Targeted, selective inhibition of trypsin-like enzymes to study and treat disease
Official title: Exploiting new approaches for selective inhibition of trypsin-like serine proteases
Funded at Mayo Clinic Jacksonville · NIH-11364264 · Data updated 2026-11-12
Researchers are developing new, highly selective ways to block specific trypsin-like enzymes to better understand their roles in diseases and potentially guide safer therapies.
Quick facts
| Grant type | R01 grant |
|---|---|
| Study type | NIH-funded research |
| Funding institution | Mayo Clinic Jacksonville NIH-funded |
| Lab location | 1 site (Jacksonville, United States) |
| Project start | January 1, 2022 |
| Project end | June 30, 2030 |
| Funding year | 2026 |
| Award (this year) | $326,840 |
| NIH project number | 2R01GM144393-05 |
| Project ID | NIH-11364264 on NIH RePORTER |
Who could benefit from this research
✓Could help
Ideal candidates are individuals with diseases where mesotrypsin or related trypsin-like proteases drive disease progression, such as certain cancers or inflammatory/coagulation disorders.
✕Less likely to help
Healthy volunteers or patients whose conditions are not driven by these proteases may see no direct benefit.
What this research studies
This project at Mayo Clinic in Jacksonville aims to design and validate allosteric inhibitors that selectively shut down mesotrypsin and related enzymes. By combining computer modeling, high-throughput screening, and X-ray crystallography, the team hopes to uncover cryptic pockets near the active site and stabilize them to block disease-causing activity. The work will connect how enzyme shapes and movements control function, with the goal of creating precise inhibitors that minimize off-target effects. If successful, the findings could inform treatments for pancreatitis, cancer progression, and coagulation disorders. The approach includes structural predictions, kinetic studies, and experimental validation to link conformational changes with regulation of protease activity.
Why it matters
Potential benefit: If successful, patients could benefit from more selective drugs with fewer side effects for conditions linked to these proteases.
How similar studies have gone: Preliminary work showed that a cryptic pocket can be targeted to achieve allosteric inhibition, indicating promise for this strategy.
Where this research is happening
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Mayo Clinic Jacksonville
Jacksonville, United States Active
Researchers
- Principal investigator: Radisky, Evette S — Mayo Clinic Jacksonville
- Study coordinator: Radisky, Evette S
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.