Improving drugs that target the Y537S estrogen receptor in breast cancer
Structural-Transcriptional Relationships that Improve Y537S Estrogen Receptor Antagonism
Looks at how different anti-hormone drugs change the Y537S estrogen receptor mutation in ER-positive breast cancer to help find better treatments.
Quick facts
| Grant type | R37 grant |
|---|---|
| Study type | NIH-funded research |
| Funding institution | Loyola University Chicago NIH-funded |
| Lab location | 1 site (Maywood, United States) |
| Project ID | NIH-11302676 on NIH RePORTER |
What this research studies
Researchers will use laboratory models of hormone-resistant ER-positive breast cancer that carry the Y537S ESR1 mutation to see how different anti-estrogen drugs bind and change the receptor's shape. They will determine high-resolution receptor structures (for example by X-ray crystallography) and measure how those drug-induced changes alter gene activity programs in cancer cells. By linking specific structural changes to the drugs' anti-tumor effects in cells, they aim to identify molecular features that restore control of the mutant receptor. Findings are intended to guide which drug designs or existing therapies might work better against this common resistance mechanism.
Who could benefit from this research
Good fit: People with ER-positive breast cancer whose tumors carry the ESR1 Y537S mutation or who have developed resistance to standard hormone therapies are the most relevant population.
Not a fit: Patients with ER-negative breast cancer or without ESR1 mutations are unlikely to benefit directly from this work.
Why it matters
Potential benefit: Could point to drugs or drug features that work better against hormone-resistant ER-positive breast cancers with the Y537S mutation.
How similar studies have performed: Some next-generation SERDs and lab studies have shown promise against ESR1 mutations, but response to Y537S has been variable and translating structural insights into consistently effective therapies is still an active area of research.
Where this research is happening
Maywood, United States
- Loyola University Chicago — Maywood, United States (Active)
Researchers
- Principal investigator: Fanning, Sean William — Loyola University Chicago
- Study coordinator: Fanning, Sean William
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.