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Conventional aromatic radiofluorination via nucleophilic sub
2019-08-09
Conventional aromatic radiofluorination via nucleophilic substitution requires electron-withdrawing activating group(s) at the ortho or para position to achieve good radiolabeling yield. In the case of CJ-042794 (), the phenoxy substitution para to the fluoro group is considered an electro-donating
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To provide a brief critical evaluation of this technology an
2019-08-09
To provide a brief critical evaluation of this technology and an outlook, we note that performance of SMEPT is critically dependent on each of the components making up this platform, namely the substrate, the enzyme, and the prodrug. With regards to the latter, SMEPT is built on the experience and s
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To provide a brief critical evaluation of this technology an
2019-08-09
To provide a brief critical evaluation of this technology and an outlook, we note that performance of SMEPT is critically dependent on each of the components making up this platform, namely the substrate, the enzyme, and the prodrug. With regards to the latter, SMEPT is built on the experience and s
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In looking at exist http www apexbt com media diy
2019-08-09
In looking at existing FGE substrates from other organisms, there are no reported effects on conversion efficiency of the general XCXPXRX pattern with respect to placement within or at the N′ or C′ terminus of polypeptides, and it has been suggested that the aldehyde formation is independent of the
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The EGFR belongs to the
2019-08-09
The EGFR belongs to the ErbB family of receptor tyrosine kinases (RTKs), comprised of four members: EGFR (ErbB1, HER1), HER2 (ErbB2), HER3 (ErbB3) and HER4 (ErbB4) [24]. HER receptors are activated by a group of epidermal growth factor (EGF) ligands and undergo homo- or hetero-dimerization during th
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Modulating protein stability specifically inhibiting ubiquit
2019-08-09
Modulating protein stability, specifically inhibiting ubiquitin E3 ligases, provides potential advantages over other druggable targets given the presence of biochemically multiple, unique pharmacophores within complexes that can bind a variety of small molecules [12]. The FBXO3 inhibitors used here
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Main Text Post translational modifications by ubiquitin Ub a
2019-08-09
Main Text Post-translational modifications by ubiquitin (Ub) and ubiquitin-like proteins (Ubl) regulate a diverse array of cellular and physiological processes including protein degradation, localization, and activation. While ubiquitination has primary responsibility for targeting substrates for p
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COH inhibited global SUMOylation in cells and
2019-08-09
COH000 inhibited global SUMOylation in β-Funaltrexamine hydrochloride and blocked the E1 catalyzed attachment of SUMO to the corresponding conjugating enzyme Ubc9, but not the attachment of ubiquitin or NEDD8 to their respective E2s, confirming inhibition and specificity in cellulo. Consistent with
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The consistent anti anxiety effects obtained
2019-08-08
The consistent anti-anxiety effects obtained with intra-mPFC injections of CP 376395 strongly suggest a tonic role of CRF at CRF1 receptors located within this limbic jasplakinolide powder area in the modulation of anxiety in the mouse on the EPM. Intra-mPFC injection of CP 376395 led mice to explor
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There have been attempts to stimulate the dopaminergic
2019-08-08
There have been attempts to stimulate the dopaminergic system to influence cognition in women around menopause who have subjective complaints about their cognition by Epperson et al. (Epperson et al., 2011, Epperson et al., 2015). In perimenopausal and postmenopausal women, Epperson et al. found tha
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br STAR Methods br Acknowledgments
2019-08-08
STAR★Methods Acknowledgments We thank members of R.L. lab and F. Schweisguth for critical reading of the manuscript. We are also grateful to F. Janody, M. Miura, C. Bökel, H.D. Ryoo, G. Jiménez, the Bloomington Drosophila Stock Center, the Drosophila Genetic Resource Center, the Vienna Drosoph
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br Acknowledgement We acknowledge for funding support
2019-08-08
Acknowledgement We acknowledge for funding support from Maryada Foundation, a DoD/Army Contract No. W911NF-06-1-0095, and National Institutes of Health through the New England Center of Excellence for Biodefense (Grant AI057159-01). Introduction The Gram-negative bacterium Lysobacter sp. XL1
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The loss of secondary mutation T M
2019-08-08
The loss of secondary mutation T790M mutation after AR and SCLC transformation was also reported for Rociletinib. Piotrowska et al. using the MGH NGS platform recently reported in 13 biopsies among 12 EGFR T790M+ patients progressing after treatment with Rociletinib the loss of EGFR T790M mutation i
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Introduction Activation of epidermal growth factor receptor
2019-08-08
Introduction Activation of epidermal growth factor receptor (EGFR)-receptor tyrosine kinases (RTKs) is a key factor in the progression of non-small cell lung cancer (NSCLC). EGFR-RTKs cause proliferation, invasion, metastasis, and angiogenesis, as well as suppress apoptosis, in lung adenocarcinoma
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How does an increase in E affinity for
2019-08-08
How does an increase in E2 affinity for the RING domain favor higher activity and polyubiquitination by the E2? Binding of the RING domain to the E2 positions the donor Ub in the E2~Ub conjugate in a closed complex [16], [17], [18] that increases the reactivity of the thioester [60]. A higher affini
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