# Development of GPER Agonists as Cancer Therapeutics

> **NIH NIH R44** · LINNAEUS THERAPEUTICS, LLC · 2020 · $1,000,000

## Abstract

Project summary:
This project is designed to evaluate a new class of anti-cancer agents for treatment of invasive
melanoma, pancreas, lung, and colon carcinomas. The study compounds are small, synthetic
molecules that have not previously been used in people, and bind to a surface receptor, G protein-
coupled estrogen receptor (GPER) on tumor cells that has not previously been targeted in cancer.
Strong preliminary results indicate that the study compounds potentiate the efficacy of the new immune
checkpoint inhibitors that are now the standard of care for metastatic melanoma. In this proposal, we
will determine the biologically active enantiomer of the GPER agonist G-1, routes of administration that
will have the most favorable pharmacokinetics and maximize the anti-cancer effects, assay clinical
cancer samples for expression of GPER and downstream signaling molecules. Completion of the
proposed work will contribute to the completion of IND-enabling work necessary to translate these
discoveries to first in human trials.

## Key facts

- **NIH application ID:** 9878823
- **Project number:** 5R44CA228695-03
- **Recipient organization:** LINNAEUS THERAPEUTICS, LLC
- **Principal Investigator:** TINA GARYANTES
- **Activity code:** R44 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2020
- **Award amount:** $1,000,000
- **Award type:** 5
- **Project period:** 2018-03-16 → 2022-02-28

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/9878823

## Citation

> US National Institutes of Health, RePORTER application 9878823, Development of GPER Agonists as Cancer Therapeutics (5R44CA228695-03). Retrieved via AI Analytics 2026-05-22 from https://api.ai-analytics.org/grant/nih/9878823. Licensed CC0.

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