Document Detail


A Non-Ionic Inhibitor with High Specificity for the UDP-Gal Donor Binding Site of Human Blood Group B Galactosyltransferase - Design, Synthesis and Characterization.
MedLine Citation:
PMID:  23406460     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
(5-O-alpha-D-galactopyranosyl)-D-arabinityl-1,3,7-trihydropurine-2,6,8-trione (1) was designed and synthesized as non-ionic inhibitor for the donor binding site of human blood group B galactosyltransferase (GTB). Enzymatic characterization showed 1 to be extremely specific as the highly homologous human N acetylgalactosaminyltransferase (GTA) is not inhibited. The binding epitope of 1 demonstrates a high involvement of the arabinityl linker whereas the galactose residue is only making contact to the protein via its C-2 site, which is very important for the discrimination between galactose and N-acetylgalactosamine, the substrate transferred by GTA. The approach can generate highly specific glycosyltransferase inhibitors.
Authors:
Katrin Schaefer; Nora Sindhuwinata; Thomas Hackl; Miriam P Koetzler; Felix C Niemeyer; Monica M Palcic; Thomas Hubert Peters; Bernd Meyer
Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2013-2-14
Journal Detail:
Title:  Journal of medicinal chemistry     Volume:  -     ISSN:  1520-4804     ISO Abbreviation:  J. Med. Chem.     Publication Date:  2013 Feb 
Date Detail:
Created Date:  2013-2-14     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9716531     Medline TA:  J Med Chem     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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