ArticlemAbs2015
Generation and characterization of a target-selectively activated antibody against epidermal growth factor receptor with enhanced anti-tumor potency.
Article in mAbs, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
What it found
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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.
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Who cites it
17 citing papers in PubMed.
- Article
- Rational Design, Synthesis, and Systematic Evaluation of Redox-Responsive SN-38 Prodrugs for Selective Activation in Hypoxic Tumor Microenvironments.Pharmaceuticals (Basel, Switzerland) · 2026Article
- A facile yeast-display approach for antibody mask discovery.Protein engineering, design & selection : PEDS · 2025Article
- A Generic Antibody-Blocking Protein That Enables pH-Switchable Activation of Antibody Activity.ACS chemical biology · 2024Article
- CD47-SIRPα blocking-based immunotherapy: Current and prospective therapeutic strategies.Clinical and translational medicine · 2022Review
- Identification, Efficacy, and Stability Evaluation of Succinimide Modification With a High Abundance in the Framework Region of Golimumab.Frontiers in chemistry · 2022Article
- Conjugation of glucosylated polymer chains to checkpoint blockade antibodies augments their efficacy and specificity for glioblastoma.Nature biomedical engineering · 2021Article
- Selective activation of pro-anti-IL-1β antibody enhances specificity for autoinflammatory disorder therapy.Scientific reports · 2021Article
- The Masking Game: Design of Activatable Antibodies and Mimetics for Selective Therapeutics and Cell Control.ACS central science · 2021Review
- Ab locks for improving the selectivity and safety of antibody drugs.Journal of biomedical science · 2020Review
- Optical Control of Antibody Activity by Using Photocleavable Bivalent Peptide-DNA Locks.Chembiochem : a European journal of chemical biology · 2019Article
- A coiled-coil masking domain for selective activation of therapeutic antibodies.Nature biotechnology · 2019Article
- EGFR-Targeted Immunotoxin Exerts Antitumor Effects on Esophageal Cancers by Increasing ROS Accumulation and Inducing Apoptosis via Inhibition of the Nrf2-Keap1 Pathway.Journal of immunology research · 2018Article
- Selective antibody activation through protease-activated pro-antibodies that mask binding sites with inhibitory domains.Scientific reports · 2017Article
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Corrections and comments
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Authors and funding
15 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Panitumumab, as a commercially available antibody, is an effective anticancer therapeutic against epidermal growth factor receptor (EGFR), although it exerts weak antibody-dependent cell-mediated cytotoxicity (ADCC) activity owing to its IgG2 nature. Here, we firstly engineered panitumumab by grafting its variable region into an IgG1 backbone. The engineered panitumumab (denoted as Pan) retained binding activity identical to the parental antibody while exhibiting stronger ADCC activity in vitro and more potent antitumor effect in vivo. To further enhance the target selectivity of Pan, we generated Pan-P by tethering an epitope-blocking peptide to Pan via a tumor-specific protease selective linker. Pan-P showed almost 40-fold weaker affinity compared with Pan, but functional activity was restored to a similar extent as Pan when Pan-P was selectively activated by urokinase-type plasminogen activator (uPA). More importantly, targeted localization of Pan-P was observed in tumor samples from colorectal cancer (CRC) patients and tumor-bearing nude mice, strongly indicating that specific activation also existed ex vivo and in vivo. Furthermore, Pan-P also exhibited effective in vivo antitumor potency similar to Pan. Taken together, our data evidence the enhanced antitumor potency and excellent target selectivity of Pan-P, suggesting its potential use for minimizing on-target toxicity in anti-EGFR therapy.
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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.