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Updated: Jul 6, 2026

Measuring Caspase Activity Using a Fluorometric Assay or Flow Cytometry
Published on: March 24, 2023
Caspase activity modulators as anticancer agents
Ilya Okun1, Konstantin V Balakin, Sergey E Tkachenko
1ChemDiv, Inc. San Diego, CA 92121, USA. iokun@chemdiv.com
Abstract:
Proteolytic caspase enzymes play a central role in cell apoptosis, or programmed cell death, often as integrating elements of different stimuli leading to the cell death. Since blockade of apoptotic pathways are fundamental for cell survival and proliferation, particularly in cancer cells, the activation of caspases is an attractive target for anticancer therapy. This review describes some of the druggable therapeutic targets thus far identified within the core apoptotic machinery, the corresponding drugs that have been developed, their effects on caspase-dependent apoptotic pathways and their potential impact on the therapy of cancer. With several successful anticancer drugs on the market and numerous compounds in preclinical and clinical developments, modulators of caspase-dependent apoptotic pathways belong to the most important category of anticancer agents.
Insights
Caspase activation is crucial for programmed cell death (apoptosis) and cancer cell survival. Targeting these enzymes offers a promising strategy for developing novel anticancer therapies.
Area of Science:
- Biochemistry
- Molecular Biology
- Oncology
Background:
- Proteolytic caspase enzymes are central to apoptosis, or programmed cell death.
- Inhibition of apoptotic pathways is critical for cancer cell survival and proliferation.
- Caspase activation presents an attractive therapeutic target for anticancer drug development.
Purpose of the Study:
- To review druggable therapeutic targets within the core apoptotic machinery.
- To discuss developed drugs targeting caspases.
- To evaluate the impact of these drugs on caspase-dependent apoptotic pathways and cancer therapy.
Main Methods:
- Literature review of identified druggable targets in apoptosis.
- Analysis of developed drugs targeting caspase pathways.
- Assessment of preclinical and clinical data on caspase modulators.
Main Results:
- Several druggable targets within the apoptotic machinery have been identified.
- Multiple compounds targeting caspase-dependent pathways are in preclinical and clinical development.
- Modulators of caspase-dependent apoptotic pathways are a significant category of anticancer agents.
Conclusions:
- Targeting caspases is a key strategy in anticancer therapy.
- Numerous caspase-modulating drugs show potential for cancer treatment.
- Caspase-dependent apoptotic pathways are vital for developing new cancer therapeutics.
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