# Targeting the ETV/PEA3 transcriptional circuitry with selective small molecule probes

> **NIH NIH R01** · UNIVERSITY OF MICHIGAN AT ANN ARBOR · 2020 · $339,052

## Abstract

Project Summary
The transition of localized breast cancer to metastatic disease is a major contributor to increased disability and
death associated with advanced disease. Treatment options are limited once metastatic status has been reached;
although metastases originate from the primary tumor, fundamental shifts in cell phenotype occur during the
stages of dissemination, formation of micro-metastases, and the growth of metastases themselves. The origin
and influence of these differences remains poorly understood. There is thus a great need for small molecule tools
that modulate uniquely activated metastatic pathways in order to identify specific and effective therapeutic
options. Through this work we will both provide small molecule tools targeted to a cellular invasion pathways
that are uniquely activated in metastasis and test if pharmacological inhibition of these pathways can block
metastatic phenotypes in breast cancer. This will be accomplished through targeting a dysregulated
transcription factor complex formed between the ETV/PEA3 transcriptional activators (ETV1, ETV4, and ETV5)
and the coactivator Med25 with natural product-based modulators. Taken together, these studies will define
new pathways for therapeutic targeting of advanced cancer and the natural product modulators will serve as
starting points for the long-term development of novel therapies.

## Key facts

- **NIH application ID:** 9956984
- **Project number:** 5R01CA140667-10
- **Recipient organization:** UNIVERSITY OF MICHIGAN AT ANN ARBOR
- **Principal Investigator:** ANNA K. MAPP
- **Activity code:** R01 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2020
- **Award amount:** $339,052
- **Award type:** 5
- **Project period:** 2009-05-20 → 2022-06-30

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/9956984

## Citation

> US National Institutes of Health, RePORTER application 9956984, Targeting the ETV/PEA3 transcriptional circuitry with selective small molecule probes (5R01CA140667-10). Retrieved via AI Analytics 2026-05-23 from https://api.ai-analytics.org/grant/nih/9956984. Licensed CC0.

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