Systematic Strategy for Developing Glycosyltransferase Inhibitors: Diversity-Oriented Synthesis of FUT8 Inhibitors
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Systematic Strategy for Developing Glycosyltransferase Inhibitors : Diversity-Oriented Synthesis of FUT8 Inhibitors. / Manabe, Yoshiyuki; Hizume, Koki; Takakura, Yohei; Takamatsu, Shinji; Miyoshi, Eiji; Kamad, Yoshihiro; Hurtado-Guerrer, Ramón; Fukase, Koichi.
I: Synlett, Bind 35, Nr. 11, 2024, s. 1273-1278.Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › fagfællebedømt
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TY - JOUR
T1 - Systematic Strategy for Developing Glycosyltransferase Inhibitors
T2 - Diversity-Oriented Synthesis of FUT8 Inhibitors
AU - Manabe, Yoshiyuki
AU - Hizume, Koki
AU - Takakura, Yohei
AU - Takamatsu, Shinji
AU - Miyoshi, Eiji
AU - Kamad, Yoshihiro
AU - Hurtado-Guerrer, Ramón
AU - Fukase, Koichi
N1 - Publisher Copyright: © 2023 Georg Thieme Verlag. All rights reserved.
PY - 2024
Y1 - 2024
N2 - Glycans control various biological processes depending on their structures. Particularly, core fucose, formed by a1,6-fucosyltransferase (FUT8), has a substantial influence on multiple biological processes. In this study, we investigated the development of FUT8 inhibitors with structural elements encompassing both the glycosyl donor (GDP-fucose) and acceptor (N-glycan) of FUT8. To efficiently optimize the structure of FUT8 inhibitors, we employed a strategy involving fragmentation of the target structure, followed by the structure optimization using diversity-oriented synthesis approaches. This study proposes an efficient strategy to accelerate the structural optimization of middle molecules.
AB - Glycans control various biological processes depending on their structures. Particularly, core fucose, formed by a1,6-fucosyltransferase (FUT8), has a substantial influence on multiple biological processes. In this study, we investigated the development of FUT8 inhibitors with structural elements encompassing both the glycosyl donor (GDP-fucose) and acceptor (N-glycan) of FUT8. To efficiently optimize the structure of FUT8 inhibitors, we employed a strategy involving fragmentation of the target structure, followed by the structure optimization using diversity-oriented synthesis approaches. This study proposes an efficient strategy to accelerate the structural optimization of middle molecules.
KW - compound library
KW - diversity-oriented synthesis
KW - glycosyltransferase
KW - inhibitor
KW - middle molecule
U2 - 10.1055/a-2221-9096
DO - 10.1055/a-2221-9096
M3 - Journal article
AN - SCOPUS:85179737044
VL - 35
SP - 1273
EP - 1278
JO - SYNLETT: Accounts and Rapid Communications in Chemical Synthesis
JF - SYNLETT: Accounts and Rapid Communications in Chemical Synthesis
SN - 0936-5214
IS - 11
ER -
ID: 389365237