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Synthesis of a Bisubstrate‐Type Inhibitor of N ‐Acetylglucosaminyltransferases
Author(s) -
Hanashima Shinya,
Manabe Shino,
Inamori Keiichiro,
Taniguchi Naoyuki,
Ito Yukishige
Publication year - 2004
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.200460388
Subject(s) - chemistry , aqueous medium , combinatorial chemistry , linkage (software) , acceptor , enzyme , coupling (piping) , stereochemistry , aqueous solution , biochemistry , organic chemistry , materials science , physics , metallurgy , gene , condensed matter physics
Transfer interference : Synthesis of the bisubstrate‐type N ‐acetylglucosaminyltransferase (GnT) inhibitor 1 was achieved by a polymer‐resin hybrid capture–release strategy for the construction of the acceptor component. One‐pot ligation in aqueous media produced the coupling product, and subsequent construction of a diphosphate linkage led to 1 . Inhibitory activities toward GnT‐V and GnT‐IX were evaluated and revealed the potency of 1 toward the latter enzyme.