ArticleInternational journal of molecular sciences2020
Kaempferol and Its Glycoside, Kaempferol 7-O-Rhamnoside, Inhibit PD-1/PD-L1 Interaction In Vitro.
Article in International journal of molecular sciences, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 36 citations in OpenAlex.
- Dodonaea viscosa in Breast Cancer: Phytochemistry, Anticancer Mechanisms, and Emerging Immunotherapeutic and Translational Perspectives.Cancer medicine · 2026Review
- Metabolomics of Eryngium heterophyllum by UHPLC-QToF-MS and In Silico Insights Into Potential Metabolic Syndrome Targets.Chemistry & biodiversity · 2026Article
- Strategies to target PD-1/PD-L1 in the tumor microenvironment.Cellular oncology (Dordrecht, Netherlands) · 2026Review
- Phytochemistry, Bioactivity, and Toxicological Duality ofMolecules (Basel, Switzerland) · 2025Review
- Role of PD-1/PD-L1 signaling axis in oncogenesis and its targeting by bioactive natural compounds for cancer immunotherapy.Military Medical Research · 2024Review
- Progress in small-molecule inhibitors targeting PD-L1.RSC medicinal chemistry · 2024Review
- Investigation of the potential effects of estrogen receptor modulators on immune checkpoint molecules.Scientific reports · 2024Article
- Effect of Fragment 1 on the Binding of Epigallocatechin Gallate to the PD-L1 Dimer Explored by Molecular Dynamics.Molecules (Basel, Switzerland) · 2023Article
- Kaempferol and Biomodified Kaempferol fromInternational journal of molecular sciences · 2023Article
- Natural Blockers of PD-1/PD-L1 Interaction for the Immunotherapy of Triple-Negative Breast Cancer-Brain Metastasis.Cancers · 2022Review
- A systematic review of anti-cancer roles and mechanisms of kaempferol as a natural compound.Cancer cell international · 2022Review
- Further investigation of blockade effects and binding affinities of selected natural compounds to immune checkpoint PD-1/PD-L1.Frontiers in oncology · 2022Article
- Qingfei Jiedu decoction inhibits PD-L1 expression in lung adenocarcinoma based on network pharmacology analysis, molecular docking and experimental verification.Frontiers in pharmacology · 2022Article
- Network pharmacology and molecular docking analysis reveal insights into the molecular mechanism of shiliao decoction in the treatment of cancer-associated malnutrition.Frontiers in nutrition · 2022Article
- Small molecule inhibitors against PD-1/PD-L1 immune checkpoints and current methodologies for their development: a review.Cancer cell international · 2021Review
- Antioxidant vs. Prooxidant Properties of the Flavonoid, Kaempferol, in the Presence of Cu(II) Ions: A ROS-Scavenging Activity, Fenton Reaction and DNA Damage Study.International journal of molecular sciences · 2021Article
- Unripe Black Raspberry (Foods (Basel, Switzerland) · 2020Article
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Authors and funding
8 authors at 2 institutions in 1 country.
Funding
Abstract
Kaempferol (KO) and kaempferol 7-O-rhamnoside (KR) are natural products from various oriental herbs such as Geranii Herba. Previous studies have reported some biological activities of KO and KR; however, their effects on PD-1/PD-L1 interaction have not been reported yet. To elucidate their inhibitory activities on PD-1/PD-L1 protein-protein interaction (PPI), biochemical assays including competitive ELISA and biolayer interferometry (BLI) systems were performed. Cellular PD-1/PD-L1 blocking activity was measured in a co-culture system with PD-1 Jurkat and PD-L1/aAPC CHO-K1 cells by T-cell receptor (TCR) activation-induced nuclear factor of activated T cells (NFAT)-luciferase reporter assay. The detailed binding mode of action was simulated by an in silico docking study and pharmacophore analysis. Competitive ELISA revealed that KO and its glycoside KR significantly inhibited PD-1/PD-L1 interaction. Cellular PD-1/PD-L1 blocking activity was monitored by KO and KR at non-cytotoxic concentration. Surface plasmon resonance (SPR) and biolayer interferometry (BLI) analysis suggested the binding affinity and direct inhibition of KR against PD-1/PD-L1. An in silico docking simulation determined the detailed mode of binding of KR to PD-1/PD-L1. Collectively, these results suggest that KR could be developed as a potent small molecule inhibitor for PD-1/PD-L1 blockade.
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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.