OnCo

Checkpoints: PD-1, CTLA-4, LAG-3

T cells carry brakes so they do not attack the body. Tumours lean on them: PD-L1 on their surface, Tregs with CTLA-4, LAG-3 and TIGIT on exhausted T cells. Checkpoint inhibitors release the brakes; exhausted cells that are only tired recover, the broken do not.

Diagram

Pick a product above a diagram to see the nodes it hits and the escape routes below the block. Hover or tap any node or arrow for what it is; every node opens its target, glossary entry or the pathway page. Violet boxes are druggable targets.

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Dendritic cell (antigen + B7) activates TCR-peptide/MHCDendritic cell (antigen + B7) activates CD28-B7 (go)TCR-peptide/MHC activates Activated CD8 T cellCD28-B7 (go) activates Activated CD8 T cellCTLA-4 (stop) inhibits CD28-B7 (go)Activated CD8 T cell activates IFN-γIFN-γ activates PD-L1 on tumourPD-L1 on tumour activates PD-1 on T cellPD-1 on T cell inhibits Activated CD8 T cellLAG-3 / TIGIT inhibits Activated CD8 T cellActivated CD8 T cell activates Tumour cell killingDendritic cell (antigen + B7)Dendritic cell (antigen +…TCR-peptide/MHCTCR-peptide/MHCCD28-B7 (go): CD28 is the second signal a T cell needs before it attacks. Many CAR-T cells carry a piece of CD28 inside them to fire harder, ipilimumab works by stopping CTLA-4 from hogging CD28's partners, and a new bispecific…CD28-B7 (go)CTLA-4 (stop): The first immune brake ever targeted for cancer; releasing it won a Nobel Prize and cures a fraction of melanomas.CTLA-4 (stop)Activated CD8 T cellActivated CD8 T cellIFN-γIFN-γPD-L1 on tumour: PD-L1 is the tumour's side of the PD-1 brake, and also the biomarker that decides who gets immunotherapy.PD-L1 on tumourPD-1 on T cell: PD-1 is a brake on T cells. Blocking it releases the immune system against the tumour and has cured some previously incurable cancers.PD-1 on T cellLAG-3 / TIGIT: LAG-3 is the third immune brake to reach approval, combined with PD-1 blockade in melanoma.LAG-3 / TIGITTumour cell killingTumour cell killingactivatesinhibitsdruggable target (click)hit by selected productescape route
PD-1 / PD-L1 immune checkpoint & T-cell activationHow T cells decide to attack. A T cell needs to see the target (TCR-MHC) and get a 'go' signal (CD28). PD-1 and CTLA-4 are 'stop' signals; tumours exploit them. Checkpoint inhibitors remove the stop.

A soldier needs a target in the sights (TCR) and an order to fire (CD28). CTLA-4 is a commander revoking orders during training; PD-1 is a white flag the enemy waves on the battlefield that makes the soldier lower their weapon. Checkpoint inhibitors tear up the white flag.

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Chronic antigen, no help activates TCF1+ progenitor (stem-like)TCF1+ progenitor (stem-like) activates Transitory effectorTransitory effector activates Terminally exhaustedChronic antigen, no help activates TOX, NR4A, NFATTOX, NR4A, NFAT activates PD-1, LAG-3, TIM-3, TIGITTOX, NR4A, NFAT activates DNMT3A epigenetic scarDNMT3A epigenetic scar activates Terminally exhaustedPD-1, LAG-3, TIM-3, TIGIT inhibits Cytokines, killingTransitory effector activates Cytokines, killingCheckpoint blockade inhibits PD-1, LAG-3, TIM-3, TIGITCheckpoint blockade activates TCF1+ progenitor (stem-like)Chronic antigen, no help activates CAR-T exhaustionChronic antigen, no helpChronic antigen, no helpTCF1+ progenitor (stem-like)TCF1+ progenitor (stem-li…Transitory effectorTransitory effectorTerminally exhaustedTerminally exhaustedTOX, NR4A, NFAT: TOX (Thymocyte selection-associated high mobility group box protein TOX) is a protein that switches other genes on and off.TOX, NR4A, NFATDNMT3A epigenetic scarDNMT3A epigenetic scarPD-1, LAG-3, TIM-3, TIGIT: PD-1 is a brake on T cells. Blocking it releases the immune system against the tumour and has cured some previously incurable cancers.PD-1, LAG-3, TIM-3, TIGITCytokines, killingCytokines, killingCheckpoint blockade: LAG-3 is the third immune brake to reach approval, combined with PD-1 blockade in melanoma.Checkpoint blockadeCAR-T exhaustion: CD19 is a marker on B cells and B-cell cancers, and was the target of the first CAR-T therapies ever approved.CAR-T exhaustionactivatesinhibitsdruggable target (click)hit by selected productescape route
T-cell exhaustionT cells that see their target for weeks on end without winning gradually shut down: they raise a set of brakes (PD-1, LAG-3, TIM-3, TIGIT), lose their ability to kill, and eventually lock this state into their DNA. Checkpoint drugs rescue the ones that are only partly exhausted; the terminally exhausted are beyond reach.

