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In recent years there has been much interest within the
2020-01-13
In recent years, there has been much interest within the endothelin community regarding the possibility that ETA and ETB receptors may form homo- and heterodimers. Heterodimerization of endothelin receptors may provide an explanation for the results mentioned in the previous paragraph and might also
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br Introduction br Structure of the Ku heterodimer associate
2020-01-13
Introduction Structure of the Ku heterodimer associated to DNA The atomic structure of the Ku heterodimer, alone and bound to a small DNA fragment, was recently determined (Walker et al., 2001) and has significantly improved our understanding of DNA recognition by DNA-PK holoenzyme (Fig. 3). B
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br Materials and methods br
2020-01-13
Materials and methods Results Discussion We found that mRNA expression of PCNA significantly was down-regulated in BCP-ALL muscarinic receptor antagonists following co-treatment with doxorubicin and NU7441 (Fig. 6e). Our result is congruent with Gehen et al. study reporting that down-regula
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We have reported previously that aminoacrylate derivatives o
2020-01-13
We have reported previously that β-aminoacrylate derivatives of the general structure () are inhibitors of DHODH. In particular, tricyclic derivatives and displayed sub-micromolar IC values against DHODH, and in the case of there was a 1000-fold greater potency compared to the human enzyme (DHOD
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The CRTH inhibitory activities of the synthesized
2020-01-13
The CRTH2 inhibitory activities of the synthesized compounds are listed in , . At first we introduced halogen or other substituents at the 4,4′-position of phenyl rings in the benzhydryl moiety in order to obtain SAR and to improve the metabolic stability at this moiety (–). It is well-known that in
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Alrestatin Resistance to avermectins has been associated wit
2020-01-11
Resistance to avermectins has been associated with point mutations of GluCls in C. elegans, D. melanogaster, T. urticae and P. xylostella (Dent et al., 2000; Dermauw et al., 2012; Kane et al., 2000; Kwon et al., 2010; Wang et al., 2016a, 2017). Our electrophysiological study found a 8.2-fold reducti
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Estrogen treatment in postmenopausal women
2020-01-11
Estrogen treatment in postmenopausal women requires combination with a progestogen in order to prevent endometrial stimulation. This is not necessary, however, with tibolone as progestogenic activity is associated with its Δ4-metabolite that is formed in the liver, as well as locally in the endometr
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In the present study promoting bile acid synthesis by activa
2020-01-11
In the present study, promoting bile PMX 205 synthesis by activating EP4 receptors was shown to exert protection against hepatic steatosis. This finding may be relevant for treatment of non-alcoholic fatty liver disease, a major cause of liver disease and prominent indication for liver transplantati
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br Activatable bioorthogonal reactions reagents br Cycloprop
2020-01-11
Activatable bioorthogonal reactions/reagents Cyclopropenes as bioorthogonal reagents for IEDDA substrates Cyclopropenes have become popular bioorthogonal reagents due to their small size, inertness to biological nucleophiles, ability to be genetically encoded (Yu et al., 2012), and participati
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In looking at exist http www apexbt
2020-01-11
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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br Acknowledgements We would like to thank
2020-01-11
Acknowledgements We would like to thank Dr Ron Mason (NIEHS, Research Triangle Park, NC) for helpful discussion regarding the analysis of CCl4 metabolism, to Dr Karla Thrall and Dr Rick Corley (Battelle) for helpful discussions regarding study design and data interpretation, and to Jim Merdink an
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Recently Schenck et al identified an active
2020-01-11
Recently, Schenck et al. [25] identified an active site asparagine 222 (N222) residue in the Glycine max TyrAp/PDH (GmPDH1) that is responsible for its prephenate substrate specificity. Mutating the single N222 into an acidic residue (i.e. aspartate, D) in the legume TyrAp/PDH shifted from prephenat
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Introduction Cytochrome P CYP A is the most
2020-01-11
Introduction Cytochrome P450 (CYP)3A is the most important enzyme involved in the metabolism of 30–40% of currently prescribed drugs [1]. The Bikinin level and activity of CYP3A show large intra- and inter-individual variability, which contributes to unpredictable drug response and toxicity. A mult
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Leupeptin br Results and discussion br Conclusion
2020-01-11
Results and discussion Conclusion Experimental section Pharmacological studies Introduction Survival analysis is a set of statistical methods that aim at modeling the relationship between a set of predictor variables and an outcome variable and, in particular, prediction of the time w
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However the Moon is not the only
2020-01-11
However, the Moon is not the only possible source for space resources. Asteroids, in particular near-Earth asteroids (NEAs), can provide an alternative source for propellant and other materials, sometimes at lower cost. There are an expected 4000 NEAs that require less propellant (delta-V) per trip
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