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ptc chemical Acknowledgments br Introduction Various researc
2020-09-27
Acknowledgments Introduction Various researches have been made in the field of the treatment of cancer and inflammatory diseases. Different mechanisms are involved in the progression of cellular damage that gives an idea about new drug targets. There are always some efforts to improve efficacy,
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Among prostaglandins PG PGD remained the most elusive specie
2020-09-27
Among prostaglandins (PG), PGD2 remained the most elusive species for a long time and was initially regarded as having negligible biological activity [1]. In 1974 its inhibitory effect on platelet aggregation was discovered by Smith et al. [2] and Mills & McFarlain [3], and both pressor and depresso
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br Results br Discussion Unraveling the
2020-09-27
Results Discussion Unraveling the molecular details of nucleoporin-karyopherin interactions, which have to be strong enough to promote transport but sufficiently weak to avoid stalling of transport complexes within the pore, is key to our understanding of the mechanisms of nucleocytoplasmic tr
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The small GTPase Ran regulates karyopherin
2020-09-27
The small GTPase Ran regulates karyopherin–cargo interactions and the directionality of karyopherin-mediated transport. Like other Ras-family GTPases, Ran cycles between GTP- and GDP-bound states, and the two surface loops in Ran, referred to as the switch I and switch II loops, undergo significant
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br Clinical trials of CRM
2020-09-27
Clinical trials of CRM1 inhibitors KPT-330 clinical trials have been initiated with promising very early results. One trial includes patients with advanced solid tumors whose disease has progressed after at least one prior therapy for metastatic disease (NCT01607905). Another trial includes patie
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Elevated homocysteine has been considered to be a
2020-09-27
Elevated homocysteine has been considered to be a risk factor for vascular dysfunction, vascular disease, and preeclampsia , . The methionine-homocysteine metabolism is responsible for supplying COMT with the methyl-group donor (-adenosyl methionine; SAM) necessary for 2-ME synthesis, and alteration
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br Study design br Results To explore
2020-09-27
Study design Results To explore potential differences in the volume the different swabs absorb, the loss of weight of tubes filled with water after soaking the different swabs under defined conditions was determined. This revealed that the different swabs absorbed between approximately 0.07 an
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Future advances in the in
2020-09-25
Future advances in the in vivo molecular imaging of enzyme activity will greatly benefit from the progress towards the quantitative detection of enzymes. Quantitative imaging requires knowledge of both the location and concentration of a specific enzyme, which is dependent on the simultaneous measu
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The synthetic route chosen for the preparation of the substr
2020-09-25
The synthetic route chosen for the preparation of the substrates 18 is shown in Scheme 3. Commercially available 4-aminobenzyl alcohol 13 was found to be relatively unstable to storage and hence it was prepared immediately before use by reduction of the readily available and inexpensive 4-nitrobenzy
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More than thirty enzymes with PLA activity
2020-09-25
More than thirty enzymes with PLA2 activity have been described and, based on sequence similarities, they are currently classified in 16 groups, each containing several sub-groups [16]. However, based on biochemical features these enzymes are frequently grouped into six major families: secreted phos
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OxLDL down regulates eNOS and up regulates iNOS
2020-09-25
OxLDL down-regulates eNOS and up-regulates iNOS, thereby augmenting the formation of NO and protein S-nitrosylation in human endothelial STF 31 [26]. Importantly, iNOS-mediated S-nitrosylation plays an increasingly significant role in cardiovascular diseases [34]. For example, iNOS-mediated IRE1α S
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Methacholine MCh is a bronchoconstrictive agent
2020-09-25
Methacholine (MCh) is a bronchoconstrictive agent that has been widely used in the diagnoses of airway narrowing and hyperresponsiveness (Jonasson et al., 2009). MCh induces muscle contractions by stimulating the muscarinic cholinergic receptors that are found in both the airways and the lung parenc
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br Conflicts of interest br Acknowledgements This work was s
2020-09-25
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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Accordingly we prepared three compounds and as
2020-09-25
Accordingly, we prepared three compounds (, , and ) as shown in . Condensation of commercially available VUF 11207 fumarate with glycine methyl ester gave amide . A Friedel–Crafts reaction between compound and 4-methyl valeryl chloride in the presence of aluminum chloride mainly produced undesir
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Despite the important agronomic traits
2020-09-25
Despite the important agronomic traits regulated by SUMO, most research studies on SUMOylation have been mainly limited to model plants, such as Arabidopsis and rice (Wang et al., 2011), due to the lack of molecular tools specific to other economically relevant plants. On the other hand, plants harb
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