Synthesis of a Bisubstrate‐Type Inhibitor of  N ‐Acetylglucosaminyltransferases | Zendy

Hanashima Shinya | Zendy; Manabe Shino | Zendy; Inamori Keiichiro | Zendy; Taniguchi Naoyuki | Zendy; Ito Yukishige | Zendy

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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.

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