ArticleActa pharmaceutica Sinica. B2022
YPD-30, a prodrug of YPD-29B, is an oral small-molecule inhibitor targeting PD-L1 for the treatment of human cancer.
Article in Acta pharmaceutica Sinica. B, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 19 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
19 citing papers in PubMed, 27 citations in OpenAlex.
- Integrated Machine Learning and Molecular Simulation-Guided Discovery of Novel Small-Molecule PD-L1 Inhibitors.Pharmaceuticals (Basel, Switzerland) · 2026Article
- Epigenetic activation of NK-cell effector programs and caspase-8-dependent apoptosis mediates the antitumor activity of LGP in NSCLC.Journal of ginseng research · 2026Article
- Temporal Dynamics of PD-L1 Surface in RKO Cells: Characterizing the Reversible Impact of the Small-Molecule Dimerizer BMS-202.Biomedicines · 2026Article
- Immune Checkpoint-Based Therapies in Colorectal Cancer-Current Approaches and Future Perspectives.International journal of molecular sciences · 2026Review
- Design, Synthesis and Biological Evaluation of Oxadiazole-Biphenyl Derivatives as Small Molecule Inhibitors Targeting PD-1/PD-L1 Immune Checkpoint.ACS medicinal chemistry letters · 2026Article
- Novel PD-L1 Small-Molecule Inhibitors Advancing Cancer Immunotherapy.Anti-cancer agents in medicinal chemistry · 2026Review
- In Situ Engineering of Tumor Cells as Self-Sustaining cDC1 Programming Factories for Effective Cancer Immunotherapy.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2026Article
- Phenotypic and targeted drug discovery in immune therapeutics: challenges, opportunities, and future directions.RSC advances · 2025Review
- Characterization of Clinically Evaluated Small-Molecule Inhibitors of PD-L1 for Immunotherapy.ACS medicinal chemistry letters · 2025Article
- Immune checkpoint inhibitors in cancer therapy: what lies beyond monoclonal antibodies?Medical oncology (Northwood, London, England) · 2025Review
- Article
- Development of small molecule drugs targeting immune checkpoints.Cancer biology & medicine · 2024Review
- Progress in small-molecule inhibitors targeting PD-L1.RSC medicinal chemistry · 2024Review
- The regulatory relationship between NAMPT and PD-L1 in cancer and identification of a dual-targeting inhibitor.EMBO molecular medicine · 2024Article
- Targeting PD-1/PD-L-1 immune checkpoint inhibition for cancer immunotherapy: success and challenges.Frontiers in immunology · 2024Review
- Challenges Coexist with Opportunities: Spatial Heterogeneity Expression of PD-L1 in Cancer Therapy.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2024Review
- Identification of CBPA as a New Inhibitor of PD-1/PD-L1 Interaction.International journal of molecular sciences · 2023Article
- A Potential Off-Target Effect of the Wnt/β-Catenin Inhibitor KYA1797K: PD-L1 Binding and Checkpoint Inhibition.Biomedicine hubArticle
- Article
Corrections and comments
- Erratum issued
Authors and funding
11 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
PD-1 and PD-L1 antibodies have brought about extraordinary clinical benefits for cancer patients, and their indications are expanding incessantly. Currently, most PD-1/PD-L1 agents are administered intravenously, which may be uncomfortable for some cancer patients. Herein, we develop a novel oral-delivered small molecular, YPD-29B, which specifically targets human PD-L1. Our data suggested that YPD-29B could potently and selectively block the interaction between PD-L1 and PD-1, but did not inhibit any other immune checkpoints. Mechanistically, YPD-29B induced human PD-L1 dimerization and internalization, which subsequently activated T lymphocytes and therefore overcomes immunity tolerance
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.