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Fluorescent Activity-Based Probe To Image and Inhibit Factor XIa Activity in Human Plasma.
Sylwia Modrzycka1, Sonia Kołt1, Ty E Adams2
1Department of Chemical Biology and Bioimaging, Faculty of Chemistry, Wrocław University of Science and Technology, Wybrzeże Wyspiańskiego 27, 50-370 Wrocław, Poland.
Journal of Medicinal Chemistry
|March 10, 2023
Summary
Targeting factor XIa (FXIa) offers a promising approach for anticoagulation with reduced bleeding risk. New chemical tools, including activity-based probes, selectively identify FXIa in plasma, aiding further research into its role in thrombosis.
Area of Science:
- Biochemistry
- Hematology
- Pharmacology
Background:
- Conventional anticoagulants carry bleeding risks alongside antithrombotic benefits.
- Factor XI deficiency (hemophilia C) rarely causes bleeding but is linked to lower rates of ischemic stroke and venous thromboembolism.
- Factor XI (FXI) and its activated form, FXIa, are emerging targets for safer antithrombotic therapies.
Purpose of the Study:
- To develop selective inhibitors of FXIa.
- To create chemical tools for investigating FXIa activity and substrate preferences.
- To validate a novel activity-based probe (ABP) for FXIa detection.
Main Methods:
- Utilized natural and unnatural amino acid libraries to profile FXIa substrate preferences.
- Developed chemical tools: substrates, inhibitors, and activity-based probes (ABPs).
- Tested the selectivity of a novel ABP for FXIa in human plasma.
Main Results:
- Identified FXIa substrate preferences using diverse amino acid libraries.
- Successfully developed various chemical tools, including selective inhibitors and ABPs.
- Demonstrated that the developed ABP selectively labels FXIa in human plasma.
Conclusions:
- FXIa is a viable target for developing anticoagulants with an improved safety profile.
- Novel chemical tools, particularly the FXIa-selective ABP, are valuable for studying FXIa in biological systems.
- This research paves the way for further investigation into FXIa's role in thrombotic disorders and the development of targeted therapies.
