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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.

Drug Discovery: Overview

Drug Discovery: Overview

Drug discovery is a multifaceted process involving extensive screening, testing, and optimization of lead compounds to identify potential new drugs for therapeutic use. It combines several approaches, including screening large numbers of natural products, chemical modification of known active molecules, identification of new drug targets, and rational design based on biological mechanisms and drug-receptor structure. These approaches are carried out in both academic research laboratories and...

CRISPR/Cas9 Genome Editing

CRISPR/Cas9 Genome Editing

The CRISPR-Cas system serves as a bacterial defense mechanism against invading genetic elements such as viruses and plasmids, forming the foundation for its adaptation as a powerful genome-editing tool. Originally discovered in prokaryotes, this system has been repurposed to revolutionize genetic engineering across a wide range of organisms, including plants, animals, and humans. The core component, Cas9, is an endonuclease derived from Streptococcus pyogenes, capable of introducing...

Targets for Drug Action: Overview

Targets for Drug Action: Overview

Drugs target macromolecules to modify ongoing cellular processes. Primary drug targets include receptors, ion channels, transporters, and enzymes.
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...

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...

The Extrinsic Apoptotic Pathway

The Extrinsic Apoptotic Pathway

The extrinsic apoptotic pathway is initiated when extracellular death-inducing signals, such as specific cytokines, activate the death receptors expressed on the cell surface. The immune cells involved in this pathway are natural killer cells (NK cells) and cytotoxic T-lymphocytes. NK cells are critical in innate immune response, while cytotoxic T-lymphocytes are associated with adaptive immune response. These cells recognize specific receptors expressed on the altered cells and activate...

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Related Experiment Video

Updated: Jun 21, 2026

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

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

Published on: October 13, 2022

Caspases: a drug discovery perspective.

¹Department of Neuroscience Therapeutics, Parke-Davis Pharmaceutical Research, Ann Arbor, MI 48105, USA. kevin.wang@wl.com

Current Opinion in Drug Discovery & Development

|August 4, 2009

Summary

This summary is machine-generated.

Unscheduled cell death, or apoptosis, is significant in many diseases. Caspase inhibitors show promise for treating these conditions by suppressing apoptosis.

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Area of Science:

Biochemistry
Molecular Biology
Pathology

Background:

Unscheduled apoptosis is implicated in numerous human diseases, including stroke, Alzheimer's, and liver/cardiac injury.
The apoptosis cascade involves a family of intracellular cysteine proteinases known as caspases.
Caspase inhibitors have emerged as a key area of research in understanding and potentially treating apoptosis-related disorders.

Purpose of the Study:

To highlight the role of caspases in the apoptosis cascade.
To discuss the therapeutic potential of caspase inhibition in various human diseases.
To underscore the significance of apoptosis in disease pathogenesis.

Main Methods:

Review of recent advances in apoptosis research.
Elucidation of the biochemical machinery of apoptosis.
Analysis of in vitro and in vivo studies on caspase inhibitors.

Main Results:

Caspases play a central role in the apoptosis cascade.
Caspase inhibitors (peptide or protein) effectively suppress unscheduled apoptotic cell death.
Evidence supports the therapeutic potential of targeting caspases.

Conclusions:

Targeting caspases offers a promising therapeutic strategy for diseases characterized by unscheduled apoptosis.
Further research into caspase inhibition could lead to novel treatments for a range of debilitating conditions.