Development of a diketopiperazine-forming dipeptidyl Gly-Pro spacer for preparation of an antibody–drug conjugate

Abstract

We developed a novel diketopiperazine-forming dipeptidyl spacer aimed at application in antibody–drug conjugates. Enzymatic cleavage of a peptide linked to the Gly-Pro spacer resulted in formation of diketopiperazine, which was stable and non-toxic, and release of the parent drug.