Targeting prostate cancer cells with PSMA inhibitor-guided gold nanoparticles

Benjamin B. Kasten, Tiancheng Liu, Jessie R. Nedrow-Byers, Paul D. Benny, Clifford E. Berkman

Research output: Contribution to journalArticlepeer-review


Prostate-specific membrane antigen (PSMA) is a notable biomarker for diagnostic and therapeutic applications in prostate cancer. Gold nanoparticles (AuNPs) provide an attractive nanomaterial platform for combining a variety of targeting, imaging, and cytotoxic agents into a unified device for biomedical research. In this study, we present the generation and evaluation of the first AuNP system functionalized with a small molecule phosphoramidate peptidomimetic inhibitor for the targeted delivery to PSMA-expressing prostate cancer cells. The general approach involved the conjugation of streptavidin-coated AuNPs with a biotin-linked PSMA inhibitor (CTT54) to generate PSMA-targeted AuNPs. In vitro evaluations of these targeted AuNPs were conducted to determine PSMA-mediated and time-dependent binding to PSMA-positive LNCaP cells. The PSMA-targeted AuNPs exhibited significantly higher and selective binding to LNCaP cells compared to control non-targeted AuNPs, thus demonstrating the feasibility of this approach.

Original languageEnglish (US)
Pages (from-to)565-568
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Issue number2
StatePublished - Jan 15 2013
Externally publishedYes


  • Biotin
  • Gold nanoparticles
  • Prostate cancer
  • Prostate-specific membrane antigen
  • Streptavidin

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry


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