S-(nitrocarbobenzoxy)glutathiones: potent competitive inhibitors of mammalian glyoxalase II.
Three potent competitive inhibitors of mammalian liver glyoxalase II, the S-(o-, m-, and p-nitrocarbobenzoxy)-glutathiones, have been synthesized and studied. The Ki values of the ortho, meta, and para isomers, as inhibitors of rat liver glyoxalase II, were 15, 9, and 6.5 microM, respectively. While showing marked competitive inhibition of glyoxalase II, the glutathione derivatives were almost inactive as inhibitors of glyoxalase I. For example, with the para isomer, [I]0.5 values for rat liver glyoxalase I and II were 925 and 12 microM, respectively. This is in marked contrast to other glyoxalase II competitive inhibitors, which in general are even more effective against glyoxalase I. The S-(o-, m-, and p-nitrocarbobenzoxy)glutathiones have found utility as affinity ligands for the purification of rat liver glyoxalase II and may well have use in the study of the glyoxalase enzymes in vivo.[1]References
- S-(nitrocarbobenzoxy)glutathiones: potent competitive inhibitors of mammalian glyoxalase II. Bush, P.E., Norton, S.J. J. Med. Chem. (1985) [Pubmed]
Annotations and hyperlinks in this abstract are from individual authors of WikiGenes or automatically generated by the WikiGenes Data Mining Engine. The abstract is from MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.About WikiGenesOpen Access LicencePrivacy PolicyTerms of Useapsburg