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Immune checkpoint inhibitor targets

Molecular classification
Receptor (cell-surface protein), Immune checkpoint molecule, Immunoregulatory cell-surface glycoprotein
01

Overview

Immune checkpoint inhibitor targets are cell-surface proteins, most notably **PD-1**, **CTLA-4**, **PD-L1**, and newer proteins such as **LAG-3**, that function as negative regulators of the immune response. These checkpoints are essential for maintaining self-tolerance and modulating the strength and duration of immune responses, thereby preventing autoimmunity. Tumor cells can exploit these pathways by expressing ligands like PD-L1, thereby inhibiting T cell–mediated antitumor responses. Immune checkpoint inhibitors are monoclonal antibodies that block these inhibitory signals, thereby restoring and enhancing T cell activity against cancer cells. Their use has revolutionized the management of various cancers but is associated with distinctive immune-related toxicities requiring careful management[1][2][4][5][6]. **Note:** "Immune checkpoint inhibitor targets" is not a canonical molecular target name, but instead refers to a group or family of proteins. For structured data, each target (e.g., PD-1, CTLA-4, PD-L1, LAG-3) should be extracted and described separately for precise records.

Other names
Immune checkpoint moleculesimmune inhibitory receptorscoinhibitory immune receptorscheckpoint proteinsimmune inhibitory ligands
02

Mechanism of action

Monoclonal antibody blockade of immune checkpoint receptors (e.g., PD-1, CTLA-4, LAG-3), preventing their interaction with ligands and thus relieving inhibitory signals on T cells, allowing enhanced immune-mediated destruction of tumor cells[4][5][6].

03

Biological functions

Immune response modulationDownregulation of T cell activationMaintenance of immune self-toleranceLimiting autoimmunityImmune evasion by tumor cells
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Disease associations

CancerInfectionAutoimmunity (in the context of therapeutic adverse effects)
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Safety considerations

Immune-related adverse events including colitis, hepatitis, pneumonitis, endocrinopathies, dermatologic, and other systemic inflammatory reactions[4][6].Risk of severe or fatal autoimmunity.
06

Interacting drugs

8 more in the full profile.

07

Biomarkers

PD-L1 expression levels (tumor/immune cells)Microsatellite instability-high (MSI-H)Mismatch repair deficiency (dMMR)Tumor mutational burden-high (TMB-H)[5]

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