Synthesis and therapeutic evaluation of an aptide-docetaxel conjugate targeting tumor-associated fibronectin

Hyungjun Kim, Yonghyun Lee, In Hyun Lee, Sunghyun Kim, Daejin Kim, Phei Er Saw, Jinju Lee, Minsuk Choi, Yong Chul Kim, Sangyong Jon

Research output: Contribution to journalArticlepeer-review

40 Scopus citations


Targeted delivery of anticancer drugs to tumors has attracted considerable research interest because of its potential to reduce adverse toxicity while improving therapeutic efficacy. In this study, we synthesized and evaluated the therapeutic efficacy of a conjugate of a high-affinity peptide (aptide) and the anticancer drug docetaxel (DTX). A fibronectin extra domain B (EDB)-specific aptide (APTEDB) was used as a cancer-specific targeting ligand. An APTEDB-DTX conjugate was synthesized from an alkyne-modified aptide and azide-modified DTX via click chemistry. A microscopy study revealed selective binding of dye-labeled APTEDB to EDB-overexpressing cancer cells. The cytotoxicity of the conjugate toward EDB-overexpressing murine lung carcinoma (LLC) and human glioblastoma (U87MG) was similar to that of free DTX. In a pharmacokinetic study, APTEDB-DTX formulated with PEG400/ethanol(5%) exhibited a circulation half-life similar to that of a Tween-80/ethanol formulation of parent DTX. Finally, an evaluation of intravenously injected APTEDB-DTX in mice bearing EDB-positive tumors showed that APTEDB-DTX inhibited the growth of both LLC allograft and U87MG xenograft tumors with an efficacy better than the parent-DTX formulation but with much lower toxicity, as evidenced by reduced body weight loss. Taken together, these results indicate that the aptide-drug conjugate system described here may hold potential as a targeted therapy regimen.

Original languageEnglish
Pages (from-to)118-124
Number of pages7
JournalJournal of Controlled Release
Issue number1
StatePublished - 28 Mar 2014

Bibliographical note

Funding Information:
This work was supported by grants from the Radiation Technology R&D program (no. 2012035409 ) and Global Research Laboratory (no. 2012045436 ) through the National Research Foundation of Korea, funded by the Ministry of Science, ICT & Future Planning.


  • Aptides
  • Conjugates
  • Docetaxel
  • Drug delivery
  • Extra domain B
  • Targeted therapy


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