Selection and identification of a novel bone-targeting peptide for biomedical imaging of bone

Jinho Bang, Heesun Park, Jihye Yoo, Donghyun Lee, Won Il Choi, Jin Hyung Lee, Young Ran Lee, Chungho Kim, Heebeom Koo, Sunghyun Kim

Research output: Contribution to journalArticlepeer-review

7 Citations (Scopus)


The global burden of bone-related diseases is increasing in the aging society; thus, improved bone targeted imaging for their early identification and treatment are needed. In this study, we screened novel peptide ligands for hydroxyapatite, a major inorganic component of teeth and bones, and identified a peptide enabling in vivo bone targeting and real-time fluorescence bone detection. To isolate peptides highly specific for hydroxyapatite, we used negative and positive selection from a randomized 8-mer peptide phage library and identified hydroxyapatite-specific peptides (HA-pep2, HA-pep3, and HA-pep7). Among these three peptides, HA-pep3 showed the highest binding capacity and superior dissociation constant towards hydroxyapatite surfaces over time (~ 88.3% retained on hydroxyapatite after two weeks). Furthermore, HA-pep3 was highly specific for hydroxyapatite compared to other calcium salt-based materials. Using this superior specificity, HA-pep3 showed higher accumulation in skull, spine, and joints in comparison with scrambled control peptide during real-time whole-body imaging. Ex vivo analysis of the major organs and bone from mice demonstrated that the fluorescence intensity in bone was about 3.32 folds higher in the case of HA-pep3 than the one exhibited by the scrambled control peptide. Our study identified a novel approach for targeting ligands for bone specific imaging and can be useful for drug delivery applications.

Original languageEnglish
Article number10576
JournalScientific reports
Issue number1
Publication statusPublished - 2020 Dec 1

Bibliographical note

Funding Information:
This work was supported by grants from the Fundamental R&D program funded by the Korea Institute of Ceramic Engineering and Technology (KICET) and from the Basic Research Program (2016R1C1B3013951) through the National Research Foundation of Korea (NRF) funded by the Korean Government (Ministry of Science, ICT, & Future Planning).

Publisher Copyright:
© 2020, The Author(s).

ASJC Scopus subject areas

  • General


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