450366-22-0Relevant academic research and scientific papers
Development of a diketopiperazine-forming dipeptidyl Gly-Pro spacer for preparation of an antibody-drug conjugate
Manabe, Shino,Machida, Hikaru,Aihara, Yoshiyuki,Yasunaga, Masahiro,Ito, Yukishige,Matsumura, Yasuhiro
, p. 792 - 796 (2013)
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. The Royal Society of Chemistry 2013.
Synthesis of an immunoconjugate of camptothecin
Walker, Michael A.,Dubowchik, Gene M.,Hofstead, Sandra J.,Trail, Pamela A.,Firestone, Raymond A.
, p. 217 - 219 (2007/10/03)
The first immunoconjugate of camptothecin has been synthesized wherein the drug is attached to the tumor-recognizing antibody BR96 via a Cathepsin B cleavable linker. Endocytosis of the immunoconjugate upon binding to the tumor cell followed by enzymatic cleavage of the linker inside the endosome ensures tumor-specific release of the drug. In this way, it is hoped that the dose-limiting side effects associated with camptothecin can be eliminated while the antitumor activity is preserved.
