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The possibility that a carboxyl group attached to the
2020-02-26
The possibility that a carboxyl group attached to the or position of an -arylaminomethylenemalonate ester would lead to increased selectivity for DHODH has been tested and found not to be the case. Indeed, reduced selectivity compared with the corresponding ester is observed and is attributed to a ‘
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Next the BE obtained for the different
2020-02-26
Next, the BE obtained for the different complexes were evaluated. From the BE obtained from our MD simulations, a very good binder can be differentiated from a very weak binder (−11.85 kcal/mol for MTX vs. −6.74 and −3.61 kcal/mol for compounds 14b and 15c, respectively) but ligands with similar bin
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Due to cell cell interactions high concentrations of
2020-02-25
Due to cell-cell interactions, high concentrations of LTs can be locally generated in a short period of time during an inflammatory response, thus potentiating LT function. The cellular communication can be mediated between immune cells as well as between immune cells other cell types. Several studi
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Our results also showed that the highest dose
2020-02-25
Our results also showed that the highest dose of Astressin2-B increased the rewarding effects of cocaine, since non-defeated animals treated with this dose developed CPP with a sub-threshold dose. We monitored the acute effects of 30 µg/kg of Astressin2-B and found an increase of anxiety in the open
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Having generated synthetic cytokines and synthetic
2020-02-25
Having generated synthetic cytokines and synthetic cytokine receptors, the logical next step has been to design fully synthetic cytokine/cytokine receptor systems, modifying either cytokine/cytokine receptor binding interfaces or cytokine-unrelated combinations of substances and their binding domain
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br Conclusion Blueberry is becoming a
2020-02-25
Conclusion Blueberry is becoming a worldwide crop with the fastest rising consumer demand trends for its health benefits. However, the berry size is one of the key parameters for determining fruit quality and consumers’ preferences (Milic et al., 2018). Understanding the physiological and molecul
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Data on optimal hormone formulations
2020-02-25
Data on optimal hormone formulations, routes of administration, doses and duration of hormone use in young women with POF are lacking (Box 1). Transdermal BGJ398 administration, which avoids the first-pass hepatic circulation and the increase in inflammatory markers such as C-reactive protein, whil
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In contrast irinotecan has shown much less myelosuppression
2020-02-25
In contrast, irinotecan has shown much less myelosuppression and may be more active in Ewing sarcoma both alone and in combination with temozolamide. One phase II study of 13 heavily pretreated Ewing sarcoma patients demonstrated a response rate of 38% including 2 complete responses (Bisogno et al.,
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Eeyarestatin I Enlarging the ligand binding pocket by reduct
2020-02-25
Enlarging the ligand-binding pocket by reduction of the size of the residue F435 switched DES to an agonist indicating that F435 is involved in mediating the antagonistic effect of DES (Fig. 7E) [13]. The conformation of the smaller side chain of L435 was either not altered by DES or was too small t
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Materials and methods br Results Assay of botulinum toxin ac
2020-02-25
Materials and methods Results Assay of botulinum toxin activity is critical for the risk-assessment, diagnosis, and treatment of botulism cases. The frequently encountered active forms of the toxin are; L chain (inside intoxicated neuronal cells), BoNT (in the blood stream of a botulism patient,
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br Conflicts of interest br Acknowledgements This work
2020-02-25
Conflicts of interest Acknowledgements This work was supported by the Swiss National Science Foundation No 31003A-179400 to AO. We thank Dr. Thierry Langer, University of Vienna and Inte:Ligand GmbH, for providing the LigandScout Software, and Dr. Daniela Schuster, Paracelsus Medical Universit
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br Multi subunit RINGs There are RING type E s
2020-02-25
Multi-subunit RINGs There are RING-type E3s that exist as multi-subunit assemblies (see Fig. 3B). A striking example is the Cullin RING Ligase (CRL) superfamily [35], which exhibits enormous plasticity in substrate specificity. Each CRL subfamily is characterized by a cullin protein (Cul-1, 2, 3,
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br Results br Discussion Previous studies have mapped ABCF a
2020-02-25
Results Discussion Previous studies have mapped ABCF1 as a risk factor gene for rheumatoid arthritis and autoimmune pancreatitis (Ota et al., 2007, Richard et al., 1998). Additionally, recent genome-wide association studies have also associated ABCF1 with the risk of gout (Dong et al., 2017) a
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p as a cyclin dependent kinase inhibitor exert significant
2020-02-25
p21, as a cyclin-dependent kinase inhibitor, exert significant negative regulator of proliferation, and it could be transcriptional upregulated by p53 in order to impel transient AGI5198 mg arrest (Romanov et al., 2010). Using western blotting, we found that the protein expression of p21 upgrades f
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In regards to regional variation in metabolic behavior of
2020-02-24
In regards to regional variation in metabolic behavior of adipose tissue, subcutaneous adipose tissue transplantation has been shown to reprogram visceral adipose tissue to have subcutaneous-like phenotypic behavior, whereas visceral-to-subcutaneous transplantation does not promote a more detrimenta
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