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Caspases

Caspases

Caspase, a family of cysteine proteases, serve as effectors in apoptosis. The ced3 gene in C.elegans was first identified to be involved in apoptosis. This gene encodes the ced-3 caspase that is similar to the interleukin-1-beta converting enzyme or ICE in mammals. In addition to apoptosis, caspases also function in the inflammatory response. Inflammatory caspases are essential in activating pro-inflammatory cytokines that recruit immune cells and block the replication of pathogens inside cells.

Inhibition of Cdk Activity

Inhibition of Cdk Activity

The orderly progression of the cell cycle depends on the activation of Cdk protein by binding to its cyclin partner. However, the cell cycle must be restricted when undergoing abnormal changes. Most cancers correlate to the deregulated cell cycle, and since Cdks are a central component of the cell cycle, Cdk inhibitors are extensively studied to develop anticancer agents. For instance, cyclin D associates with several Cdks, such as Cdk 4/6, to form an active complex. The cyclin D-Cdk4/6 complex...

Inhibition of CDK Activity

Inhibition of CDK Activity

The orderly progression of the cell cycle depends on the activation of Cdk protein by binding to its cyclin partner. However, the cell cycle must be restricted when undergoing abnormal changes. Most cancers correlate to the deregulated cell cycle, and since Cdks are a central component of the cell cycle, Cdk inhibitors are extensively studied to develop anticancer agents. For instance, cyclin D associates with several Cdks, such as Cdk 4/6, to form an active complex. The cyclin D-Cdk4/6 complex...

The Intrinsic Apoptotic Pathway

The Intrinsic Apoptotic Pathway

Internal cellular stress, such as cellular injury or hypoxia, triggers intrinsic apoptosis. The B-cell lymphoma 2 (Bcl-2) family of proteins are the primary regulators of the intrinsic apoptotic pathway. For example, during DNA damage, checkpoint proteins, such as Ataxia Telangiectasia Mutated (ATM protein) and Checkpoints Factor-2 (Chk2) proteins, are activated. These proteins phosphorylate p53 which further activates pro-apoptotic proteins, such as Bax, Bak, PUMA, and Noxa, and inhibits...

Combination Therapies and Personalized Medicine

Combination Therapies and Personalized Medicine

Combining two or more treatment methods increases the life span of cancer patients while reducing damage to vital organs or tissue from the overuse of a single treatment. Combination therapy also targets different cancer-inducing pathways, thus reducing the chances of developing resistance to treatment.
The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...

Targeted Cancer Therapies

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against specific...

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Related Experiment Video

Updated: Jul 6, 2026

Measuring Caspase Activity Using a Fluorometric Assay or Flow Cytometry

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

Anti-Cancer Agents in Medicinal Chemistry

|April 9, 2008

Summary

This summary is machine-generated.

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.

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Measuring Caspase Activity Using a Fluorometric Assay or Flow Cytometry

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Exploring Caspase Mutations and Post-Translational Modification by Molecular Modeling Approaches

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Lighting Up the Pathways to Caspase Activation Using Bimolecular Fluorescence Complementation

Lighting Up the Pathways to Caspase Activation Using Bimolecular Fluorescence Complementation

Published on: March 5, 2018

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.