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Characterizing Modulators of Protease-Activated Receptors with a Calcium Mobilization Assay Using a Plate Reader
Published on: May 24, 2024
Serpins (serine protease inhibitors).
Susannah J Bauman1, Herbert C Whinna1, Frank C Church1
1The University of North Carolina at Chapel Hill, Chapel Hill, North Carolina.
Current Protocols in Protein Science
|April 23, 2008
Summary
Serine protease inhibitors (serpins) regulate protease activity in human injury responses. Defective serpins cause pathologies, highlighting their critical roles in health and disease.
Area of Science:
- Biochemistry
- Molecular Biology
- Proteomics
Background:
- Serpins are crucial regulators of serine and other proteases.
- In humans, serpins are vital for processes like coagulation, inflammation, and tissue repair.
- Loss-of-function mutations in serpin genes lead to various pathologies.
Purpose of the Study:
- To describe serine protease inhibitors (serpins) and their regulatory functions.
- To present protocols for quantifying antithrombin's inhibition of thrombin.
- To provide a list of other serpins and their purification techniques.
Main Methods:
- Description of serpin protein family and their biological roles.
- Protocols for determining the second-order rate constant of antithrombin (AT) inhibition of thrombin.
- Methods for purification of various serpins.
Main Results:
- Antithrombin III (AT) is presented as a key example of a serpin.
- Protocols for measuring AT's inhibition kinetics with thrombin, with and without heparin, are detailed.
- A partial catalog of other serpins and their purification strategies is included.
Conclusions:
- Serpins are essential for regulating protease activity in physiological processes.
- Deficiencies in serpins contribute to disease pathogenesis.
- The study provides practical methods for studying serpin function and purification.
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