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Target intelligence / Profile preview
Apoptotic protease-activating factor 1 (APAF1)
- Target
- APAF1
- Molecular classification
- Scaffold protein, Adaptor protein
01
Overview
Apoptotic protease-activating factor 1 (APAF1) is a key cytoplasmic protein that plays a central role in the intrinsic (mitochondrial) pathway of apoptosis. It acts as an essential hub in the regulation and execution of programmed cell death by forming the apoptosome complex, which activates downstream caspases. Upon release of cytochrome c from mitochondria into the cytosol during apoptosis, cytochrome c binds to APAF1 along with dATP/ATP. This binding induces conformational changes in APAF1, leading to its oligomerization into a heptameric structure known as the apoptosome. The apoptosome then recruits procaspase‑9 via CARD–CARD interactions, leading to its activation and the initiation of the caspase cascade.
02
Mechanism of action
Not applicable; APAF1 itself is not directly targeted by drugs. Drugs influence upstream processes that affect APAF1 activity.
03
Biological functions
ApoptosisCaspase activationApoptosome formation
04
Disease associations
CancerTherapy resistance
05
Safety considerations
Inhibition of APAF1 could lead to unwanted cell survival and tumor progressionActivation of APAF1 in healthy cells could induce unwanted apoptosis
06
Biomarkers
APAF1 expression levels as a predictor of response to chemotherapyMutations in APAF1 as a marker of resistance to apoptosis-inducing therapies
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