Don't Lose Your (War)head: Structure-Activity Relationships of Covalent Warheads as Substrates for GST-Catalyzed Glutathione Conjugation.

Key Points

• The study aims to understand how covalent warheads function as substrates for GST and their role in GSH conjugation.
• Characterization of various covalent warheads as substrates for GST activity.
• Analysis of their compound half-lives in human liver cytosol.
• Found strong correlation between compound half-lives and GST susceptibility.
• Established that GST susceptibility is a tunable factor influencing metabolic GSH conjugation.