A Hybrid Platform Based on a Bispecific Peptide–Antibody Complex for Targeted Cancer Therapy

Byeongjun Yu, Dobeen Hwang, Hyungsu Jeon, Hyungjun Kim, Yonghyun Lee, Hyeongseop Keum, Jinjoo Kim, Dong Yun Lee, Yujin Kim, Junho Chung, Sangyong Jon

Research output: Contribution to journalArticlepeer-review

7 Scopus citations


Peptide-based therapeutics have suffered from a short plasma half-life. On the other hand, antibodies suffer from poor penetration into solid tumors owing to their large size. Herein, we present a new molecular form, namely a hybrid complex between a hapten-labeled bispecific peptide and an anti-hapten antibody (“HyPEP-body”), that may be able to overcome the aforementioned limitation. The bispecific peptide containing a cotinine tag was synthesized by linking a peptide specific to fibronectin extra domain B (EDB) and a peptide able to bind and inhibit vascular endothelial growth factor (VEGF), yielding cot-biPEP EDB-VEGF . Simple mixing of cot-biPEP EDB-VEGF and anti-cotinine antibody (Ab cot ) yielded the hybrid complex, HyPEP EDB-VEGF . HyPEP EDB-VEGF retained the characteristics of the included peptides, and showed improved pharmacokinetic behavior. Moreover, HyPEP EDB-VEGF showed tumor growth inhibition with excellent tumor accumulation and penetration. These findings suggest that the hybrid platform described here offers a solution for most peptide therapeutics that suffer from a short circulation half-life in blood.

Original languageEnglish
Pages (from-to)2005-2010
Number of pages6
JournalAngewandte Chemie - International Edition
Issue number7
StatePublished - 11 Feb 2019

Bibliographical note

Publisher Copyright:
© 2019 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim


  • antibodies
  • aptides
  • cancer therapy
  • fibronectin
  • peptide therapeutics


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