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Updated: Feb 11, 2026

Identification of Growth Inhibition Phenotypes Induced by Expression of Bacterial Type III Effectors in Yeast
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Identification of a Small Molecule That Selectively Inhibits ERG-Positive Cancer Cell Growth

Ahmed A Mohamed1, Charles P Xavier1, Gauthaman Sukumar2

  • 1Center for Prostate Disease Research, Department of Surgery, Uniformed Services University of the Health Sciences and the Walter Reed National Military Medical Center, Bethesda, Maryland.

Cancer Research
|May 2, 2018
PubMed

Insights

Researchers identified ERGi-USU, a novel small molecule that selectively inhibits the ETS-related gene (ERG) protein. This compound shows promise for treating ERG-positive prostate cancer and other malignancies with minimal toxicity.

Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Discovery

Background:

  • The ETS-related gene (ERG) is frequently activated by gene fusions in early prostate cancer.
  • Targeting ERG represents a validated therapeutic strategy for ERG-positive malignancies.

Purpose of the Study:

  • To identify and characterize novel small-molecule inhibitors of ERG protein.
  • To evaluate the therapeutic potential of ERGi-USU in ERG-driven cancers.

Main Methods:

  • Screening of small-molecule libraries using In-Cell Western Assay.
  • Characterization of ERGi-USU in cancer cell lines and xenograft models.
  • Kinase screening to identify direct targets of ERGi-USU.

Main Results:

  • ERGi-USU selectively inhibited the growth of ERG-positive cancer cells.
  • ERGi-USU demonstrated additive effects when combined with enzalutamide.
  • ERGi-USU directly targets RIOK2, inducing ribosomal stress and inhibiting tumor xenograft growth without apparent toxicity.

Conclusions:

  • ERGi-USU is a potent and selective inhibitor of ERG.
  • ERGi-USU shows significant potential for the development of novel ERG-targeted therapies for prostate cancer and other cancers.

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