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In summary we have identified a series of
2019-12-26
In summary, we have identified a series of amides as ERRγ agonists with suitable potency for further development. Our SAR studies of this chemotype identified SR19881 as the most potent full agonist of ERRγ with an EC=0.39 μM in a binding assay and an EC=4.7 μM in a cell-based assay. SR19881 was als
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EphB and ephrinB mRNA levels were
2019-12-26
EphB4 and ephrinB2 mRNA levels were determined from three parts taken from each tumor, and each sample was analyzed in triplicate. The differences in the histoscores and mRNA levels of EphB4 and ephrinB2 were analyzed by Student\'s t test. The correlation coefficients were evaluated both by linear r
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CI 976 We found that Th cells
2019-12-26
We found that Th17 cells, derived either from in vivo immunization or in vitro polarization under pathogenic conditions (in presence of IL-23 and/or IL-1β) expressed high levels of EBI2. In contrast, Th17 CI 976 that were generated in absence of IL-23 or IL-1β lost EBI2 expression during differentia
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Oxidation of N hydroxyguanidine by DbH was studied by HPLC
2019-12-26
Oxidation of N-hydroxyguanidine 1 by DbH was studied by HPLC and some oxidation products for 1 could be characterized. The compounds generally observed with iron-containing systems are 4-methoxyphenylurea 11 and 4-methoxyphenylcyanamide 12 (Fig. 2). Oxidation of N-(4-chlorophenyl)-N′-hydroxyguanidin
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br Acknowledgements br Introduction Serum triglyceride conce
2019-12-26
Acknowledgements Introduction Serum triglyceride concentrations increase following ingestion of a fat containing meal resulting in postprandial hyperlipidemia. Peak serum triglyceride levels are observed within 2 to 4h of fat consumption and then gradually return to baseline levels within appr
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Acknowledgments The authors thank Dr Vladimir
2019-12-24
Acknowledgments The authors thank Dr. Vladimir Poltoratsky and Zhihui Xiao for their help with the in vitro FRET assay. Support for this research was provided by Saint John’s University. Introduction We predicted the existence of endothelium-derived contractile factors (EDCFs) in 1982 [1]. In
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Therefore the SPH algorithm in AUTODYN D was used to
2019-12-24
Therefore, the SPH algorithm in AUTODYN-3D™ was used to simulate the experiment in Ref. [5] to verify the credibility of the numerical simulation method by results that could be measured accurately. Then the verified numerical simulation method was used to simulate BAD generated by RHA subjected to
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br Discussion EFTs are sarcomas with almost undifferentiated
2019-12-24
Discussion EFTs are sarcomas with almost undifferentiated histologic features, consequently their differentiation from other small, blue, round cell tumors may be difficult. Substantial intracellular 59 7 on PAS stain is a useful diagnostic feature. The addition of CD99 and FLI1 immunohistochemi
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br Results br Discussion Fetal development occurs under cond
2019-12-24
Results Discussion Fetal development occurs under conditions of low oxygen tension and steady maternal glucose such that physiologic systems including the pancreas are functionally poised in the prenatal state. Postnatally, oxidative metabolism becomes dominant and intermittent feeding exposes
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br Introduction Rhabdomyosarcoma RMS is a myogenic tumor tha
2019-12-24
Introduction Rhabdomyosarcoma (RMS) is a myogenic tumor that accounts for approximately 50% of all pediatric soft tissue sarcomas. Diagnostic criteria for RMS pkd kinase on the validation of proteins of the skeletal muscle lineage, such as Desmin, MyoD or Myogenin [1]. RMS cells are persistently
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br Target enzyme attributes and
2019-12-24
Target enzyme attributes and substrate peptide selection Protein kinases catalyze the phosphorylation of serine, threonine, and tyrosine residues in both proteins and peptides using ATP as the phosphoryl donor. The human kinome is comprised of 518 protein kinases and 40 lipid kinases. The vast ma
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TraM is one of two transfer proteins from pIP
2019-12-24
TraM is one of two transfer proteins from pIP501 T4SS that have structural similarity to the A. tumefaciens VirB8 protein (Fercher et al., 2016, Goessweiner-Mohr et al., 2013), a central member of the inner membrane complex (Bailey et al., 2006, Guglielmini et al., 2014, Trokter et al., 2014). VirB8
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Our study provides proof of principle for dimerizing
2019-12-24
Our study provides proof of principle for dimerizing two different E3 ligases as a novel approach to inducing one ligase to degrade the other one. The outcome of ‘ligase versus ligase’ PROTAC-mediated activity might be unpredictable a priori, but could reveal a new mechanism for proximity-mediated h
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In humans several different small
2019-12-24
In humans, several different small ubiquitin-related modifier (SUMO) paralogs can be conjugated to cellular proteins. The human genome codes for five SUMO paralogs (SUMO1–5); of these, SUMO1 and the almost identical SUMO2 and SUMO3 are ubiquitously expressed. Sumoylation is executed by an enzymatic
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SIRT is a representative member
2019-12-24
SIRT1 is a representative member of Sirtuins, which is a family of highly conserved NAD+-dependent class III histone deacetylases. SIRT1 deacetylates plentiful nonhistone protein substrates [Atgs, Foxo1, Foxo3, PGC-1α, NF-kB, E2F1 and p53] (Conrad et al., 2016; Gu et al., 2016; Tu et al., 2018) to p
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