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Exploring Caspase Mutations and Post-Translational Modification by Molecular Modeling Approaches
Published on: October 13, 2022
The potential for caspases in drug discovery
Sarah H MacKenzie1, Joshua L Schipper, A Clay Clark
1North Carolina State University, Department of Molecular and Structural Biochemistry, 128 Polk Hall, Raleigh, NC 27695, USA.
Current Opinion in Drug Discovery & Development
|September 3, 2010
Summary
Caspase inhibitors and activators offer therapeutic potential for diseases linked to apoptosis and inflammation. Research focuses on designing effective caspase inhibitors and novel procaspase-3 activators for treatment.
Area of Science:
- Biochemistry
- Molecular Biology
- Pharmacology
Background:
- Caspases are proteases crucial for apoptosis and inflammation.
- Dysregulation of these processes underlies numerous diseases.
- Targeting caspases is a key therapeutic strategy.
Purpose of the Study:
- To review progress in designing specific and pan-caspase inhibitors.
- To highlight the development of procaspase-3 activators.
- To discuss therapeutic strategies for caspase-related diseases.
Main Methods:
- Review of rational drug design principles for caspase modulators.
- Analysis of peptide and peptidomimetic inhibitor development.
- Examination of procaspase-3 activator design strategies.
Main Results:
- Limited success of current caspase inhibitors in clinical trials due to poor drug-like properties.
- Growing interest in activating procaspases as a therapeutic approach.
- Advancements in designing both inhibitors and activators.
Conclusions:
- Caspase modulation remains a promising therapeutic avenue.
- Overcoming pharmacological constraints is essential for inhibitor development.
- Procaspase-3 activation presents a novel therapeutic strategy for diseases with reduced apoptosis.
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