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In most cases the ligand affinity
2021-08-24

In most cases, the ligand affinity between subtypes is similar, but their tissue distribution is different. In the case of the estrogen receptors (ER), two subtypes (ERα and ERβ) exist (Kuiper et al., 1996) and ERβ has several isoforms, designated ERβ1–5 (Moore et al., 1998) or ERβcx (Ogawa et al.,
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The new ESC guidelines incorporate data from a network meta
2021-08-24

The new ESC guidelines incorporate data from a network meta-analysis of 100 studies confirming that new-generation drug-eluting stents (DES) improve survival compared with medical treatment, although this has not been demonstrated in any individual study. REVASCULARIZATION IN NON–ST-ELEVATION ACU
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We recently employed a functional
2021-08-24

We recently employed a functional drug screening approach to identify mithramycin as an inhibitor of EWS–FLI1. In our study, we employed a stepwise approach involving a luciferase primary screen and a novel multiplex PCR screen to evaluate over 50,000 compounds to identify mithramycin as an inhibito
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br Methods br Results and
2021-08-24

Methods Results and discussion Conclusions Conflict of interest Acknowledgment The research is supported by the National Natural Science Foundation of China (Grant No. U1603285). Overview of the MAPK pathway The mitogen-activated protein kinases (MAPK) pathway, often known as a ca
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br STAR Methods br Acknowledgments We are
2021-08-24

STAR★Methods Acknowledgments We are grateful to Amaia Lujambio, James Fagin, and Ramon Parsons for providing cell lines and Evripidis Gavathiotis for critical reading of the manuscript. We would like to thank Saboor Hekmaty for providing expertise with RNA-seq analysis. P.I.P. would like to ac
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Results are expressed as mean s
2021-08-24

Results are expressed as mean±s.e.m. Paired or unpaired Student's t test was used for comparisons between 2 groups and one-way ANOVA followed by Bonferroni's post-test for more groups. Statistical significance was assigned if p Results and discussion Variations in [Ca2+]i in cardiomyocytes loaded
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The compounds listed in Table Table
2021-08-24

The compounds listed in Table 1, Table 2, Table 3, Table 4, Table 5 were biologically evaluated for their inhibition of the specific binding of a radiolabeled ligand [3H]PGE2 to membrane fractions prepared from cells stably expressing each mouse prostanoid receptor. The EP1 antagonist activity of th
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Protease Inhibitor Cocktail (EDTA-Free, 200X in DMSO) The pr
2021-08-24

The prospects of the use of this novel approach for the selective local thermo-activation of enzymes include biomedical and biotechnological applications. As NPs could be engineered to gain access to Protease Inhibitor Cocktail (EDTA-Free, 200X in DMSO) through the endosomal compartment [47] or thr
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Previous studies demonstrated that cPLA
2021-08-24

Previous studies demonstrated that cPLA2α translocates to the phagosomal membrane during macrophage phagocytosis through mechanisms that, in humans, involve phosphorylation of the enzyme by c-Jun N-terminal kinases and membrane association via the cationic cluster of four lysine residues present at
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PI3K Akt mTOR Compound Library br Methods br Results br
2021-08-24

Methods Results Discussion With this study, we provided evidence that acriflavine can interfere with EMT and UPR, two well-described pathways associated with cancer aggressiveness. And, because drug resistance is also clearly associated with the mesenchymal state [36], blocking of the epith
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br Marginal zone lymphoma Marginal
2021-08-24

Marginal zone lymphoma Marginal zone lymphoma (MZL) comprises three lymphoma entities that arise from the marginal zone surrounding the germinal center: extranodal MZL or mucosa-associated lymphoid tissue (MALT), splenic MZL, and nodal MZL. Deep sequencing of nodal MZL patients found that 5/35 (1
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It is interesting to note that
2021-08-24

It is interesting to note that Eibinger and colleagues [23] recently reported chemotactic movement to 25-OHC in THP1 cells as well as in primary human monocytes. RNA interference suggested that in part this migration was mediated by EBI2. Competing financial interest statement Acknowledgments
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Likewise the conserved cysteine in the E
2021-08-24

Likewise, the conserved cysteine in the E2 protein is the only residue shown to be essential for the transfer of Ub/Ubl from E2 to the HECT ligases (Dye and Schulman, 2007, Wu et al., 2003). However, all other terminal Ub/Ubl transfer reactions involving E2 enzymes suggest a critical role for the ta
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The authors identified inhibitors of
2021-08-24

The authors identified inhibitors of SUMOylation using two assays to monitor the conjugation of SUMO1 to RanGAP1 by E1 and E2 enzymes: a fluorescence resonance energy transfer (FRET) primary screen that evaluated over 250,000 compounds and a chemiluminescence secondary screen. A counter screen was u
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Mammalian cells have two distinct
2021-08-24

Mammalian kynurenine synthesis have two distinct DNA repair pathways for DSBs, NHEJ and HR. Our data are consistent with the suggestion that the DNA–PK-mediated NHEJ pathway recognizes DSBs faster than the HR pathway and acts before the activation of the DNA damage S-phase checkpoint. The activatio
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