Glyoxalase system is a ubiquitous system in human cells which has been examined thoroughly
for its role in different disease conditions. It is composed of Glyoxalase-I (Glo-I) and Glyoxalase-
II which perform an essential metabolic process inside the cell by detoxifying endogenous harmful
metabolites, mainly methylglyoxal (MG) into non-toxic D-lactic acid. Tumor cells are well-known
for their high metabolic rate which results in elevated levels of toxic metabolites. The over-expression
of Glo-I in tumor cells makes this enzyme a pivotal target for anticancer drug development. Glo-I is
metalloenzyme with two polypeptide chains and encompasses two active sites with an integral zinc
atoms at their center. This review aims to highlight the important role of Glo-I in different pathogenic
conditions, and more importantly, it provides a thorough discussion of all known human Glo-I inhibitors
since its discovery, a hundred years ago, up to date. It embraces the different classes they belong
to, their design and chemical structures. We believe this review will help guide the design of novel and
potent human Glo-I inhibitors by providing a handy reference for interested researchers in this target.
Keywords: Human glyoxalase-I, metalloenzyme, pathogenesis, inhibitors, zinc-binding, GSH.
Rights & PermissionsPrintExport