The glyoxalase enzymes have been the focus of pharmaceutical development for inhibitors in metabolic and psychiatric disorders for many years.38,39 One such small-molecule enzyme inhibitor, DiFMOC-G, has been identified as the most potent competitive inhibitor of GLO2,40 which could be slowly hydrolyzed by GLO2 in vivo and demonstrates excellent pharmacokinetics and safety. The gene discussed is HAGH; the disease is psychiatric disorder.