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br Restenosis after angioplasty remains a remarkable
2020-10-10
Restenosis after angioplasty remains a remarkable challenge, although drug-eluting stents have reduced the incidence of restenosis considerably . Vascular smooth muscle s1p receptor (VSMCs) play a pivotal role in the development of intimal thickening and restenosis. VSMCs proliferate and migrate
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cGAS has a central role
2020-10-10
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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This hydrophobic biphenyl tail gave good binding affinity
2020-10-10
This hydrophobic biphenyl tail gave good binding affinity for human DHODH enzyme (IC mineralocorticoid receptor antagonists was found to be the main metabolite in human microsomes and it was 100-fold less active against hDHODH than the ester. In an attempt to identify the specific non-covalent bind
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Bioactive Compound Library As temperatures increase rates of
2020-10-10
As temperatures increase, rates of spontaneous deamination also increase such that hyperthermophilic organisms must have efficient mechanisms for dealing with this potential hazard.8., 9. The hyperthermophile Methanococcus jannaschii has both a dCTP deaminase (encoded by the gene at locus MJ0430) an
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Multivariate models take interactions between cytokines into
2020-10-10
Multivariate models take interactions between cytokines into account and were used to accurately distinguish samples from different time points in pregnancy. The distinction accuracy did not increase with increasing time between the gestational time points, indicating that the cytokine development d
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In this review we first
2020-10-10
In this review, we first introduce the in vivo metabolism profile of VD3, and the mediation of Cyp3a gene transcription by PXR and CAR in humans, mice and rats. We then focus on the species-specific VDR-dependent regulation of human (CYP3A4, CYP3A5 and CYP3A7), mouse (mainly CYP3A11 and CYP3A13), an
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br Conclusion CSF R may contribute to limitation of targeted
2020-10-10
Conclusion CSF-1R may contribute to limitation of targeted therapies by providing EGFR-bypassing signals that support proliferation. Multi-kinase inhibitors such as cabozantinib are available, and agents targeting CSF-1R are in clinical trials, however, at present, as inhibitors of tumor-associat
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AZD8186 Since we found that the pharmacokinetic properties o
2020-10-10
Since we found that the pharmacokinetic properties of KPT-185 were unsuitable when given subcutaneously or orally, it is not a candidate for in vivo therapy for NHL. However, the pharmacokinetic properties of KPT-276, a CRM1-inhibiting SINE structurally related to and with functional activities simi
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Beside the previously reported Topo
2020-10-10
Beside the previously reported Topo I inhibition, time and concentration dependent CRM1 inhibitory properties of klavuzon derivatives have been shown as a second mechanism of action in this work. Especially, compounds 3 and 20 are the most effective derivatives and they completely inhibit CRM1 activ
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The importance of mitochondria as
2020-10-10
The importance of mitochondria as site of aerobic oxidation of metabolic fuels, such as FA, has been recognized for a long time. It has been observed that the number of mitochondria may vary in response to cellular metabolic requirements and hormonal environment (Gao et al., 2014). In order to susta
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The different diagnostic outcomes of the
2020-10-10
The different diagnostic outcomes of the two assays are also dependent on the used stimuli. The QuantiFERON-CMV assay targets CD8 + T Efaproxiral Sodium by using peptides whereas the T-Track-CMV targets CD4+ and CD8 + T cells by stimulation with two viral proteins [18]. In our study, a specificity
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It would be very useful if unphosphorylated CK s
2020-10-10
It would be very useful if unphosphorylated CK1s could be prepared using an E. coli expression system without the troublesome in vitro phosphatase treatment. So far, it has been shown that coexpressed λPPase, a Mn2+-dependent protein phosphatase that can dephosphorylate phospho-Ser/Thr/Tyr [20,21],
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Several CHK inhibitors have been reported in the literature
2020-10-10
Several CHK-1 inhibitors have been reported in the literature. Of these, UCN-01 (7-hydroxystaurosporine) is a potent inhibitor of CHK-1 (=5.6nM), , and has modest selectivity among other kinases. UCN-01 is currently in clinical trials. Other CHK-1 inhibitors reported in the literature include indaz
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AMG 487 br Materials and methods br Results br Discussion En
2020-10-09
Materials and methods Results Discussion Enolase (2-phospho-D-glycerate hydrolase) is a glycolytic enzyme that is also involved with various important roles in the intracellular and extracellular space (Copley, 2003; S. Zhang et al., 2015) such as transcriptional regulation, apoptosis, grow
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During the past few years
2020-10-09
During the past few years, several studies have addressed macrophage phenotype in experimental models, such as angiotensin II-induced AAA. A first study investigated macrophage phenotype using flow cytometry to identify M1 and M2 macrophages and qPCR analysis for expression of NOS2 and Ym1/2. The au
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