Zopolrestat as a Human Glyoxalase I Inhibitor and Its Structural Basis

Old drugs new tricks: Zopolrestat, an aldose reductase inhibitor developed by Pfizer for the treatment of diabetic complications, is a potent competition inhibitor of human glyoxalase I (GLOI) in vitro. Crystal structures of GLOI in complex with zopolrestat and indomethacin, a nonsteroidal anti‐infl...

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Published in:ChemMedChem 2013-09, Vol.8 (9), p.1462-1464
Main Authors: Zhai, Jing, Zhang, Hong, Zhang, Ligping, Zhao, Yining, Chen, Sangke, Chen, Yunyun, Peng, Xinyu, Li, Qing, Yuan, Minggui, Hu, Xiaopeng
Format: Article
Language:English
Subjects:
Animals
Anti-Inflammatory Agents, Non-Steroidal - chemistry
Anti-Inflammatory Agents, Non-Steroidal - metabolism
Benzothiazoles - chemistry
Benzothiazoles - metabolism
Binding Sites
crystal structures
Crystallography, X-Ray
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - metabolism
glyoxalase I
Humans
indomethacin
Indomethacin - chemistry
Indomethacin - metabolism
inhibitors
Lactoylglutathione Lyase - chemistry
Lactoylglutathione Lyase - metabolism
Mice
Phthalazines - chemistry
Phthalazines - metabolism
Protein Binding
Protein Structure, Tertiary
zinc metalloenzymes
zopolrestat
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Summary:Old drugs new tricks: Zopolrestat, an aldose reductase inhibitor developed by Pfizer for the treatment of diabetic complications, is a potent competition inhibitor of human glyoxalase I (GLOI) in vitro. Crystal structures of GLOI in complex with zopolrestat and indomethacin, a nonsteroidal anti‐inflammatory drug and moderate inhibitor of GLOI, provide a structural basis for the development of novel GLOI inhibitors with excellent pharmacokinetics profiles.
ISSN:1860-7179
1860-7187
DOI:10.1002/cmdc.201300243