Omomyc Reveals New Mechanisms To Inhibit the MYC Oncogene
Open accessAbstract
The MYC oncogene is upregulated in human cancers by translocation, amplification, and mutation of cellular pathways that regulate Myc. Myc/Max heterodimers bind to E box sequences in the promoter regions of genes and activate transcription. The MYC inhibitor Omomyc can reduce the ability of MYC to bind specific box sequences in promoters of MYC target genes by binding directly to E box sequences as demonstrated by chromatin immunoprecipitation (CHIP). Here, we demonstrate by both a proximity ligation assay (PLA) and double chromatin immunoprecipitation (ReCHIP) that Omomyc preferentially binds to Max, not Myc, to mediate inhibition of MYC-mediated transcription by replacing MYC/MAX heterodimers with Omomyc/MAX heterodimers. The formation of Myc/Max and Omomyc/Max heterodimers occurs cotranslationally; Myc, Max, and Omomyc can interact with ribosomes and Max RNA under conditions in which ribosomes are intact. Taken together, our data suggest that the mechanism of action of Omomyc is to bind DNA as either a homodimer or a heterodimer with Max that is formed cotranslationally, revealing a novel mechanism to inhibit the MYC oncogene. We find that in vivo, Omomyc distributes quickly to kidneys and liver and has a short effective half-life in plasma, which could limit its use in vivo.
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Omomyc is one of the most studied c-Myc/Max inhibitors, derived from the bHLH structural domain of Myc.
“Omomyc is one of the most studied c-Myc/Max inhibitors, derived from the bHLH structural domain of Myc.”
From Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials (2023) · cites this paper as [419]
Omomyc competes with c-Myc for binding to Max, forming Omomyc/Max complexes that prevent the transcriptional activation of Myc target genes involved in proliferation and metabolism.
“It competes with c-Myc for binding to Max, forming Omomyc/Max complexes that prevent the transcriptional activation of Myc target genes involved in proliferation and metabolism.418–420”
From Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials (2023) · cites this paper as [419]
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- Authors
- Demma, M. J., Mapelli, C., Sun, A., Bodea, S., Ruprecht, B., Javaid, S., Wiswell, D., Muise, E., Chen, S., Zelina, J., Orvieto, F., Santoprete, A., Altezza, S., Tucci, F., Escandon, E., Hall, B., Ray, K., Walji, A., & O’Neil, J.
- Affiliations
- Merck & Co., Inc., Rahway, NJ, USA (United States) (US)
- IRBM (IT)
- Assay Development, Merck & Co., Inc.
- Corresponding author
- Demma, Mark J.
- ORCID
- Venue
- Molecular and Cellular Biology
- Publisher
- Informa UK Limited
- Published
- 2019-11-01
- Volume
- 39
- Issue
- 22
- ISSN
- 0270-7306 (ISSN-L)
- 1098-5549
- PMC
- PMC6817756
- OpenAlex
- W2972460236
- Cited by
- 92
- References
- 52
- Citations by year
- 2026: 6 · 2025: 22 · 2024: 18 · 2023: 13 · 2022: 5 · 2021: 14 · 2020: 12 · 2019: 1
- FWCI
- 3.34
- Type
- journal article
- Language
- en
- Open access
- hybrid
- doi.org
- Licence
- Locations
- Molecular and Cellular Biology (publishedVersion, cc-by)
- Europe PMC (PubMed Central) (publishedVersion, cc-by)
- PubMed Central (publishedVersion, cc-by)
- PubMed (publishedVersion)
- Funders
- Deakin University
- Topics
- Health Sciences › Medicine › Oncology › Cancer-related Molecular Pathways
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Genomics and Chromatin Dynamics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Chromatin Remodeling and Cancer
- Keywords
- Omomyc, Myc-Max heterodimer, Max, E-box binding, transcriptional repression, MYC target genes, pharmacokinetics, anticancer drug mechanism
- MeSH terms
- Amino Acid Sequence, Animals, Cell Line, DNA, DNA-Binding Proteins, Female, Humans, Mice, Inbred BALB C, Peptide Fragments, Promoter Regions, Genetic, Protein Binding, Recombinant Proteins, Transcription, Genetic, Transcriptional Activation, Genes, myc, Proto-Oncogene Proteins c-myc, HCT116 Cells, Cell Line, Tumor, Chromatin Immunoprecipitation, Mice, Basic Helix-Loop-Helix Leucine Zipper Transcription Factors
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