Tumour lineage-homing cell-penetrating peptides as anticancer molecular delivery systems

Eisaku Kondo, Ken Saito, Yuichi Tashiro, Kaeko Kamide, Shusei Uno, Tomoko Furuya, Masao Mashita, Kiichiro Nakajima, Tomoyuki Tsumuraya, Naoya Kobayashi, Masahiro Nishibori, Mitsune Tanimoto, Masayuki Matsushita

Research output: Contribution to journalArticlepeer-review

129 Citations (Scopus)


Cell-penetrating peptides have gained attention owing to their promise in noninvasive delivery systems. Among the identified cell-penetrating peptides, the TAT peptide has been preferentially used for transduction into cells of diverse origins. However, this activity is nonselective between neoplastic and non-neoplastic cells. Here we describe artificial cell-penetrating peptides that are selectively and efficiently incorporated into human tumour cells, according to their lineage. Ten representative tumour lineage-homing cell-penetrating peptides were obtained by screening of a random peptide library constructed using messenger RNA display technology, and some of the isolates were further modified by amino-acid substitution. Their advantageous tumour cell-targeting ability is corroborated in an in vivo mouse model for imaging and growth suppression of metastatic xenoplant tumours. These cell-penetrating peptides are potentially useful for the efficient targeting of human neoplasms in a tumour origin-dependent manner, and provide a framework for the development of peptide-based anti-tumour technologies.

Original languageEnglish
Article number951
JournalNature communications
Publication statusPublished - 2012

ASJC Scopus subject areas

  • General Chemistry
  • General Biochemistry,Genetics and Molecular Biology
  • General Physics and Astronomy


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