Journal
NANOMEDICINE
Volume 10, Issue 2, Pages 241-251Publisher
FUTURE MEDICINE LTD
DOI: 10.2217/NNM.14.101
Keywords
c-Myc inhibitor; melanoma; nanotherapy; prodrug
Funding
- American Heart Association (AHA) [0835426N, 11IRG5690011]
- NIH [NS059302, CA119342, CA1547371, NS073457, HL073646]
- National Cancer Institute (NCI) [N01CO37007]
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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 alpha(v)beta(3)-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.
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