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Disruption of the MYC transcriptional function by a small-molecule antagonist of MYC/MAX dimerization

Lookup NU author(s): Dr Xiaohong Lu, Professor John LunecORCiD

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Abstract

Inhibition of MYC/MAX dimerization by a small-molecule antagonist (IIA6B17) has been shown to interfere with MYC-induced transformation of chick embryo fibroblasts, suggesting that the functional inhibitors of the MYC family of oncoproteins have potential as therapeutic agents. In the present study, a functional MYC reporter gene assay has been developed, using a luciferase gene construct under the control of the ornithine decarboxylase (ODC) gene promoter. This luciferase gene construct has been stably transfected into the MYCN amplified neuroblastoma cell line (NGP) and MYCC-overexpressed neuroepithelioma cell line (NB100). After exposure of the cell lines to IIA6B17 for 24 h, a significant reduction of luciferase activity was only observed in the NB100 cells, with IC50 values of ∼28±9 μM, indicating that IIA6B17 has cell line-specific activity which may be selective for individual members of the MYC family.

Publication metadata

Author(s): Lu X, Vogt P, Boger D, Lunec J

Publication type: Article

Publication status: Published

Journal: Oncology Reports

Year: 2008

Volume: 19

Issue: 3

Pages: 825-830

ISSN (print): 1021-335X

ISSN (electronic): 1791-2431

Publisher: Spandidos Publications

URL: http://dx.doi.org/10.1007/978-3-540-77385-6

DOI: 10.1007/978-3-540-77385-6

PubMed id: 18288422

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