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A Bioluminescent and Fluorescent Orthotopic Syngeneic Murine Model of Androgen-dependent and Castration-resistant Prostate Cancer
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Prostate cancer cells' growth is decreased by novel MYC inhibitors

Bita Nickkholgh1,2, Joseph McGrath3, Sivanandane Sittadjody1

  • 1Wake Forest Institute for Regenerative Medicine (WFIRM), Wake Forest University School of Medicine, Winston-Salem, NC, 27101, USA.

Investigational New Drugs
|April 28, 2026
PubMed

Insights

New MYC/MAX inhibitors, including proteomimetics, show promise in suppressing prostate cancer cell growth. Second-generation and proteomimetic MYC inhibitors are more effective than first-generation ones in 3D models.

Area of Science:

  • Oncology
  • Molecular Biology
  • Biochemistry

Background:

  • MYC is a proto-oncogene frequently dysregulated in cancers.
  • Directly targeting MYC is challenging due to its disordered structure.
  • Targeting the MYC/MAX protein-protein interaction offers an indirect therapeutic strategy.

Purpose of the Study:

  • To compare the efficacy of first- and second-generation MYC/MAX inhibitors (10,058-F4 and 3jc48-3) and a novel proteomimetic inhibitor (JKY-2-169).
  • To evaluate inhibitor efficacy in 2D cell culture and advanced 3D models, including patient-derived spheroids.
  • To identify cellular pathways affected by MYC/MAX inhibition.

Main Methods:

  • Inhibition of human prostate cancer cell line DU145 growth in 2D culture.
  • Validation of inhibitor efficacy in 3D microcapsules and patient-derived prostate cancer spheroids.
  • Comparative proteomic analysis of treated and untreated DU145 cells to identify altered cellular pathways.

Main Results:

  • Second-generation (3jc48-3) and proteomimetic (JKY-2-169) MYC/MAX inhibitors reduced cell viability in 3D models.
  • Inhibitor-treated patient-derived spheroids showed no significant growth, unlike the control group.
  • Proteomimetic and second-generation inhibitors suppressed cell growth at lower concentrations than first-generation inhibitors.
  • Proteomic analysis revealed MYC/MAX inhibition impacts pathways involved in cytoskeletal organization, cell cycle, metabolism, and RNA functions.

Conclusions:

  • Second-generation and proteomimetic MYC/MAX inhibitors demonstrate superior efficacy compared to first-generation inhibitors.
  • These novel inhibitors show potential for suppressing prostate cancer cell growth in 3D environments.
  • Further investigation and development of these MYC inhibitors are warranted for cancer therapy.
Keywords:
3D cultureDU145MAXMYCProstate cancerProtein–protein interactionProteomicsProteomimeticSpheroids

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