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Target intelligence / Profile preview
Cytotoxic T-Lymphocyte–Associated Protein 4 (CTLA-4)
- Target
- CTLA-4
- Molecular classification
- Receptor, Immune Checkpoint
01
Overview
CTLA-4 is a protein receptor that functions as an immune checkpoint, acting as a critical negative regulator of T-cell mediated immune responses. It is primarily expressed on activated T cells and constitutively on regulatory T cells (Tregs). CTLA-4 competes with the costimulatory receptor CD28 for binding to CD80 and CD86 on antigen-presenting cells, delivering an inhibitory rather than stimulatory signal when engaged. It is essential for maintaining immune homeostasis and preventing autoimmunity. Blockade of CTLA-4 has become a foundational strategy in immuno-oncology.
- Other names
- CD152
02
Mechanism of action
Inhibition of T-cell activation by competing with CD28 for B7 ligands (CD80/CD86) and recruiting phosphatases to dephosphorylate key signaling kinases.
03
Biological functions
Immune regulationT-cell inhibitionMaintenance of self-toleranceDownregulation of effector responses
04
Disease associations
Autoimmune diseaseCancerLymphoproliferative disorders
05
Safety considerations
Autoimmune side effectsImmune-related adverse events (irAEs)
06
Interacting drugs
Anti-CTLA-4 antibodies (e.g., Ipilimumab)
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