# Peptoid conjugates as inhibitors of androgen receptor dimerization and function in enzalutamide-resistant prostate cancer

> **NIH NIH R21** · NEW YORK UNIVERSITY SCHOOL OF MEDICINE · 2020 · $180,449

## Abstract

Project Summary
 We are pursuing creative efforts to develop therapies urgently needed to treat prostate cancers that
become resistant to new anti-androgen therapies. Our approach combines innovations in chemical synthesis
with expertise in androgen receptor signaling and prostate cancer. This will allow us to discover a new family of
therapeutic agents that combat castration resistant prostate cancer (CRPC) through a unique mode of action
that blocks androgen receptor (AR) activity.
 Indeed, we have developed a new strategy to inhibit the activity of AR by disrupting AR dimerization by
displaying AR ligands upon a molecular scaffold. AR dimerization has only been recently recognized as key to
determinant to AR activity, and we have developed a novel and facile cell free AR dimerization assay to rapidly
test the for effects of the peptoid conjugates on disrupting AR dimerization. We have pioneered an effective
method for generating “peptoid” oligomers that incorporate ligands precisely located along the molecular
backbone. Our concept is that the conjugates with high affinity ligands for AR will facilitate receptor binding and
block AR dimerization more potently and at lower concentrations than low affinity ligands for AR. This has the
potential to be exploited to promote an anti-tumor response by targeting AR in a different way than current AR-
directed therapies, making this therapeutic strategy conceptually novel and highly innovative.
!

## Key facts

- **NIH application ID:** 9964725
- **Project number:** 5R21CA234291-02
- **Recipient organization:** NEW YORK UNIVERSITY SCHOOL OF MEDICINE
- **Principal Investigator:** Michael J. Garabedian
- **Activity code:** R21 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2020
- **Award amount:** $180,449
- **Award type:** 5
- **Project period:** 2019-08-01 → 2022-07-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/9964725

## Citation

> US National Institutes of Health, RePORTER application 9964725, Peptoid conjugates as inhibitors of androgen receptor dimerization and function in enzalutamide-resistant prostate cancer (5R21CA234291-02). Retrieved via AI Analytics 2026-05-26 from https://api.ai-analytics.org/grant/nih/9964725. Licensed CC0.

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