ArticleiScience2019
The FG Loop of PD-1 Serves as a "Hotspot" for Therapeutic Monoclonal Antibodies in Tumor Immune Checkpoint Therapy.
Article in iScience, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 33 papers.
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Who cites it
33 citing papers in PubMed, 49 citations in OpenAlex.
- Humanized Anti-PD-1 Antibodies Generated Using The Conditional Kernel-Elastic Autoencoder.bioRxiv : the preprint server for biology · 2026Article
- De Novo Protein Design Enables Targeting of Intractable Oncogenic Protein-Protein Interfaces.Biologics (Basel, Switzerland) · 2026Article
- Engineering strategies and binding mechanisms of therapeutic anti-PD-1 antibodies approved by regulatory agencies globally.Frontiers in immunology · 2026Review
- De novo protein design enables targeting of intractable oncogenic interfaces.bioRxiv : the preprint server for biology · 2025Article
- Tislelizumab: Structural Innovations and Expanding Clinical Horizons in Next-Generation PD-1 Immunotherapy.Chronic diseases and translational medicine · 2025Review
- Phenotypic and targeted drug discovery in immune therapeutics: challenges, opportunities, and future directions.RSC advances · 2025Review
- Programmed cell death protein 1 in cancer cells.Cell communication and signaling : CCS · 2025Review
- An engineered PD1-Fc fusion produced in N. benthamiana plants efficiently blocks PD1/PDL1 interaction.Plant cell reports · 2025Article
- Are all programmed cell death protein 1 inhibitors the same?Frontiers in oncology · 2025Review
- Emerging therapeutic frontiers in cancer: insights into posttranslational modifications of PD-1/PD-L1 and regulatory pathways.Experimental hematology & oncology · 2024Review
- Variable PD-1 glycosylation modulates the activity of immune checkpoint inhibitors.Life science alliance · 2024Article
- Toripalimab, a therapeutic monoclonal anti-PD-1 antibody with high binding affinity to PD-1 and enhanced potency to activate human T cells.Cancer immunology, immunotherapy : CII · 2024Article
- Targeting PD-1/PD-L-1 immune checkpoint inhibition for cancer immunotherapy: success and challenges.Frontiers in immunology · 2024Review
- NSCLC: from tumorigenesis, immune checkpoint misuse to current and future targeted therapy.Frontiers in immunology · 2024Review
- An in silico investigation on the binding site preference of PD-1 and PD-L1 for designing antibodies for targeted cancer therapy.PloS one · 2024Article
- Mapping the epitope of PD-L1 to the paratope of the antibody durvalumab using molecular dynamics simulation.American journal of translational research · 2024Article
- Helicobacter pylori CagA promotes immune evasion of gastric cancer by upregulating PD-L1 level in exosomes.iScience · 2023Article
- KRAS G12V neoantigen specific T cell receptor for adoptive T cell therapy against tumors.Nature communications · 2023Article
- Passive Membrane Permeability of Sizable Acyclic β-Hairpin Peptides.ACS medicinal chemistry letters · 2023Article
- Exploiting the Innate Plasticity of the Programmed Cell Death-1 (PD1) Receptor to Design Pembrolizumab H3 Loop Mimics.Chembiochem : a European journal of chemical biology · 2022Article
Corrections and comments
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Authors and funding
15 authors at 6 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Programmed cell death 1 (PD-1)/PD-1 ligand-1 (PD-L1)-blocking monoclonal antibodies (mAbs) have taken center stage for tumor immune checkpoint therapy. Identification of the "hotspots" on PD-1 for mAbs will help to develop next-generation oral deliverable agents with long-lasting efficacy. Here, we identified two PD-1-targeting mAbs, GY-5 and GY-14, with PD-1/PD-L1-blocking efficacy. Complex structural information revealed that both mAbs mainly bind to the FG loop of PD-1, which also contributes multiple interactions with PD-L1. The FG loop adopts substantially varied conformations upon binding to different mAbs, providing a novel targetable region for the development of PD-1-specific biologics and small chemical molecules. Glycosylation modifications of PD-1 could be observed in three of the four potential N-linked glycosylation sites. However, the binding of GY-5 and GY-14 to PD-1 was not affected by glycosylation. These findings broaden our understanding of the mechanism of anti-PD-1 mAbs and provide insight into the development of agents targeting PD-1.
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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.