Target intelligence / Profile preview

Cytotoxic T lymphocyte–associated antigen 4 (CTLA-4)

Target
CTLA-4
Molecular classification
Receptor, Immunoglobulin superfamily, Transmembrane glycoprotein
01

Overview

CTLA-4 (Cytotoxic T lymphocyte–associated antigen 4), also known as CD152, is a protein receptor found primarily on the surface of activated T cells and regulatory T cells (Tregs). It is a member of the immunoglobulin superfamily and plays a critical role as an immune checkpoint molecule, helping to regulate and suppress immune responses. It acts as an inhibitory regulator at early stages of the immune response, competing with the costimulatory receptor CD28 for binding to B7 molecules (CD80/CD86) on APCs. Blocking antibodies against CTLA-4 can enhance anti-tumor immunity but may also increase risk for autoimmune side effects.

Other names
CD152
02

Mechanism of action

CTLA-4 acts as an inhibitory regulator at early stages of the immune response by competing with CD28 for binding to B7 molecules (CD80/CD86) on APCs, recruiting phosphatases, and downregulating key transcription factors.

03

Biological functions

Immune regulationT cell activationT cell inhibitionMaintenance of self-tolerance
04

Disease associations

AutoimmunityCancer
05

Safety considerations

Autoimmune side effects due to loss of peripheral tolerance control mechanisms
06

Interacting drugs

Ipilimumab

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