Structural highlights
Function
[LGUL_MOUSE] Catalyzes the conversion of hemimercaptal, formed from methylglyoxal and glutathione, to S-lactoylglutathione. Involved in the regulation of TNF-induced transcriptional activity of NF-kappa-B (By similarity).
Publication Abstract from PubMed
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.
Zopolrestat as a Human Glyoxalase I Inhibitor and Its Structural Basis.,Zhai J, Zhang H, Zhang L, Zhao Y, Chen S, Chen Y, Peng X, Li Q, Yuan M, Hu X ChemMedChem. 2013 Jul 15. doi: 10.1002/cmdc.201300243. PMID:23857942[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Zhai J, Zhang H, Zhang L, Zhao Y, Chen S, Chen Y, Peng X, Li Q, Yuan M, Hu X. Zopolrestat as a Human Glyoxalase I Inhibitor and Its Structural Basis. ChemMedChem. 2013 Jul 15. doi: 10.1002/cmdc.201300243. PMID:23857942 doi:10.1002/cmdc.201300243
