ArticleJournal of biomolecular screening2016
High-Throughput Screening for Internalizing Antibodies by Homogeneous Fluorescence Imaging of a pH-Activated Probe.
Article in Journal of biomolecular screening, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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
21 citing papers in PubMed, 38 citations in OpenAlex.
- Antibody-Drug Conjugates in Oncology: Principles, Clinical Development, and Future Directions.MedComm · 2026Review
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- Recent Advances in Antibody Discovery Using Ultrahigh-Throughput Droplet Microfluidics: Challenges and Future Perspectives.Biosensors · 2025Review
- Preclinical Characterization of theInternational journal of molecular sciences · 2023Article
- Semaphorin 6C Suppresses Proliferation of Pancreatic Cancer Cells via Inhibition of the AKT/GSK3/β-Catenin/Cyclin D1 Pathway.International journal of molecular sciences · 2022Article
- Semaphorin 4C promotes motility and immunosuppressive activity of cancer cells via CRMP3 and PD-L1.American journal of cancer research · 2022Article
- Halogenation at the Phenylalanine Residue of Monomethyl Auristatin F Leads to a FavorableMolecular pharmaceutics · 2021Article
- Misfolded amyloid-β-42 impairs the endosomal-lysosomal pathway.Cellular and molecular life sciences : CMLS · 2020Article
- Improving Receptor-Mediated Intracellular Access and Accumulation of Antibody Therapeutics-The Tale of HER2.Antibodies (Basel, Switzerland) · 2020Review
- Rapid conjugation of antibodies to toxins to select candidates for the development of anticancer Antibody-Drug Conjugates (ADCs).Scientific reports · 2020Article
- Mathematical modeling of drug-induced receptor internalization in the HER2-positive SKBR3 breast cancer cell-line.Scientific reports · 2019Article
- A high-throughput inhibition assay to study MERS-CoV antibody interactions using image cytometry.Journal of virological methods · 2019Article
- Development of a Novel EGFR-Targeting Antibody-Drug Conjugate for Pancreatic Cancer Therapy.Targeted oncology · 2019Article
- Challenges in Optimising the Successful Construction of Antibody Drug Conjugates in Cancer Therapy.Antibodies (Basel, Switzerland) · 2018Review
- Novel Antibody Drug Conjugates Targeting Tumor-Associated Receptor Tyrosine Kinase ROR2 by Functional Screening of Fully Human Antibody Libraries Using Transpo-mAb Display on Progenitor B Cells.Frontiers in immunology · 2018Article
- Novel high-throughput cell-based hybridoma screening methodology using the Celigo Image Cytometer.Journal of immunological methods · 2017Article
- Evaluation of Factors Influencing Antibody Reduction for Development of Antibody Drug ConjugatesIranian biomedical journal · 2017Article
- Responsive Contrast Agents: Synthesis and Characterization of a Tunable Series of pH-Sensitive Near-Infrared Pentamethines.ACS omega · 2016Article
- A high-throughput AO/PI-based cell concentration and viability detection method using the Celigo image cytometry.Cytotechnology · 2016Article
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Antibody-drug conjugates (ADCs) represent a rapidly growing class of biotherapeutics that deliver drugs specifically to target cells by binding of the antibody component to surface receptors. The majority of ADCs require receptor internalization depending on intrinsic features of the specific ADC-antigen interaction. The development of potent ADCs would greatly benefit from the identification of efficiently internalizing antibodies at early stages of discovery. We developed a highly sensitive and rapid antibody internalization assay using an indirect Cypher5E label. The pH-activated CypHer5E label becomes fluorescent upon internalization into the acidic environment of endocytic organelles, whereas background fluorescence of noninternalized CypHer5E is minimal. The pH-dependency of the CypHer5E signal enables robust discrimination of antibody internalization from surface binding. The favorable signal-over-background ratio allows a homogeneous assay design with high-throughput fluorescence imaging in 384- and 1536-well formats. The biophysical readout of the primary internalization event substantially shortens incubation times compared to killing assays using toxin internalization. The assay was validated with tumor-relevant targets, including receptor tyrosine kinases (EGFR and HER2) and a class II cytokine receptor (TF) expressed by A431, AU565, and SKOV-3 cells and transient expression systems (CHO-S). Our method enables functional screening of large antibody libraries to identify therapeutic antibody candidates with internalization characteristics favorable for the development of ADCs.
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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.