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Updated: Oct 29, 2025
Identifying PD-1/PD-L1 Inhibitors with Surface Plasmon Resonance Technology
Published on: May 2, 2025
Advance investigation on synthetic small-molecule inhibitors targeting PD-1/PD-L1 signaling pathway
Annoor Awadasseid1, Yanling Wu2, Wen Zhang3
1Lab of Chemical Biology and Molecular Drug Design, College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou 310014, China; Institute of Drug Development & Chemical Biology, Zhejiang University of Technology, Hangzhou 310014, China; Department of Biochemistry & Food Sciences, University of Kordofan, El-Obeid 51111, Sudan.
Abstract:
Immune checkpoint blockade has displayed substantial anti-tumor resistance in a variety of forms of cancer, but the fundamental regulation role remains unclear, and several questions continue to be addressed. PD-1/PD-L1 has been recognized as an anti-cancer drug target for several years, and through targeting the PD-1/PD-L1 signaling pathway, many monoclonal antibodies have thus far produced promising results in cancer therapy. The discovery of small-molecule inhibitors focused on the PD-1/PD-L1 signaling pathway is steadily reviving over decades, owing to the intrinsic shortcomings of the antibodies. PD-1 function and its PD-L1 or PD-L2 ligands are essential for the activation, proliferation, and cytotoxic secretion of T-cells in cancer to degenerate anti-tumor immune response. The axis PD-1/PD-L1 is important for the immune escape of cancer which has an immense impact on cancer treatment. In this review, we summarize the function of PD-1 and PD-L1 in cancer and aiming to enhance cancer therapy.
Insights
Immune checkpoint inhibitors targeting PD-1/PD-L1 show promise in cancer therapy. This review explores PD-1 and PD-L1 functions to improve anti-cancer treatments.
Area of Science:
- Immunology
- Oncology
- Pharmacology
Background:
- Immune checkpoint blockade demonstrates significant anti-tumor effects across various cancers.
- The PD-1/PD-L1 signaling pathway is a validated target for cancer immunotherapy.
- Antibodies targeting PD-1/PD-L1 have yielded promising clinical outcomes.
Purpose of the Study:
- To review the critical roles of PD-1 and its ligands (PD-L1, PD-L2) in cancer.
- To elucidate the mechanisms by which PD-1/PD-L1 axis contributes to immune evasion in cancer.
- To explore strategies for enhancing cancer therapy by modulating the PD-1/PD-L1 pathway.
Main Methods:
- Literature review of studies on PD-1/PD-L1 pathway in cancer.
- Analysis of the function of PD-1 and its ligands in T-cell regulation.
- Evaluation of current and emerging therapeutic strategies targeting PD-1/PD-L1.
Main Results:
- PD-1/PD-L1 interaction is crucial for T-cell dysfunction and tumor immune escape.
- Small-molecule inhibitors offer an alternative to antibodies, addressing antibody-related limitations.
- Targeting PD-1/PD-L1 is essential for overcoming anti-tumor resistance.
Conclusions:
- Understanding PD-1/PD-L1 functions is key to improving cancer immunotherapy efficacy.
- Modulating the PD-1/PD-L1 axis holds significant potential for advancing cancer treatment.
- Further research into PD-1/PD-L1 inhibitors can lead to more effective anti-cancer therapies.
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