
Bioorganic and Medicinal Chemistry Letters p. 4533 - 4537 (2014)
Update date:2022-08-04
Topics:
Hanashima, Shinya
Korekane, Hiroaki
Taniguchi, Naoyuki
Yamaguchi, Yoshiki
N-Acetylglucosaminyltransferase (GnT) III is a glycosyltransferase which produces bisected N-glycans by transferring GlcNAc to the 4-position of core mannose. Bisected N-glycans are involved in physiological and pathological processes through the functional regulation of their carrier proteins. An understanding of the biological functions of bisected glycans will be greatly accelerated by use of specific inhibitors of GnT-III. Thus far, however, such inhibitors have not been developed and even the substrate-binding mode of GnT-III is not fully understood. To gain insight into structural features required of the substrate, we systematically synthesized four N-glycan units, the branching parts of the bisected and non-bisected N-glycans. The series of syntheses were achieved from a common core trimannose, giving bisected tetra- and hexasaccharides as well as non-bisected tri- and pentasaccharides. A competitive GnT-III inhibition assay using the synthetic substrates revealed a vital role for the Manβ(1-4)GlcNAc moiety. In keeping with previous reports, GlcNAc at the α1,3-branch is also involved in the interaction. The structural requirements of GnT-III elucidated in this study will provide a basis for rational inhibitor design.
Changzhou Anyi Biochem Co., Ltd.(expird)
Contact:+86-519-88836158
Address:no,51 caoda
Ningbo Tide Imp. & Exp. Co., Ltd.
Contact:+86-571-8993 7933; +86-571-8993 6453
Address:7/F Anno Domini Building, Tower South, 8 Qiu Shi Road,Hangzhou,China.
Melone Pharmaceutical Co., ltd
Contact:+86-411 82593920, 82593631
Address:No 232, JInma Roda, Development Zone, Dalian, China
Nanjing Raise Pharmatech Co., Ltd
website:http://www.raisechem.com
Contact:+86-25-58649566
Address:B381,No.606,Ningliu Road,Jiangbei New Area,Nanjing,Jiangsu Province,China
Jiaxing Anrui Material Technology Co., Ltd.
Contact:86-573-82651652 13305832579
Address:Room 407, Technology Building, 1369 Chennan Road, Jiaxing City, Zhejiang, China
Doi:10.1021/jo01323a001
(1979)Doi:10.1016/j.tetasy.2004.01.021
(2004)Doi:10.1021/ol0499046
(2004)Doi:10.7164/antibiotics.31.985
(1978)Doi:10.1002/jps.2600671009
(1978)Doi:10.1002/chem.200305386
(2004)