Source:http://linkedlifedata.com/resource/pubmed/id/17507233
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
14
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pubmed:dateCreated |
2007-6-6
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pubmed:abstractText |
The trisaccharide substructure 13 of the ganglioside GQ1balpha shows a remarkable affinity for the myelin-associated glycoprotein (MAG). In the search for structurally simplified and pharmacokinetically improved mimics of 13, sialosides with modifications at the reducing and non-reducing end were synthesized. The biological evaluation of mimics 12a-o was performed in a competitive target-based assay. It was found that the relative inhibitory potency (rIP) of antagonist 12h was enhanced by more than 1000-fold in comparison to the reference trisaccharide 13, despite the former having a much simpler structure. In addition, the sialic acid derivatives, for example, 12h, have clearly improved pharmacokinetic properties due to the presence of aromatic moieties, a lower molecular weight, and a reduced number of polar hydroxy functions compared to the reference compound 13.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Jul
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pubmed:issn |
0968-0896
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
15
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pubmed:volume |
15
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
4951-65
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pubmed:meshHeading |
pubmed-meshheading:17507233-Animals,
pubmed-meshheading:17507233-CHO Cells,
pubmed-meshheading:17507233-Cricetinae,
pubmed-meshheading:17507233-Cricetulus,
pubmed-meshheading:17507233-Inhibitory Concentration 50,
pubmed-meshheading:17507233-Ligands,
pubmed-meshheading:17507233-Molecular Structure,
pubmed-meshheading:17507233-Myelin-Associated Glycoprotein,
pubmed-meshheading:17507233-N-Acetylneuraminic Acid,
pubmed-meshheading:17507233-Structure-Activity Relationship
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pubmed:year |
2007
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pubmed:articleTitle |
Synthesis of sialic acid derivatives as ligands for the myelin-associated glycoprotein (MAG).
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pubmed:affiliation |
Institute of Molecular Pharmacy, Pharmacenter, University of Basel, Klingelbergstrasse 50, CH-4056 Basel, Switzerland.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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