Target intelligence / Profile preview

Cytotoxic T-lymphocyte associated protein 4 receptor (CTLA-4)

Target
CTLA-4
Molecular classification
Receptor, Immune checkpoint, Member of the immunoglobulin superfamily
01

Overview

Cytotoxic T‑lymphocyte associated protein 4 receptor (CTLA‑4) is an inhibitory immune checkpoint receptor expressed primarily on activated and regulatory T cells. It is a type I transmembrane glycoprotein belonging to the immunoglobulin superfamily. Upon binding its ligands CD80 or CD86 on antigen-presenting cells with high affinity, it transmits an inhibitory signal that downregulates early stages of T cell activation. This function serves as a critical brake on adaptive immunity to maintain self-tolerance and prevent excessive immune responses. Therapeutically targeting CTLA‑4 with monoclonal antibodies releases this inhibition, enhancing anti-tumor immunity but also increasing risk for autoimmune side effects.

Other names
CD152CTLA4Cytotoxic T-lymphocyte antigen 4Cytotoxic T-lymphocyte associated antigen 4 receptor
02

Mechanism of action

Drugs such as ipilimumab block the interaction between CTLA‑4 and its ligands (CD80/CD86), thereby preventing inhibitory signaling. This enhances T cell activation and proliferation, boosting anti-tumor immune responses.

03

Biological functions

Negative regulation of T cell activationImmune response modulationMaintenance of self-tolerance by limiting immune responsesInhibition of co-stimulatory signaling in T cells
04

Disease associations

Cancer (immune evasion)Autoimmune diseases (loss or dysfunction leads to autoimmunity)Inflammation
05

Safety considerations

Immune-related adverse events due to loss of self-toleranceColitisDermatitisHepatitisEndocrinopathiesSevere autoimmunity due to overactivation
06

Interacting drugs

Ipilimumab (monoclonal antibody)

2 more in the full profile.

07

Biomarkers

CTLA‑4 expression on activated or regulatory T cells for patient selection in immunotherapySoluble forms of CTLA‑4 for efficacy or immune-related adverse events monitoring

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