A soldier posted at a wall for months with no relief. First tired, then unwilling to fire, finally unable to, and the last stage is written into their habits so deeply that no order can undo it. Checkpoint inhibitors work on the tired, not the broken.

What happens

In plain words, then the glossary entries the stage rests on. Chapter 6, Escaping the immune system: Every tumour that exists has already beaten the immune system once.

T cells carry brakes so they do not attack the body. Tumours lean on them: PD-L1 on their surface, Tregs with CTLA-4, LAG-3 and TIGIT on exhausted T cells. Checkpoint inhibitors release the brakes; exhausted cells that are only tired recover, the broken do not.

PD-1 / PD-L1 immune checkpoint & T-cell activation. How T cells decide to attack. A T cell needs to see the target (TCR-MHC) and get a 'go' signal (CD28). PD-1 and CTLA-4 are 'stop' signals; tumours exploit them. Checkpoint inhibitors remove the stop.

T-cell exhaustion. T cells that see their target for weeks on end without winning gradually shut down: they raise a set of brakes (PD-1, LAG-3, TIM-3, TIGIT), lose their ability to kill, and eventually lock this state into their DNA. Checkpoint drugs rescue the ones that are only partly exhausted; the terminally exhausted are beyond reach.

The molecular players

The proteins and genes at this stage, with their role and how many products act on each. Listed players come from the atlas; drawn players sit as nodes in the diagrams above.

Where medicines act

Products grouped by the node they hit, most advanced first, with the cancers an approved product is linked to. Pick one above the diagram to see it light up.

AtLAG-3node LAG-3 / TIGIT, Checkpoint blockade in PD-1 / PD-L1 immune checkpoint & T-cell activation and T-cell exhaustion3 products
Technologies acting hereImmune checkpoint inhibitors

How tumours escape

Records tied to this stage that describe resistance, evasion or tolerance. The resistance atlas lists the routes class by class.

Ideas that attack the escape
Papers on the escape

Measured by

Biomarkers, tests and assays in the corpus that read this stage in a patient.

Open questions

What is not known at this stage: the atlas's own questions, the bottlenecks it bears on, and the ideas in the corpus that try to answer them.

  • Which second checkpoint adds real benefit, and for whom (LAG-3 yes in melanoma; TIGIT mixed)?
  • Can exhaustion be reversed at the epigenetic level?
Ideas 58 linked ideas

48 more ideas are linked to this stage's pathways, targets and terms; see the rankings →

Key evidence

Papers in the corpus tied to this stage's pathways, targets and terms, newest first.

49 more papers in the key-papers index →

How this page is built: the stage is one entry in a curated atlas (src/data/mechanics-atlas.ts). Players, medicines, escape routes, tests, ideas and papers are resolved from the knowledge graph at build time through the stage's pathways, targets and terms, so every item here has its own page and sources. Where a section is missing, the corpus has no record tied to the stage yet. Nothing here is medical advice; see about and methodology. Stage 6.2 of 56.