ArticleFEBS open bio2021
Tislelizumab uniquely binds to the CC' loop of PD-1 with slow-dissociated rate and complete PD-L1 blockage.
Article in FEBS open bio, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 59 papers, 1 of them a synthesis that pooled it.
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The trial behind it
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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
59 citing papers in PubMed, 1 synthesis or guideline pooled it, 71 citations in OpenAlex.
- Tislelizumab plus chemotherapy versus pembrolizumab plus chemotherapy for the first-line treatment of advanced non-small cell lung cancer: systematic review and indirect comparison of randomized trials.Frontiers in pharmacology · 2023Pooled it
- First-line tislelizumab plus chemotherapy versus placebo plus chemotherapy in adults with advanced or metastatic esophageal squamous cell carcinoma: a Japanese subgroup analysis of RATIONALE-306 with ≥ 3 years of follow-up.Esophagus : official journal of the Japan Esophageal Society · 2026Trial
- Adjuvant anlotinib plus TACE in hepatocellular carcinoma with postoperative high-risk recurrence: a single-arm, multi-center, phase II study.Clinical & translational oncology : official publication of the Federation of Spanish Oncology Societies and of the National Cancer Institute of Mexico · 2026Trial
- Phase Ib/II Study of Zanidatamab in Combination with Tislelizumab and Chemotherapy in First-Line HER2-Positive Gastric/Gastroesophageal Junction Adenocarcinoma.Clinical cancer research : an official journal of the American Association for Cancer Research · 2026Trial
- Sitravatinib plus tislelizumab in locally recurrent or metastatic triple-negative breast cancer: a multi-cohort, single-arm, phase II clinical trial (SPARK Trial).Molecular cancer · 2025Trial
- Trial
- Tislelizumab vs Sorafenib as First-Line Treatment for Unresectable Hepatocellular Carcinoma: A Phase 3 Randomized Clinical Trial.JAMA oncology · 2023Trial
- Tislelizumab plus chemotherapy for patients withJournal for immunotherapy of cancer · 2023Trial
- Tislelizumab with gemcitabine and oxaliplatin in patients with relapsed or refractory classic Hodgkin lymphoma: a multicenter phase II trial.Haematologica · 2023Trial
- Beyond trastuzumab: redefining first-line HER2-positive gastroesophageal cancer with bispecific HER2 targeting.Journal of gastrointestinal oncology · 2026Article
- Rapidly evolved PD-1 for enhance receptor and checkpoint inhibitor in immunotherapy.Molecular therapy. Oncology · 2026Article
- First-Line Tislelizumab Plus Chemotherapy for Advanced or Metastatic Squamous Non-Small Cell Lung Cancer: 4-Year Long-Term Follow-Up from RATIONALE-307.Oncology and therapy · 2026Article
- Tislelizumab combined with gemcitabine plus cisplatin for muscle-invasive upper tract urothelial carcinoma: A retrospective single-center cohort analysis.The Journal of international medical research · 2026Article
- Review
- Efficacy and safety of deep hyperthermia combined with tislelizumab and chemotherapy in the treatment of advanced squamous non-small-cell lung cancer: a single-center retrospective study.Frontiers in oncology · 2026Article
- Engineering strategies and binding mechanisms of therapeutic anti-PD-1 antibodies approved by regulatory agencies globally.Frontiers in immunology · 2026Review
- Structure-Guided In-Use Stability Assessment of Monoclonal Antibody Tislelizumab.Pharmaceuticals (Basel, Switzerland) · 2025Article
- Efficacy and safety of tislelizumab plus anlotinib and irinotecan as second-line treatment for extensive-stage small cell lung cancer: a single-arm, open-label, phase II trial.EClinicalMedicine · 2025Article
- Tislelizumab: Structural Innovations and Expanding Clinical Horizons in Next-Generation PD-1 Immunotherapy.Chronic diseases and translational medicine · 2025Review
- Monoclonal Antibodies (mAbs) and Proteins: The Biologic Drugs Approved by the Food and Drug Administration (FDA) in 2024.Biomedicines · 2025Review
Corrections and comments
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Authors and funding
15 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Programmed cell death protein 1 (PD-1), an immune checkpoint receptor expressed by activated T, B, and NK cells, is a well-known target for cancer immunotherapy. Tislelizumab (BGB-A317) is an anti-PD-1 antibody that has recently been approved for treatment of Hodgkin's lymphoma and urothelial carcinoma. Here, we show that tislelizumab displayed remarkable antitumor efficacy in a B16F10/GM-CSF mouse model. Structural biology and Surface plasmon resonance (SPR) analyses revealed unique epitopes of tislelizumab, and demonstrated that the CC' loop of PD-1, a region considered to be essential for binding to PD-1 ligand 1 (PD-L1) but not reported as targeted by other therapeutic antibodies, significantly contributes to the binding of tislelizumab. The binding surface of tislelizumab on PD-1 overlaps largely with that of the PD-L1. SPR analysis revealed the extremely slow dissociation rate of tislelizumab from PD-1. Both structural and functional analyses align with the observed ability of tislelizumab to completely block PD-1/PD-L1 interaction, broadening our understanding of the mechanism of action of anti-PD-1 antibodies.
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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.