Target intelligence / Profile preview

Cluster of differentiation 80 and Cluster of differentiation 86 co-stimulatory molecules (CD80/CD86)

Target
CD80/CD86
Molecular classification
Receptor ligand (co-stimulatory molecule), Immunoglobulin superfamily protein, Cell surface glycoprotein
01

Overview

CD80 and CD86 are closely related cell surface glycoproteins belonging to the immunoglobulin superfamily. They are primarily expressed on professional antigen-presenting cells such as dendritic cells, activated B-cells, macrophages, and some activated T-cells. Both function as critical co-stimulatory ligands required for full T-cell activation. They bind two key receptors on T-cells: * **CD28**, which delivers a positive signal promoting T-cell proliferation, cytokine production, survival, and effector function; * **CTLA‑4**, which delivers an inhibitory signal dampening immune responses. The balance between these signals is essential for effective immunity while preventing autoimmunity. Both proteins play central roles in transplant rejection, allergy/asthma pathogenesis, anti-tumor immunity regulation, infectious disease responses—including Epstein-Barr virus—and tolerance induction. Therapeutically targeting this axis has led to approved biologics like abatacept/belatacept that inhibit co-stimulation by mimicking CTLA‑4 binding; conversely checkpoint inhibitors like ipilimumab block inhibitory signaling through CTLA‑4. The expression pattern and functional state of these molecules can be used as biomarkers in clinical settings. Structurally: * **CD80/B7–1:** Type I transmembrane protein (~33 kDa), predominantly forms dimers; higher affinity binding than CD86; upregulated upon stimulation by various cytokines/LPS. * **CD86/B7–2:** Constitutively expressed at low levels but rapidly upregulated after APC stimulation; binds same receptors but with different kinetics compared to CD80.

Other names
B7-1 (for CD80)B7-2 (for CD86)B7 family co-stimulatory moleculesCostimulatory ligands/receptors
02

Mechanism of action

Drugs targeting these molecules typically: - Block or modulate the interaction between CD80/CD86 on antigen-presenting cells and their receptors on T cells—CD28 for activation or CTLA‑4 for inhibition. - Inhibit costimulation to suppress unwanted immune responses in autoimmunity or transplantation. - Enhance costimulation to boost anti-tumor immunity in cancer therapy.

03

Biological functions

Immune response modulationT cell activation and inhibitionCo-stimulation of T lymphocytesRegulation of self-tolerance and immune homeostasis
04

Disease associations

Cancer (immunotherapy target, tumor immune evasion)Inflammation/autoimmune disease (e.g., asthma, transplant rejection)Infection (regulation during viral infections such as EBV)
05

Safety considerations

Risk of over-suppression leading to infection or malignancy when blocking costimulation.Risk of excessive immune activation leading to autoimmunity when enhancing costimulation.Therapeutic manipulation must balance efficacy with risk for immune-related adverse events.
06

Interacting drugs

Abatacept (CTLA4-Ig fusion protein)

2 more in the full profile.

07

Biomarkers

Expression levels of CD80/CD86 on antigen-presenting cells can serve as biomarkers for: Immune activation statusPredicting response to immunotherapies targeting the CTLA‑4/B7 axis

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