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Updated: Mar 30, 2026
Exploring Caspase Mutations and Post-Translational Modification by Molecular Modeling Approaches
Published on: October 13, 2022
Small Molecule Active Site Directed Tools for Studying Human Caspases
Marcin Poreba1, Aleksandra Szalek1, Paulina Kasperkiewicz1
1Department of Bioorganic Chemistry, Faculty of Chemistry, Wroclaw University of Technology , Wyb. Wyspianskiego 27, 50-370 Wroclaw, Poland.
Abstract:
Caspases are proteases of clan CD and were described for the first time more than two decades ago. They play critical roles in the control of regulated cell death pathways including apoptosis and inflammation. Due to their involvement in the development of various diseases like cancer, neurodegenerative diseases, or autoimmune disorders, caspases have been intensively investigated as potential drug targets, both in academic and industrial laboratories. This review presents a thorough, deep, and systematic assessment of all technologies developed over the years for the investigation of caspase activity and specificity using substrates and inhibitors, as well as activity based probes, which in recent years have attracted considerable interest due to their usefulness in the investigation of biological functions of this family of enzymes.
Insights
Caspases are key regulators of cell death and inflammation. This review assesses technologies for studying caspase activity, including substrates, inhibitors, and activity-based probes, crucial for understanding diseases and developing drugs.
Area of Science:
- Biochemistry
- Molecular Biology
- Enzymology
Background:
- Caspases are proteases involved in apoptosis and inflammation.
- Dysregulation of caspases is linked to cancer, neurodegenerative, and autoimmune diseases.
- Caspases are significant drug targets in academic and industrial research.
Purpose of the Study:
- To systematically review technologies for investigating caspase activity and specificity.
- To highlight the utility of substrates, inhibitors, and activity-based probes.
- To provide a comprehensive assessment of tools for caspase research.
Main Methods:
- Literature review of technologies for caspase activity assessment.
- Analysis of substrates, inhibitors, and activity-based probes.
- Evaluation of methods for studying caspase specificity and biological functions.
Main Results:
- Various technologies exist for studying caspases, including traditional substrates and inhibitors.
- Activity-based probes have emerged as powerful tools for investigating caspase functions.
- These methods are essential for understanding disease mechanisms and drug development.
Conclusions:
- A comprehensive understanding of caspase activity is vital for disease research.
- Activity-based probes offer unique advantages for studying caspase biology.
- Continued technological development is crucial for advancing caspase-targeted therapies.
