Target intelligence / Profile preview

Caspase apoptotic pathway

Molecular classification
Enzyme (specifically, cysteine-aspartic protease), Apoptosis signaling pathway, Intrinsic apoptotic pathway, Extrinsic apoptotic pathway, Death receptor pathway (part of extrinsic)
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Overview

The caspase apoptotic pathway comprises a family of cysteine-dependent aspartate-specific proteases (caspases) that execute programmed cell death (apoptosis) via a highly regulated proteolytic cascade[3][1][7][5]. There are initiator caspases (e.g., caspase-8, -9, -10) activated by extrinsic signals (death receptors) or intrinsic signals (mitochondrial stress), which then activate effector caspases (e.g., caspase-3, -6, -7) to degrade vital cellular components, ensuring orderly cell death with minimal inflammation[1][3][5]. Dysregulation of this pathway is central to many diseases, including cancer, neurodegeneration, inflammation, and transplantation injury, making the pathway and specific caspases attractive targets for drug development[4][6][2].

Other names
Caspase pathwayApoptosis pathway (caspase-mediated)Caspase cascadeApoptotic caspase pathway
02

Mechanism of action

Caspase inhibition (blocks apoptosis) Activation of caspase cascade to induce cell death (anticancer) Modulation of regulatory proteins interacting with caspases (e.g., XIAP mimetics)

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Biological functions

Programmed cell death (apoptosis)Cell turnover/homeostasisImmune responseDevelopmental morphogenesisInflammatory signaling (some caspases)Cell differentiationTissue remodeling
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Disease associations

Cancer (deficient apoptosis promotes tumor survival)Neurodegenerative diseases (excessive apoptosis kills neurons)Inflammation/autoimmune diseases (aberrant cell death or caspase activity)Cardiovascular disease (ischemia-reperfusion injury)Infection (viral manipulation of apoptosis)Transplant injuryRetinal neuropathy, lumbar disc degeneration
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Safety considerations

Risk of unwanted apoptosis in healthy tissues (neurotoxicity, organ damage)Risk of immunosuppression or impaired clearance of damaged cellsDrug resistance/adaptation in cancerPotential off-target effects due to complex caspase roles in non-apoptotic functions (e.g., immune regulation)
06

Interacting drugs

Caspase inhibitors (e.g., IDN6556, VX-765)

2 more in the full profile.

07

Biomarkers

Cleaved caspase-3Cleaved caspase-7Cleaved PARP (Poly(ADP-ribose) polymerase, a caspase substrate)Transaminase levels (liver disease)Caspase activation profile in tissues

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