A strategy for combating melanoma with oncogenic c-Myc inhibitors and targeted nanotherapy

Dipanjan Pan, Benjamin Kim, Grace Hu, Deepti Sood Gupta, Angana Senpan, Xiaoxia Yang, Anne Schmieder, Corban Swain, Samuel A. Wickline, Michael H. Tomasson, Gregory M. Lanza

Research output: Contribution to journalArticlepeer-review

Abstract

Aims: The activity of the transcription factor c-Myc is dependent upon heterodimerization with Max to control target gene transcription. Small-molecule inhibitors of c-Myc-Max have exhibited low potency and poor water solubility and are therefore unsuitable for in vivo application. We hypothesized that a nanomedicine approach incorporating a cryptic c-Myc inhibitor prodrug could be delivered and enzymatically released in order to effectively inhibit melanoma. Materials & methods: An Sn-2 lipase-labile Myc inhibitor prodrug was synthesized and included in two αvβ3-targeted nanoparticle platforms (20 and 200 nm). The inherent antiproliferate potency was compared with the lipid-free compound using human and mouse melanoma cell lines. Results & conclusion: These data demonstrate for the first time a successful nanodelivery of c-Myc inhibitors and their potential use to prevent melanoma.

Original languageEnglish (US)
Pages (from-to)241-251
Number of pages11
JournalNanomedicine
Volume10
Issue number2
DOIs
StatePublished - Jan 1 2015

Keywords

  • c-Myc inhibitor
  • melanoma
  • nanotherapy
  • prodrug

ASJC Scopus subject areas

  • Bioengineering
  • Medicine (miscellaneous)
  • Biomedical Engineering
  • Materials Science(all)

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