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New Potent Sialyltransferase Inhibitors—Synthesis of Donor and of Transition‐State Analogues of Sialyl Donor CMP‐Neu5Ac
Author(s) -
Amann Franz,
Schaub Christoph,
Müller Bernd,
Schmidt Richard R.
Publication year - 1998
Publication title -
chemistry – a european journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.687
H-Index - 242
eISSN - 1521-3765
pISSN - 0947-6539
DOI - 10.1002/(sici)1521-3765(19980615)4:6<1106::aid-chem1106>3.0.co;2-7
Subject(s) - sialyltransferase , transition (genetics) , chemistry , substrate (aquarium) , transition state analog , stereochemistry , enzyme , substrate specificity , biochemistry , active site , biology , ecology , gene
New concepts for substrate‐ and transition‐state‐derived sialyltransferase inhibitors are deduced from enzymatic sialyl transfer with CMP‐Neu5Ac as donor substrate. On this basis, transition‐state analogue ( R )‐ 1 was synthesized, which inhibits α (2–6)‐sialyltransferase from rat liver, an important lead for further investigations.