Tumor-targeting peptides from combinatorial libraries

Ruiwu Liu, Xiaocen Li, Wenwu Xiao, Kit S. Lam

Research output: Contribution to journalArticlepeer-review

98 Scopus citations


Cancer is one of the major and leading causes of death worldwide. Two of the greatest challenges in fighting cancer are early detection and effective treatments with no or minimum side effects. Widespread use of targeted therapies and molecular imaging in clinics requires high affinity, tumor-specific agents as effective targeting vehicles to deliver therapeutics and imaging probes to the primary or metastatic tumor sites. Combinatorial libraries such as phage-display and one-bead one-compound (OBOC) peptide libraries are powerful approaches in discovering tumor-targeting peptides. This review gives an overview of different combinatorial library technologies that have been used for the discovery of tumor-targeting peptides. Examples of tumor-targeting peptides identified from each combinatorial library method will be discussed. Published tumor-targeting peptide ligands and their applications will also be summarized by the combinatorial library methods and their corresponding binding receptors.

Original languageEnglish (US)
JournalAdvanced Drug Delivery Reviews
StateAccepted/In press - Mar 19 2016
Externally publishedYes


  • Biological library
  • Cell surface receptor
  • High throughput screening
  • One-bead one-compound peptide library
  • Phage-display peptide library
  • Tumor-targeting peptide

ASJC Scopus subject areas

  • Pharmaceutical Science


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