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

doi:10.1039/c3md00075c

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

PHA - Graduate School of Pharmaceutical Sciences (department affiliation only)

Research output: Contribution to journal › Article › peer-review

16 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 language	English
Pages (from-to)	792-796
Number of pages	5
Journal	MedChemComm
Volume	4
Issue number	5
DOIs	https://doi.org/10.1039/c3md00075c
Publication status	Published - 2013 May

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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.",

author = "Shino Manabe and Hikaru Machida and Yoshiyuki Aihara and Masahiro Yasunaga and Yukishige Ito and Yasuhiro Matsumura",

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AU - Manabe, Shino

AU - Machida, Hikaru

AU - Aihara, Yoshiyuki

AU - Yasunaga, Masahiro

AU - Ito, Yukishige

AU - Matsumura, Yasuhiro

PY - 2013/5

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AB - 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.

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

Abstract

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