number of access : ?
number of downloads : ?
ID 115431
Author
Toguchi, Shohei Kitasato University
Hirose, Tomoyasu Kitasato University
Sharpless, K. Barry The Scripps Research Institute
Ōmura, Satoshi Kitasato University
Sunazuka, Toshiaki Kitasato University
Keywords
fragment-based lead discovery
templated reaction
ligand-binding site
drug discovery
triazole formation
ligand affinity
Content Type
Journal Article
Description
In situ click chemistry is a target-guided synthesis approach for discovering novel lead compounds by assembling organic azides and alkynes into triazoles inside the affinity site of target biogenic molecules such as proteins. We report in situ click chemistry screening with human D-amino acid oxidase (hDAO), which led to the identification of a more potent hDAO inhibitor. The hDAO inhibitors have chemotherapeutic potential as antipsychotic agents. The new inhibitor displayed competitive inhibition of hDAO and showed significantly increased inhibitory activity against hDAO compared with that of an anchor molecule of in situ click chemistry.
Journal Title
Chemical and Pharmaceutical Bulletin
ISSN
00092363
13475223
NCID
AA00602100
Publisher
The Pharmaceutical Society of Japan
Volume
64
Issue
7
Start Page
695
End Page
703
Published Date
2016-07-01
EDB ID
DOI (Published Version)
URL ( Publisher's Version )
FullText File
language
eng
TextVersion
Publisher
departments
Institute of Advanced Medical Sciences