C115H MGL-Dz

C115H MGL-Dz is a targeted enzyme-prodrug therapy (TEPT) agent consisting of a mutant recombinant methionine γ-lyase (MGL) enzyme, specifically the C115H variant, conjugated with the isoflavone daidzein (Dz). In this system, daidzein serves as a targeting ligand that directs the enzyme to estrogen receptor (ER)-positive cancer cells. The C115H mutation in the MGL enzyme alters its catalytic specificity, allowing it to efficiently perform a β-elimination reaction on S-alkyl-L-cysteine sulfoxides, such as S-propyl-L-cysteine sulfoxide (propiin). When administered alongside the conjugate, propiin is converted in situ at the tumor site into highly reactive and cytotoxic thiosulfinates (e.g., dipropyl thiosulfinate). These thiosulfinates induce oxidative stress and apoptosis in the targeted tumor cells. Preclinical studies have demonstrated significant tumor growth inhibition in xenograft models of pancreatic, colorectal, prostate, and breast cancers.

Other names

C115H methionine γ-lyase-daidzein conjugatedaidzein-conjugated C115H methionine gamma-lyase