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A surprising second functional effect was found
2021-04-22
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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Cytochrome P CYP enzymes plays an essential
2021-04-22
Cytochrome P450 (CYP-450) enzymes plays an essential role in pharmacology of drugs and toxicology of xenobiotics. Inhibition of these enzymes may lead to increase plasma levels of a concomitantly administered drug (Lee et al., 2013). It may prolong or reduce the pharmacological effects and increase
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Quercetin competitively inhibited BFC activity in human reco
2021-04-22
Quercetin competitively inhibited BFC activity in human recombinant cDNA-expressed CYP3A4 with Ki=15.4±1.52μM, and myricetin noncompetitively with Ki=74.6±7.99μM (Fig. 4). The degree of inhibition by quercetin was not affected by a pre-incubation step and was similar in the microsomes from both gend
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There is an increase in small fruit consumption especially
2021-04-22
There is an increase in small fruit consumption especially berries in recently. Because small fruits are rich sources of both anthocyanins and phenolic compounds. These chemicals have been found in Vaccinium corymbosum in high levels. Research on small fruits is of vital importance for human nutriti
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The pharmacokinetics properties of compound were
2021-04-22
The pharmacokinetics properties of compound were evaluated in male Sprague Dawley rats following IV (0.7mg/kg) and oral (2.0mg/kg) dosing. The total body clearance and the terminal half-life were 0.73 L/h/kg and 5.1h, respectively. After oral administration the compound showed good bioavailability (
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Previously we had proposed three possible models with one be
2021-04-22
Previously we had proposed three possible models, with one being that hCrm1 fundamentally interacted more favorably or strongly with Rev-RRE complex, compared to mCrm1. We decided to test that model, which was the simplest and most straightforward, by both biochemical and genetic means. By using bac
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More recently it was discovered that BChE hydrolyzes the
2021-04-22
More recently, it was discovered that BChE hydrolyzes the neuropeptide gut hormone, ghrelin [25], [26], [27], [28]. Nonetheless, because the enzyme reaction is very slow, those who first reported this finding were initially reluctant to attribute a real physiological role for that phenomenon. Our ow
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Astrocytes play a key role in the brain
2021-04-22
Astrocytes play a key role in the brain, as these cells are involved in fluid, ion, pH, and neurotransmitter homeostasis, synapse function, energy and metabolism and blood-brain barrier (BBB) maintenance (Sofroniew and Vinters, 2010). PA is able to activate different damaging responses in astrocytes
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br Materials and methods br Results
2021-04-22
Materials and methods Results Discussion The EP4 A-1155463 for PGE2 is similar to the EP1, EP2 and EP3 receptors in that they all have seven transmembrane segments and are coupled to Gα subunits of heterotrimeric G proteins, with a different Gα subunit for each receptor (Sugimoto and Narum
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Cucurbitacin B br Protein protein interactions of LEI L
2021-04-21
Protein-protein interactions of LEI/L-DNase II and the control of cell death Evolutionary tips The serpin inhibitory mechanism is extremely well adapted to evolutionary changes because a single amino Cucurbitacin B substitution in the RSL can led to the inhibition of a totally different prote
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In the past few years neuroprotection via
2021-04-21
In the past few years, neuroprotection via GLP-1R activation has been shown in several animal models of stroke, Alzheimer's, Parkinson's, Huntington's, ALS and traumatic JNK-IN-7 injury. This research field is rapidly growing and several reviews have been recently published (Darsalia et al., 2014b,
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Herein in continuation of our interest in designing new DNA
2021-04-21
Herein, in continuation of our interest in designing new DNA photocleavage agents [18], we report the synthesis, characterization and DNA binding and cleaving properties of a novel compound: trans-N,N-dimethyl-10,11-di(pyridin-4-ium)-10,11-dihydro-9,12-dioxobenzo[e]phenanthrene tetrafluoroborate (1)
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br Introduction DNA ligation is required during DNA replicat
2021-04-21
Introduction DNA ligation is required during DNA replication and to complete almost all DNA repair events. In human cells, the DNA ligases encoded by three LIG genes are responsible for joining interruptions in the phosphodiester backbone [1]. These enzymes have distinct but overlapping functions
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The unique property of mutant IDH in
2021-04-21
The unique property of mutant IDH1/2 in producing an oncometabolite that has no known physiological function makes mutant IDH enzymes as obvious potential therapeutic targets for the treatment of IDH-mutated tumors (Rohle et al., 2013, Wang et al., 2013). Clinical studies have also suggested the pre
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Some pyrimidine analogs are substrate based inhibitors that
2021-04-21
Some pyrimidine analogs are substrate-based inhibitors that bind to the dihydroorotate binding site, but most reported inhibitors of DHODH bind to the site occupied by the ubiquinone co-factor., , , , , , , , , , , , , , , , , X-ray crystallographic studies of inhibitor complexes with DHODH and DHO
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