New estrogen-targeting drugs that avoid GPER effects
Molecular Mechanisms and Applications of Novel ER/GPER-selective Ligands
New drugs for women with ER-positive breast cancer that block estrogen signaling at the estrogen receptor while avoiding activation of GPER, which may reduce treatment resistance and uterine side effects.
Quick facts
| Grant type | R01 grant |
|---|---|
| Study type | NIH-funded research |
| Funding institution | University of New Mexico Health Scis Ctr NIH-funded |
| Lab location | 1 site (Albuquerque, United States) |
| Project ID | NIH-11159428 on NIH RePORTER |
What this research studies
Researchers are developing and testing small molecules that selectively bind the estrogen receptor (ER) without turning on a different receptor called GPER, which can contribute to drug resistance and uterine problems. The team uses lab assays, binding and bioassays, and preclinical models to study how these selective compounds work at the molecular level. Prior work from this group discovered GPER-selective compounds and a first ER-selective small molecule, and this project follows those discoveries toward applications. The work is based at an academic center and aims to move promising compounds closer to therapies that could eventually be tested in people.
Who could benefit from this research
Good fit: Women with estrogen receptor–positive (ER+) breast cancer, especially those who have had resistance to current anti-estrogen drugs or who are concerned about uterine side effects, would be the people most likely to benefit from eventual therapies developed here.
Not a fit: People with ER-negative breast cancer or cancers driven by non-hormonal mechanisms are unlikely to benefit from these ER/GPER-selective drugs.
Why it matters
Potential benefit: If successful, this could lead to hormonal therapies for ER-positive breast cancer that cause fewer side effects and are less likely to stop working over time.
How similar studies have performed: Standard hormonal drugs like tamoxifen and aromatase inhibitors are proven treatments, but the approach of making ER-selective compounds that avoid GPER activity is relatively new and builds on recent discoveries by this research group.
Where this research is happening
Albuquerque, United States
- University of New Mexico Health Scis Ctr — Albuquerque, United States (Active)
Researchers
- Principal investigator: Prossnitz, Eric R — University of New Mexico Health Scis Ctr
- Study coordinator: Prossnitz, Eric R
About this research
- This is an active NIH-funded research project — typically early-stage science, not a clinical trial accepting patient enrollment.
- Some NIH-funded labs run parallel clinical studies or seek volunteers for related work. To check, contact the principal investigator or institution listed above.
- For full project details, budget, and progress reports, visit the official NIH RePORTER page below.