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In a study on the time course of a
2020-12-11
In a study on the time course of a mechanism-based inactivation of CYP3A by HIV protease inhibitors, Katzenmaier et al. [37] reported that the suppression of CYP3A activity continued for threedays after the discontinuation of ritonavir. In the present study, the CYP3A activity on day 28 after a seve
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The requisite extended benzyl alcohols and and final
2020-12-11
The requisite extended benzyl alcohols –, , and and final potential DFG-out binding hybrid inhibitors – and – were prepared as shown in , . Benzaldehyde was alkylated with -methoxybenzyl chloride and then reduced with sodium borohydride to give benzyl alcohol . Pyridine derivative was prepared by O-
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The molecular mechanism by which CRM
2020-12-11
The molecular mechanism by which CRM1 regulates IEC apoptosis in CD remains to be explored. As an inhibitor of cyclin E-Cdk2, p27kip1 plays a pivotal role in controlling cell proliferation, S phase entry, and G1 phase exit during development and tumorigenesis [38]. As previously reported, p27kip1 is
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Using characteristic features of ECM proteins and a computat
2020-12-11
Using characteristic features of ECM proteins and a computational pipeline combining interrogation of protein and gene databases, we previously defined the matrisome as the ensemble of ECM and ECM-associated proteins [[16], [17], [18]]. In mammals, the matrisome represents 4% of the genome, or appro
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Perturbations in cell cycle are known to induce apoptosis Ou
2020-12-11
Perturbations in SBE 13 HCl are known to induce apoptosis. Our results show that a fraction of the DT40YB-1b+/− cells, in addition to becoming tetraploids, undergo apoptotic cell death. Similar observations linking polyploidy and apoptosis have been made in the past [23], [30], [31], [32], [33], [3
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The underlying mechanisms of how progesterone prolongs pregn
2020-12-11
The underlying mechanisms of how progesterone prolongs pregnancy, although not completely understood, are thought to have to do with reduction in uterine contractility, antimicrobial protein up-regulation, immunosuppression, and inflammatory inhibition. Specific to preterm PROM, progesterone has bee
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TgTCEA from petals TgTCEA and TgTCEB from pollen grains TgTC
2020-12-11
TgTCEA from petals (TgTCEA1) and TgTCEB from pollen grains (TgTCEB1) were used throughout the study. The recombinant enzymes were expressed in , and purified as the His-tag-free forms as described previously., Enzyme reactions were performed at 4 mM substrates under the same conditions as described
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br Ultrasonic pretreatment of substrates Substrate pretreatm
2020-12-11
Ultrasonic pretreatment of substrates Substrate pretreatment is widely used in the biofuel, textile and food industries since the substrates are always difficult to degrade. During some enzymatic hydrolysis reactions, the protective layer of the substrate impedes the reaction. Ultrasonic treatmen
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Methscopolamine The Acat gene was identified
2020-12-11
The Acat1 gene was identified by functional complementation of a Chinese hamster ovary cell mutant lacking ACAT activity [12]. Unlike most other genes, human Acat1 is located in two different chromosomes, Methscopolamine 1 and 7, with each site containing a distinct promoter: chromosome 1 contains e
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Moreover Hypericum perforatum L was also included
2020-12-11
Moreover, Hypericum perforatum L. was also included in the initial screening, showing only a weak percentage of inhibition on both enzymes. In fact, it was not selected among the most active plants. The phytochemical profiles of these three Hypericum species were already reported to be significantly
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Even more unambiguous was the
2020-12-11
Even more unambiguous was the relative contribution of Gq/11 signaling in AngII-mediated transactivation as measured by the ERK1/2 and the BRET-based readout. Although Gq/11 was absolutely required for ERK1/2 phosphorylation following AngII-stimulation, in contrast, we observed a sustained EGFR-Grb2
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br Conflicts of interest br Financial
2020-12-10
Conflicts of interest Financial support NZ is an Established Investigator of the Dutch Heart Foundation (2013T111) and is supported by an ERC Consolidator grant (617376) from the European Research Council and by a Vici grant from the Netherlands Organization for Scientific Research (NWO; 91818
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The modification of proteins with the small
2020-12-10
The modification of proteins with the small 76-amino Kenpaullone receptor protein ubiquitin (Ub) plays a central role in many key cellular processes. Ubiquitylation of a target protein requires the concerted action of a cascade of three enzymes (Figure 1). The ubiquitin-activating enzyme (E1) catal
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cGAS has a central role in STING activation after DNA
2020-12-10
cGAS has a central role in STING activation after DNA sensing, but it is unknown if most of the DNA sensors act independently or in cooperation with the cGAS-cGAMP pathway. This was addressed for IFI16 (Almine et al., 2017, Jønsson et al., 2017) and PQBP1 (Yoh et al., 2015) but remains to be tested
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Since the initial identification of DNA ligase inhibitors by
2020-12-10
Since the initial identification of DNA ligase inhibitors by a structure-based approach [[18], [26]], there have been several reports describing LigI inhibitors using computer modelling and derivatives of the original DNA ligase inhibitors [[49], [50], [51]]. While these studies have shown that the
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