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

doi:10.2217/nnm.14.101

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

Journal article

Peer reviewed

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, …

Nanomedicine (London, England), Vol.10(2), pp.241-251

01/2015

DOI: 10.2217/nnm.14.101

PMCID: PMC4665613

PMID: 25600969

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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. Keywords: c-Myc inhibitor; melanoma; nanotherapy; prodrug.

prodrug

melanoma

c-Myc inhibitor

nanotherapy

Details

Title: Subtitle: A strategy for combating melanoma with oncogenic c-Myc inhibitors and targeted nanotherapy
Creators: Dipanjan Pan - Department of Medicine, Washington University School of Medicine, 4320 Forest Park Avenue, Saint Louis, MO 63108, USA
Benjamin Kim - Department of Medicine, Washington University School of Medicine, 4320 Forest Park Avenue, Saint Louis, MO 63108, USA
Grace Hu - Department of Medicine, Washington University School of Medicine, 4320 Forest Park Avenue, Saint Louis, MO 63108, USA
Deepti Sood Gupta - Department of Medicine, Washington University School of Medicine, 4320 Forest Park Avenue, Saint Louis, MO 63108, USA
Angana Senpan - Department of Medicine, Washington University School of Medicine, 4320 Forest Park Avenue, Saint Louis, MO 63108, USA
Xiaoxia Yang - Department of Medicine, Washington University School of Medicine, 4320 Forest Park Avenue, Saint Louis, MO 63108, USA
Anne Schmieder - Department of Medicine, Washington University School of Medicine, 4320 Forest Park Avenue, Saint Louis, MO 63108, USA
Corban Swain - Department of Medicine, Washington University School of Medicine, 4320 Forest Park Avenue, Saint Louis, MO 63108, USA
Samuel A Wickline - Department of Medicine, Washington University School of Medicine, 4320 Forest Park Avenue, Saint Louis, MO 63108, USA
Michael H Tomasson - Department of Medicine, Washington University School of Medicine, 4320 Forest Park Avenue, Saint Louis, MO 63108, USA
Gregory M Lanza - Department of Medicine, Washington University School of Medicine, 4320 Forest Park Avenue, Saint Louis, MO 63108, USA
Resource Type: Journal article
Publication Details: Nanomedicine (London, England), Vol.10(2), pp.241-251
DOI: 10.2217/nnm.14.101
PMID: 25600969
PMCID: PMC4665613
NLM abbreviation: Nanomedicine (Lond)
ISSN: 1743-5889
eISSN: 1748-6963
Language: English
Date published: 01/2015
Academic Unit: Hematology, Oncology, and Blood & Marrow Transplantation; Internal Medicine
Record Identifier: 9984094565402771

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