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Glutathione is a tripeptide made of three amino acids: cysteine, glycine, and glutamate

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Mechanistically, APR-246 is spontaneously converted into the active species methylene quinuclidinone (MQ), which is able to covalently bind to cysteine residues in mutant p53 thereby producing thermo dynamic stabilization of the protein and shifting equilibrium toward a functional conformation.1413 APR-246 monotherapy was originally investigated in a phase I trial including AML patients with clinical activity and correlative data identifying activation of p53-dependent pathways.1615 Maslah et al

FederAParidesMKMurroughJWPerezAMMorganJESaxenaSet al