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Previously we have shown that the overexpression of ERR indu
2021-04-20
Previously, we have shown that the overexpression of ERRγ induces exercise-like oxidative muscle remodeling without engaging changes in the expression level or activity of PGC1α (Narkar et al., 2011). In this study, overexpression of ERRγ in PKO muscle reveals that ERRγ-activated target genes can ac
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Docking experiments showed that Me MeGlcA Xyl and
2021-04-20
Docking experiments showed that Me-MeGlcA3Xyl4 and MeGlc3Xyl4 were bound to EcXyn30A and the R293A variant in the same way as MeGlcA3Xyl4, having MeGlcA or its modified forms accommodated in the -2b subsite. All ligands were coordinated by the same apexbt chemicals and no new interactions were obse
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br Halogenases Enzymatic C H
2021-04-20
Halogenases Enzymatic C–H activation leading to halogenation is another emerging area in biocatalysis [55,56]. Incorporation of halogen atoms during medicinal chemistry eff ;orts is a well-established practice, presenting an effective means to control the molecule’s bioactivity and physicochemical
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In conclusion we for the first time demonstrated the enzyme
2021-04-20
In conclusion, we for the first time demonstrated the enzyme activity and immunoprotective traits of bioactive recombinant SjCE-2b, which was successfully recovered by protein refolding from inclusion bodies. The results address two essential questions that were undocumented in previous investigatio
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Due to the high attractiveness of
2021-04-20
Due to the high attractiveness of E2 and E3 ligases as drug targets, a number of drug discovery assays have been published, based on detection by fluorescence (Dudgeon et al., 2010, Krist et al., 2016, Zhang et al., 2004), thymidylate synthase inhibitors (Davydov et al., 2004, Huang et al., 2005, K
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WES and validation by Sanger sequencing in PNGS
2021-04-20
WES and validation by Sanger sequencing in PNGS-252 revealed an apparent homozygous c.4C>G missense alteration (GenBank: NM_014176.3), resulting in the amino HQNO substitution p.Gln2Glu (Figure 1A). This mutation must be very rare, because this is not listed in the NHLBI Exome Sequencing Project or
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br STAR Methods br Acknowledgments We thank the
2021-04-20
STAR★Methods Acknowledgments We thank the City of Hope core facilities, including the Animal Model Core, Bioinformatic Core, NMR Core, Flow Cytometry Core, and Florescence Microscopy Core for excellent technical support, and NIH grants R01GM086171, R01GM102538, and R01CA212119, R01CA216987, an
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NMS-873 synthesis The first hint that GLP
2021-04-20
The first hint that GLP-1 might not be completely stable came from a meeting abstract in 1992, reporting that GLP-1 could be degraded in plasma incubations [16], although the enzyme(s) involved was not identified. A year later, Mentlein and colleagues [17], in a search for peptide substrates of the
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Total synthesis requires the two key intermediates and which
2021-04-20
Total synthesis requires the two key intermediates 3 and 7, which were synthesized using the route described in below. Phenylethylamine 3 was readily synthesized from vanillin or isovanillin; the overall yield was 50–52%. To prepare the intermediates 7, bromination of 2-(4-hydroxyphenyl) acetate wit
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G DH has gained interest because of
2021-04-20
G3DH has gained interest because of its broad substrate specificity and site-selective oxidation properties [9,10]. The conversion product, 3-ketoglycoside, possesses potential as a starting material for the chemical industry such as in polymer and surfactants because the keto group becomes a specif
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Our data show a site
2021-04-20
Our data show a site-specific interaction of DDR2 with collagen II. This indicates that the DDRs recognise a particular sequence within collagen and not simply the collagenous triple helix per se. This common tertiary structure of all collagens is formed by three α chains, each with a repeating G-X-
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In summary our findings show that LPS can activate
2021-04-20
In summary, our findings show that LPS can activate CysLT2R on microglial 490 to induce microglial inflammation and microglia-dependent neuronal death. Furthermore, pharmacological inhibition or knocking down of CysLT2R expression protects neurons against neurotoxicity via suppression of LPS-induce
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BAY 57-1293 Within the Class II receptors the
2021-04-19
Within the Class II receptors, the Type I IFN receptor subunit, IFNAR-1, is exceptional in having four tandem FNIII domains, denoted here D1–D4. This structure appears to have arisen as a tandem BAY 57-1293 of the basic D1/D2 structure; thus, D1 and D3 of IFNAR-1 are more closely related, as are D2
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Compound A and Compound B Fig were
2021-04-19
Compound A and Compound B (Fig. 4) were found in our in vitro screening assays and have similar CRF1 receptor in vitro profiles (Table 1). When binding was investigated using [125I]-CRF in ex vivo assay, Compound A inhibited binding of [125I]-CRF both in the frontal cortex and the pituitary; however
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An increased CK activity was
2021-04-19
An increased CK2 activity was found in septal neuronal Beauvericin dissected from rat embryos after hypoglycemia [36]. These data indicated that CK2 activity is not only regulated by insulin but also by the glucose concentration. One essential step in insulin action is the binding of the hormone to
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