Human placental beta1,4-galactosyltransferase-I (EC 2.4.1.38) transfers the galactosyl moiety from UDP-Gal to various GlcNAc or Glc acceptors in vivo. Here, we describe the construction of its Y284L mutant as a His(6)propeptide-catbeta4GalT1 construct, in which the Gal-transferase activity was totally abolished in favor of its GalNAc-transferase activity. We used this mutant in the synthesis of three mono- and bivalent LacdiNAc glycomimetics with good yields. These compounds proved to be powerful ligands of two activation receptors of natural killer cells, NKR-P1 and CD69. A synthetic bivalent tethered di-LacdiNAc is the best currently known precipitation agent for both of these receptors and has promising potential for the development of immunoactive glycodrugs.
- MeSH
- bakteriální proteiny metabolismus MeSH
- Campylobacter jejuni enzymologie MeSH
- CD antigeny metabolismus MeSH
- diferenciační antigeny T-lymfocytů metabolismus MeSH
- epimerázy sacharidů metabolismus MeSH
- galaktosyltransferasy genetika metabolismus MeSH
- glykokonjugáty biosyntéza chemická syntéza metabolismus MeSH
- laktosa analogy a deriváty biosyntéza chemická syntéza metabolismus MeSH
- lektinové receptory NK-buněk - podrodina B metabolismus MeSH
- lektiny typu C MeSH
- lidé MeSH
- mutace MeSH
- placenta enzymologie MeSH
- substrátová specifita MeSH
- těhotenství MeSH
- Check Tag
- lidé MeSH
- těhotenství MeSH
- ženské pohlaví MeSH
- Publikační typ
- práce podpořená grantem MeSH
- publikace stažené z tisku MeSH
