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- W2156559305 startingPage "15346" @default.
- W2156559305 abstract "Abstract A series of ten glycosyltransferase inhibitors has been designed and synthesized by using pyridine as a pyrophosphate surrogate. The series was prepared by conjugation of carbohydrate, pyridine, and nucleoside building blocks by using a combination of glycosylation, the Staudinger–Vilarrasa amide‐bond formation, and azide–alkyne click chemistry. The compounds were evaluated as inhibitors of five metal‐dependent galactosyltransferases. Crystallographic analyses of three inhibitors complexed in the active site of one of the enzymes confirmed that the pyridine moiety chelates the Mn 2+ ion causing a slight displacement (2 Å) from its original position. The carbohydrate head group occupies a different position than in the natural uridine diphosphate (UDP)–Gal substrate with little interaction with the enzyme." @default.
- W2156559305 created "2016-06-24" @default.
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- W2156559305 creator A5041664332 @default.
- W2156559305 creator A5043701724 @default.
- W2156559305 creator A5068293169 @default.
- W2156559305 date "2013-09-23" @default.
- W2156559305 modified "2023-10-18" @default.
- W2156559305 title "Design of Glycosyltransferase Inhibitors: Pyridine as a Pyrophosphate Surrogate" @default.
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- W2156559305 doi "https://doi.org/10.1002/chem.201301871" @default.
- W2156559305 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/24108680" @default.
- W2156559305 hasPublicationYear "2013" @default.
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