In vivo imaging of tumor apoptosis using histone H1-targeting peptide

Kai Wang, Sangeetha Purushotham, Ji Young Lee, Moon Hee Na, Hyekyung Park, Sun Jeong Oh, Rang Woon Park, Jae Yong Park, Eungbae Lee, Byung Chae Cho, Mi Na Song, Moon Chang Baek, Wonjung Kwak, Jeongsoo Yoo, Allan S. Hoffman, Yu Kyoung Oh, In San Kim, Byung Heon Lee

Research output: Contribution to journalArticlepeer-review

72 Citations (Scopus)


In vivo imaging of apoptosis could allow monitoring of tumor response to cancer treatments such as chemotherapy. Using phage display, we identified the CQRPPR peptide, named ApoPep-1(Apoptosis-targeting Peptide-1), that was able to home to apoptotic and necrotic cells in tumor tissue. ApoPep-1 also bound to apoptotic and necrotic cells in culture, while only little binding to live cells was observed. Its binding to apoptotic cells was not dependent on calcium ion and not competed by annexin V. The receptor for ApoPep-1 was identified to be histone H1 that was exposed on the surface of apoptotic cells. In necrotic cells, ApoPep-1 entered the cells and bound to histone H1 in the nucleus. The imaging signals produced during monitoring of tumor apoptosis in response to chemotherapy was enhanced by the homing of a fluorescent dye- or radioisotope-labeled ApoPep-1 to tumor treated with anti-cancer drugs, whereas its uptake of the liver and lung was minimal. These results suggest that ApoPep-1 holds great promise as a probe for in vivo imaging of apoptosis, while histone H1 is a unique molecular signature for this purpose.

Original languageEnglish
Pages (from-to)283-291
Number of pages9
JournalJournal of Controlled Release
Issue number3
Publication statusPublished - 2010 Dec 20
Externally publishedYes

Bibliographical note

Funding Information:
This work was supported by the grant from the Regional Technology Innovation Program of the Ministry of Knowledge Economy ( RTI04-01-01 ), the grant from the National R&D Program for Cancer Control, Ministry for Health, Welfare and Family Affairs ( 0720550-2 ), and WCU Program through the National Research Foundation of Korea funded by the Ministry of Education, Science and Technology ( R33-10054 ).


  • Apoptosis
  • Histone H1
  • In vivo imaging
  • Phage display
  • Targeting peptide

ASJC Scopus subject areas

  • Pharmaceutical Science


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