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Updated: Jan 11, 2026
Identifying PD-1/PD-L1 Inhibitors with Surface Plasmon Resonance Technology
Published on: May 2, 2025
PD-L1-targeted novel molecule design: recent advances in immunomodulatory technologies and emerging insights in
Feng Zhang1, Ruyue Ni1, Liang Qian1
1Lab of Chemical Biology and Molecular Drug Design, College of Pharmaceutical Science, Zhejiang University of Technology, Deqing 313299, China; Institute of Drug Development & Chemical Biology, Zhejiang University of Technology, Deqing 313299, China.
Abstract:
Programmed death-ligand 1 (PD-L1) plays a central role in immune evasion by tumors, making it a crucial target for cancer immunotherapy. While current anti-PD-L1 therapies have shown promise, they face several clinical limitations, such as suboptimal efficacy and resistance. Recent advancements in PD-L1-targeted molecules, including bifunctional small-molecule inhibitors and protein degradation strategies, are revolutionizing cancer treatment. These novel approaches target PD-L1 at multiple levels, disrupting tumor immune escape and enhancing antitumor immunity. Bifunctional inhibitors target both PD-L1 and additional immune or non-immune pathways, providing improved tumor penetration and overcoming resistance mechanisms. Protein degradation technologies, such as PROTACs, facilitate targeted PD-L1 degradation via proteasomal or lysosomal pathways, offering more durable therapeutic effects. Furthermore, innovations like bioorthogonal chemistry and lysosome-targeting technologies promise more precise drug delivery and reduced systemic toxicity. This review highlights the latest developments in PD-L1 modulation, explores their mechanisms of action, and discusses their therapeutic potential, paving the way for next-generation cancer immunotherapies.
Insights
Novel strategies targeting programmed death-ligand 1 (PD-L1) are advancing cancer immunotherapy. Bifunctional inhibitors and protein degradation technologies offer improved efficacy and overcome resistance for better antitumor immunity.
Area of Science:
- Oncology
- Immunology
- Pharmacology
Background:
- Programmed death-ligand 1 (PD-L1) is a key mediator of tumor immune evasion.
- Current anti-PD-L1 therapies exhibit limitations including suboptimal efficacy and resistance.
- Targeting PD-L1 is crucial for enhancing cancer immunotherapy.
Purpose of the Study:
- To review recent advancements in PD-L1-targeted molecules for cancer immunotherapy.
- To explore novel mechanisms of action for disrupting tumor immune escape.
- To discuss the therapeutic potential of next-generation PD-L1 modulation strategies.
Main Methods:
- Review of emerging bifunctional small-molecule inhibitors targeting PD-L1 and other pathways.
- Analysis of protein degradation strategies like PROTACs for targeted PD-L1 elimination.
- Exploration of innovations in bioorthogonal chemistry and lysosome-targeting for drug delivery.
Main Results:
- Bifunctional inhibitors enhance tumor penetration and overcome resistance.
- Protein degradation technologies offer durable therapeutic effects via proteasomal or lysosomal pathways.
- New technologies promise more precise drug delivery and reduced systemic toxicity.
Conclusions:
- Novel PD-L1 targeting strategies are revolutionizing cancer treatment.
- These approaches disrupt tumor immune escape and boost antitumor immunity.
- Innovations pave the way for next-generation cancer immunotherapies with improved outcomes.
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