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Author Spotlight: A Selective Luciferase-Based Assay for Monitoring ATG4B 27 Activity in Cells
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Cell based functional assays for IDO1 inhibitor screening and characterization.
1Polaris Pharmaceuticals, San Diego, CA, USA.
Oncotarget
|August 17, 2018
Summary
Two new cell-based assays effectively screen indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors for cancer immunotherapy. These assays measure IDO1 activity and its impact on T cell activation, aiding drug development.
Area of Science:
- Immunology
- Pharmacology
- Cancer Biology
Background:
- Indoleamine 2,3-dioxygenase 1 (IDO1) is a key immune-oncology target.
- IDO1 inhibitors show clinical promise, particularly with immune-stimulating agents.
Purpose of the Study:
- To describe two robust, adaptable cell-based assays for screening IDO1 inhibitors.
- To evaluate the impact of IDO1 inhibition on T cell activation.
Main Methods:
- Inducing endogenous IDO1 in cancer cells with interferon-gamma.
- Measuring kynurenine production to assess IDO1 activity.
- Co-culture assays with Jurkat T cells to evaluate T cell activation and viability.
Main Results:
- Assays successfully detected IDO1 activity and inhibition by clinical candidates epacadostat and BMS-986205.
- Nanomolar concentrations of inhibitors rescued IDO1-mediated T cell inhibition.
- Micromolar concentrations of BMS-986205 showed off-target effects on T cell activation and viability.
Conclusions:
- The developed assays are suitable for screening IDO1 inhibitors in research and drug development.
- Assays provide insights into IDO1 inhibitor efficacy and potential off-target effects on immune cells.
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