ArticleScientific reports2019
Comprehensive in vitro characterization of PD-L1 small molecule inhibitors.
Article in Scientific reports, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 71 papers.
What it found
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The trial behind it
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Who cites it
71 citing papers in PubMed.
- Integrated Machine Learning and Molecular Simulation-Guided Discovery of Novel Small-Molecule PD-L1 Inhibitors.Pharmaceuticals (Basel, Switzerland) · 2026Article
- Prediction of Patients' Response to Immune Checkpoint Inhibitors Using Fluorescence Lifetime Imaging of Lymphocytes.Biomedicines · 2026Article
- Targeting PD-1 in Squamous Cell Carcinoma: Flavonoid-based Therapeutics Unveiled throughCurrent computer-aided drug design · 2026Article
- Co-treatment of ticagrelor and anti-PD-1 immunotherapy in tumor-associated macrophages reduces pancreatic cancer cell growth and migration through the TGF-β1/Smad2 pathway.Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie · 2025Article
- Discovery of novel disulfide-containing PD-1/PD-L1 inhibitor with in vivo influenza therapeutic efficacy.Scientific reports · 2025Article
- Ordinary differential equation model of cancer-associated fibroblast heterogeneity predicts treatment outcomes.NPJ systems biology and applications · 2025Article
- Phenotypic and targeted drug discovery in immune therapeutics: challenges, opportunities, and future directions.RSC advances · 2025Review
- Targeting "don't eat me" signal: breast cancer immunotherapy.Breast cancer research and treatment · 2025Review
- Molecular Dynamics-Guided Repositioning of FDA-Approved Drugs for PD-L1 Inhibition with In Vitro Anticancer Potential.International journal of molecular sciences · 2025Article
- Discovery of PD-L1 Peptide Inhibitors from Ascidian Enzymatic Hydrolysates by Affinity Ultrafiltration Coupled to NanoLC-MS/MS.Marine drugs · 2025Article
- Differential scanning fluorimetry followed by microscale thermophoresis and/or isothermal titration calorimetry as an efficient tool for ligand screening.Biophysical reviews · 2025Review
- Beyond monoclonal antibodies: constraints and the case for alternative PD-1/PD-L1-targeting formats.Frontiers in immunology · 2025Review
- Inactive-enriched machine-learning models exploiting patent data improve structure-based virtual screening for PDL1 dimerizers.Journal of advanced research · 2025Article
- In Search of Better Peptide-(Derived from PD-L2)-Based Immune Checkpoint Inhibitors.Biomolecules · 2024Article
- Development of small molecule drugs targeting immune checkpoints.Cancer biology & medicine · 2024Review
- Oral PD-L1 inhibitor GS-4224 selectively engages PD-L1 high cells and elicits pharmacodynamic responses in patients with advanced solid tumors.Journal for immunotherapy of cancer · 2024Article
- Synergistic vesicle-vector systems for targeted delivery.Journal of nanobiotechnology · 2024Review
- In silico exploration of PD-L1 binding compounds: Structure-based virtual screening, molecular docking, and MD simulation.PloS one · 2024Article
- Effect of Fragment 1 on the Binding of Epigallocatechin Gallate to the PD-L1 Dimer Explored by Molecular Dynamics.Molecules (Basel, Switzerland) · 2023Article
- Proof of concept: Pull down assay using bovine serum albumin and an immunomodulator small molecule.Heliyon · 2023Article
11 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
29 authors.
Funding
Abstract
Blockade of the programmed cell death 1 (PD-1)/programmed cell death-ligand 1 (PD-L1) interaction has emerged as a powerful strategy in cancer immunotherapy. Recently, there have been enormous efforts to develop potent PD-1/PD-L1 inhibitors. In particular, Bristol-Myers Squibb (BMS) and Aurigene Discovery Technologies have individually disclosed several promising PD-1/PD-L1 inhibitors, whose detailed experimental data are not publicly disclosed. In this work, we report the rigorous and systematic in vitro characterization of a selected set of potent PD-1/PD-L1 macrocyclic peptide (BMSpep-57) and small-molecule inhibitors (BMS-103, BMS-142) from BMS and a peptidomimetic small-molecule inhibitor from Aurigene (Aurigene-1) using a series of biochemical and cell-based assays. Our results confirm that BMS-103 and BMS-142 are strongly active in biochemical assays; however, their acute cytotoxicity greatly compromised their immunological activity. On the other hand, Aurigene-1 did not show any activity in both biochemical and immunological assays. Furthermore, we also report the discovery of a small-molecule immune modulator, whose mode-of-action is not clear; however, it exhibits favorable drug-like properties and strong immunological activity. We hope that the results presented here will be useful in guiding the development of next-generation PD-1/PD-L1 small molecule inhibitors.
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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.