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

21 Scopus citations


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
Pages (from-to)241-251
Number of pages11
Issue number2
StatePublished - Jan 1 2015


  • c-Myc inhibitor
  • melanoma
  • nanotherapy
  • prodrug


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