methyl gerfelin

Methyl gerfelin (also known as M-GFN or MeGFN) is a small-molecule inhibitor of glyoxalase I (GLO1) originally identified as the methyl ester of the natural product gerfelin, which is isolated from the fungus *Beauveria felina*. It was initially discovered by researchers at RIKEN to suppress osteoclastogenesis by binding to GLO1, sterol carrier protein 2 (SCP2), and small glutamine-rich tetratricopeptide repeat-containing protein A (SGTA). More recently, researchers at the University of California, San Diego have investigated methyl gerfelin as a novel, fast-acting antidepressant candidate. By inhibiting GLO1, methyl gerfelin prevents the detoxification of methylglyoxal (MG), an endogenous competitive partial agonist of GABAA receptors. The resulting accumulation of MG in the brain enhances GABAA receptor activity, producing rapid antidepressant-like effects in preclinical models of depression and chronic mild stress.

Other names

methyl 4-(2,3-dihydroxy-5-methylphenoxy)-2-hydroxy-6-methylbenzoatemethyl-gerfelin