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Immune Checkpoints – Immune Regulation, Cancer and Biomarker Analysis

What are immune checkpoints?

Immune checkpoints are key regulatory mechanisms of the immune system that control the activation, intensity, and duration of immune responses. They are primarily mediated by inhibitory receptors expressed on immune cells, especially T lymphocytes, and are essential for maintaining immune tolerance and preventing excessive or autoimmune reactions.

Under pathological conditions such as cancer or chronic infections, immune checkpoint pathways can be hijacked to suppress immune responses, leading to T-cell exhaustion and immune evasion.

AnyGenes Immune Checkpoints Array for Enhanced Immunotherapy Research

Immune checkpoint pathway activity can be efficiently assessed by measuring gene expression of key inhibitory receptors, ligands, and immune exhaustion–related signatures.

Mechanism of immune checkpoint-mediated T-cell inactivation.
Mechanism of immune checkpoint-mediated T-cell inactivation.

Key takeaways

  • Central regulators of T-cell activation and immune tolerance
  • Prevent autoimmunity and immune overactivation
  • Exploited by tumors for immune escape
  • Core targets of modern cancer immunotherapy
  • Highly relevant for biomarker discovery and immune profiling

Major immune checkpoint molecules

PD-1 / PD-L1 – PD-L2

PD-1 is an inhibitory receptor expressed on activated T cells. Binding to PD-L1 or PD-L2 suppresses T-cell proliferation, cytokine production, and cytotoxic activity. This pathway is frequently upregulated in tumors.

CTLA-4

CTLA-4 regulates early T-cell activation by competing with CD28 for B7 ligands on antigen-presenting cells, thereby limiting immune responses.

LAG-3

LAG-3 contributes to T-cell exhaustion and is emerging as a clinically relevant immune checkpoint, often targeted in combination with PD-1 inhibitors.

TIM-3

TIM-3 is involved in immune exhaustion in cancer and chronic infections and represents a promising next-generation immunotherapy target.

Mechanism of immune checkpoint signaling

Immune checkpoints function through inhibitory signaling cascades triggered by receptor-ligand interactions. These signals:

  • Reduce T-cell proliferation
  • Decrease cytokine production
  • Suppress cytotoxic immune functions

While essential for immune homeostasis, these pathways can be exploited by tumors to inhibit antitumor immunity.

Immune checkpoints and disease

Cancer

Tumors frequently overexpress immune checkpoint ligands (e.g. PD-L1) to suppress antitumor immune responses. Immune checkpoint inhibitors (ICIs) have transformed cancer therapy across multiple tumor types.

Chronic infections

In persistent viral infections (HIV, hepatitis), prolonged immune checkpoint activation leads to functional exhaustion of T cells and pathogen persistence.

Autoimmune diseases

Dysregulated checkpoint signaling can contribute to excessive immune activation and autoimmunity.

Therapeutic and clinical applications

Immune checkpoint molecules are among the most important therapeutic targets today:

  • PD-1, PD-L1 and CTLA-4 inhibitors in oncology
  • Combination immunotherapies
  • Emerging targets such as LAG-3 and TIM-3

Identifying immune checkpoint-related gene expression signatures is critical for patient stratification and treatment response prediction.

Why study immune checkpoints with AnyGenes?

At AnyGenes®, we provide high-performance qPCR arrays and fully customizable SignArrays® dedicated to immune checkpoint analysis.

Our solutions allow researchers to:

  • Quantify PD-1, PD-L1, CTLA-4, LAG-3, TIM-3 expression
  • Study T-cell activation and exhaustion signatures
  • Investigate cross-talk with NF-κB, JAK-STAT and cytokine pathways
  • Generate robust, reproducible, publication-ready data

Immune checkpoints biomarker analysis with AnyGenes®

What can be analyzed?

  • Immune checkpoint receptors and ligands
  • T-cell activation and exhaustion markers
  • Cytokines and immune mediators
  • Predictive biomarkers for immunotherapy response

Customize your own signaling pathways (SignArrays®) with the factors of your choice!
Simply download and complete our Personalized SignArrays® information file and send it at [email protected] to get started on your project.

Frequently asked questions

Immune checkpoints are inhibitory pathways that regulate immune activation and maintain immune tolerance.

Tumors exploit immune checkpoints to evade immune surveillance, making them key targets in cancer immunotherapy.

PD-1, PD-L1, CTLA-4, LAG-3 and TIM-3

By measuring gene expression of immune checkpoint markers using targeted qPCR pathway arrays.

  1. Meng L, et al. Mechanisms of immune checkpoint inhibitors: insights into the regulation of circular RNAS involved in cancer hallmarks. Cell Death Dis. (2024)4;15(1):3.
  2. Younis A,  Gribben J. Immune Checkpoint Inhibitors: Fundamental Mechanisms, Current Status and Future Directions. Immuno (2024):4(3),186-210.
  3. Renga G, et al. Optimizing therapeutic outcomes of immune checkpoint blockade by a microbial tryptophan metabolite. J Immunother Cancer. (2022);10(3):e003725.
  4. Cai H, et al. Immune Checkpoints in Viral Infections. Viruses. (2020)21;12(9):1051.
  5. He X, et al.  Immune checkpoint signaling and cancer immunotherapy. Cell Res. (2020);30(8):660-669.

Immune checkpoints biomarker list

You can check the biomarker list included in this pathway, see below:

Species : Homo sapiens (human)

Human signaling pathway

Signaling PathwaysProduct refInformations

Immune Checkpoints

IC1H1

List infos


Species : Mus musculus (mouse)

Mouse signaling pathway

Signaling PathwaysProduct refInformations

Immune Checkpoints

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List In progress...


Species : Rattus norvegicus (rat)

Rat signaling pathway

Signaling PathwaysProduct refInformations

Immune Checkpoints

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List In progress...


Species : Sus Scrofa (Pig)

Pig Immune Checkpoints

Signaling PathwaysProduct refInformations

Immune Checkpoints

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List In progress...


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For more information on prices, please contact us at:

[email protected]