ArticleJournal of medicinal chemistry2020
Di-bromo-Based Small-Molecule Inhibitors of the PD-1/PD-L1 Immune Checkpoint.
Article in Journal of medicinal chemistry, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 32 papers.
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Who cites it
32 citing papers in PubMed, 72 citations in OpenAlex.
- Immune Checkpoint-Based Therapies in Colorectal Cancer-Current Approaches and Future Perspectives.International journal of molecular sciences · 2026Review
- A PD-1/PD-L1-Sensitive Co-culture-Based Primary T-Cell Activation Assay.Methods in molecular biology (Clifton, N.J.) · 2026Article
- Theoretical investigation on PD-L1-In-1 for cancer immunotherapy via density functional theory.Scientific reports · 2025Article
- PD-1/PD-L1 Inhibitors and Chemotherapy Synergy: Impact on Drug Resistance and PD-L1 Expression in Breast Cancer-Immune Cell Co-Cultures.International journal of molecular sciences · 2025Article
- Characterization of Clinically Evaluated Small-Molecule Inhibitors of PD-L1 for Immunotherapy.ACS medicinal chemistry letters · 2025Article
- Article
- Advancements in drug discovery: integrating CADD tools and drug repurposing for PD-1/PD-L1 axis inhibition.RSC advances · 2025Article
- Inactive-enriched machine-learning models exploiting patent data improve structure-based virtual screening for PDL1 dimerizers.Journal of advanced research · 2025Article
- Nonsymmetrically Substituted 1,1'-Biphenyl-Based Small Molecule Inhibitors of the PD-1/PD-L1 Interaction.ACS medicinal chemistry letters · 2024Article
- C2-Symmetrical Terphenyl Derivatives as Small Molecule Inhibitors of Programmed Cell Death 1/Programmed Death Ligand 1 Protein-Protein Interaction.Molecules (Basel, Switzerland) · 2024Article
- 1,5-Disubstituted tetrazoles as PD-1/PD-L1 antagonists.RSC medicinal chemistry · 2024Article
- Progress in small-molecule inhibitors targeting PD-L1.RSC medicinal chemistry · 2024Review
- Development andJournal of medicinal chemistry · 2024Article
- Review
- Solubilizer Tag Effect on PD-L1/Inhibitor Binding Properties forACS medicinal chemistry letters · 2024Article
- Inhibitors of Immune Checkpoints: Small Molecule- and Peptide-Based Approaches.Journal of personalized medicine · 2024Review
- Targeting PD-1/PD-L-1 immune checkpoint inhibition for cancer immunotherapy: success and challenges.Frontiers in immunology · 2024Review
- Exploring Hydrophilic PD-L1 Radiotracers Utilizing Phosphonic Acids: Insights into Unforeseen Pharmacokinetics.International journal of molecular sciences · 2023Article
- Design and Biological Evaluation of Small-Molecule PET-Tracers for Imaging of Programmed Death Ligand 1.Cancers · 2023Article
- Computational Approaches Drive Developments in Immune-Oncology Therapies for PD-1/PD-L1 Immune Checkpoint Inhibitors.International journal of molecular sciences · 2023Review
Corrections and comments
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Authors and funding
13 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Immune checkpoint blockade is one of the most promising strategies of cancer immunotherapy. However, unlike classical targeted therapies, it is currently solely based on expensive monoclonal antibodies, which often inflict immune-related adverse events. Herein, we propose a novel small-molecule inhibitor targeted at the most clinically relevant immune checkpoint, PD-1/PD-L1. The compound is capable of disrupting the PD-1/PD-L1 complex by antagonizing PD-L1 and, therefore, restores activation of T cells similarly to the antibodies, while being cheap in production and possibly nonimmunogenic. The final compound is significantly smaller than others reported in the literature while being nontoxic to cells even at high concentrations. The scaffold was designed using a structure-activity relationship screening cascade based on a new antagonist-induced dissociation NMR assay, called the weak-AIDA-NMR. Weak-AIDA-NMR finds true inhibitors, as opposed to only binders to the target protein, in early steps of lead compound development, and this process makes it less time and cost consuming.
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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.