which also contained a unique N-terminal motif and a calponin homology (CH) domain, a conserved proline-tryptophan-t
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