Emerging Immune Checkpoints - ART1

Immunotherapy offers new avenues for tumor treatment with unique advantages and great potential, and immune checkpoint blockade is an important component of immunotherapy. PD-1 and CTLA4 are currently the most commonly used targets for immune checkpoint inhibition.

Now, we also need to discover more immunotherapeutic targets to provide more options for immunotherapy. Creative Biolabs is an expert in the field of immune checkpoint research and we are committed to continuously discovering new therapeutic targets and developing new immune checkpoint inhibitors. Here, we introduce an emerging immune checkpoint: ART1.

Introduction to ART1

ATR1, known as Adenosine 5'-diphosphate (ADP)-ribosyltransferase-1, is a glycosylphosphatidylinositol (GPI)-anchored enzyme with an extracellular catalytic domain. It has been found that blocking ART1 increases anti-tumor immune cells in tumors and slows or stops tumor growth in animal models of cancer, suggesting that ART1 is a promising new target for enhancing cancer immunotherapy.

ART1 is an actionable target for enhancing T cell-mediated tumor rejection. ART1 inhibition mediated at both genetic and antibody levels was found to increase CD8+ T cell infiltration, thereby slowing tumor growth in mice.

R&D Status of Targeted ART1

Tumor expression of ART1 can reduce T cell infiltration by modulating P2X7R on CD8+ T cells to complete the immune transplantation mechanism. However, ART1 development is still at an early stage, and no relevant drug studies have been reported.

  • Number of marketed drugs: 0
  • Highest stage of development: preclinical

Although no further studies and clinical trials are available, ART1-targeted drugs have demonstrated potential therapeutic options, including the combination of PD-1 antibodies, CD38 antibodies or P2X7R agonists.

Development Strategies for Targeted Inhibition of ART1

ART1 are expressed in a variety of immune cells and influence disease development through regulation of immune cells. Therefore, we explore the development of inhibitors targeting ART1 as a potential therapeutic strategy and provide related research services.

  • Development of small molecule inhibitors. We provide immune checkpoint-targeted small molecule drug development services to assist our clients in achieving their ATR1 research and drug development goals. These include high-throughput screening, structure-based drug design, organic synthesis and other methods which are available to identify small molecules that can specifically bind ART1.
  • Development of peptide-based inhibitors. Peptides can be designed to disrupt the binding of ART1 to its target proteins. With our proven peptide design system and state-of-the-art facilities, we are able to provide high-quality, comprehensive ART1-targeted peptide development services to our customers worldwide.
  • Development of antibody inhibitors. Monoclonal antibodies against ART1 can be generated to block or inhibit its activity. Our comprehensive portfolio of services includes antibody discovery and development, antibody characterization, antibody engineering, antibody optimization and antibody production.

Future Research Direction

The development of ART1 inhibitors is an active area of research and progress has been made in identifying lead compounds and optimizing their potency and selectivity. The following points are noteworthy for future research and development.

  • Specificity and selectivity. Specifically targeting ART1 should be designed to avoid unwanted side effects.
  • The specific role of ADP-ribosylation in different cellular processes and diseases. This is crucial for the rational design of ART1 inhibitors with therapeutic potential.

Creative Biolabs is committed to providing a wide range of immune checkpoint development services, including immune checkpoint ART1. Please don't hesitate to contact us.


  1. Stiles B. Targeting ART1, a Novel Immune Checkpoint, for the Treatment of Lung Cancer. CORNELL UNIV MEDICAL COLL (WEILL) NEW YORK, 2020.

All listed customized services & products are for research use only, not intended for pharmaceutical, diagnostic, therapeutic, or any in vivo human use.