Pharmacokinetic Analysis of Omomyc Shows Lasting Structural Integrity and Long Terminal Half-Life in Tumor Tissue
Open accessAbstract
MYC is an oncoprotein causally involved in the majority of human cancers and a most wanted target for cancer treatment. Omomyc is the best-characterized MYC dominant negative to date. In the last years, it has been developed into a therapeutic miniprotein for solid tumor treatment and recently reached clinical stage. However, since the in vivo stability of therapeutic proteins, especially within the tumor vicinity, can be affected by proteolytic degradation, the perception of Omomyc as a valid therapeutic agent has been often questioned. In this study, we used a mass spectrometry approach to evaluate the stability of Omomyc in tumor biopsies from murine xenografts following its intravenous administration. Our data strongly support that the integrity of the functional domains of Omomyc (DNA binding and dimerization region) remains preserved in the tumor tissue for at least 72 hours following administration and that the protein shows superior pharmacokinetics in the tumor compartment compared with blood serum.
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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 [418]
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 [418]
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- Authors
- Beaulieu, M.-E., Martínez-Martín, S., Kaur, J., Castillo Cano, V., Massó-Vallés, D., Foradada Felip, L., López-Estévez, S., Serrano del Pozo, E., Thabussot, H., & Soucek, L.
- Affiliations
- Peptomyc S.L., Vall d’Hebron Barcelona Hospital Campus, 08035 Barcelona, Spain
- Vall d'Hebron Hospital Universitari (ES)
- Vall d'Hebron Institute of Oncology (ES)
- Preclinical & Translational Research Program, Vall d’Hebron Institute of Oncology (VHIO), Vall d’Hebron Barcelona Hospital Campus, 08035 Barcelona, Spain
- Institució Catalana de Recerca i Estudis Avançats (ES)
- Corresponding author
- Soucek, Laura
- Venue
- Cancers
- Publisher
- MDPI AG
- Published
- 2023-01-29
- Volume
- 15
- Issue
- 3
- Pages
- 826
- ISSN
- 2072-6694 (ISSN-L)
- PMC
- PMC9913332
- OpenAlex
- W4318486413
- Cited by
- 12
- References
- 21
- Citations by year
- 2025: 3 · 2024: 6 · 2023: 3
- FWCI
- 1.46
- Type
- journal article
- Language
- en
- Open access
- gold
- doi.org
- Licence
- Locations
- Cancers (publishedVersion, cc-by)
- PubMed Central (publishedVersion, cc-by)
- PubMed (publishedVersion)
- Dipòsit Digital de Documents de la UAB (Universitat Autònoma de Barcelona) (submittedVersion, cc-by)
- Funders
- European Union’s Horizon 2020 research and innovation programme (872212, RTC2019-007067-1)
- Ministerio de Ciencia e Innovacion (872212, RTC2019-007067-1)
- Topics
- Health Sciences › Medicine › Oncology › Cancer-related Molecular Pathways
- Health Sciences › Medicine › Radiology, Nuclear Medicine and Imaging › Monoclonal and Polyclonal Antibodies Research
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein purification and stability
- Keywords
- Omomyc, pharmacokinetics, protein stability, tumor tissue, proteolysis, tumor xenografts, mass spectrometry, DNA-binding domain, dimerization domain, intravenous administration
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