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

Shino Manabe, Hikaru Machida, Yoshiyuki Aihara, Masahiro Yasunaga, Yukishige Ito, Yasuhiro Matsumura

Research output: Contribution to journalArticle

9 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)792-796
Number of pages5
JournalMedChemComm
Volume4
Issue number5
DOIs
Publication statusPublished - 2013 May 1
Externally publishedYes

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry

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