ArticleJournal of biomolecular screening2012
A high-content biosensor-based screen identifies cell-permeable activators and inhibitors of EGFR function: implications in drug discovery.
Article in Journal of biomolecular screening, 2012. 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
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
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
17 citing papers in PubMed, 31 citations in OpenAlex.
- Novel "C-Clamp" Design of Highly Selective Small-Molecule Sensors for Kinase Proteins.Chemical & biomedical imaging · 2026Article
- Regulation of intercellular viscosity by E-cadherin-dependent phosphorylation of EGFR in collective cell migration.Proceedings of the National Academy of Sciences of the United States of America · 2024Article
- Expression-Based Diagnosis, Treatment Selection, and Drug Development for Breast Cancer.International journal of molecular sciences · 2023Article
- Zero-Background Small-Molecule Sensors for Near-IR Fluorescent Imaging of Biomacromolecular Targets in Cells.ACS sensors · 2023Article
- Multi-Omics Immune Interaction Networks in Lung Cancer Tumorigenesis, Proliferation, and Survival.International journal of molecular sciences · 2022Article
- The Cardenolide Glycoside Acovenoside A Interferes with Epidermal Growth Factor Receptor Trafficking in Non-Small Cell Lung Cancer Cells.Frontiers in pharmacology · 2021Article
- Drug Screening with Genetically Encoded Fluorescent Sensors: Today and Tomorrow.International journal of molecular sciences · 2020Review
- A Live-Cell Screen for Altered Erk Dynamics Reveals Principles of Proliferative Control.Cell systems · 2020Article
- Growth Factor Signaling Regulates Mechanical Nociception in Flies and Vertebrates.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2019Article
- Vasculogenic and angiogenic potential of adipose stromal vascular fraction cell populations in vitro.In vitro cellular & developmental biology. Animal · 2018Article
- Image-based compound profiling reveals a dual inhibitor of tyrosine kinase and microtubule polymerization.Scientific reports · 2016Article
- Chemical & RNAi screening at MSKCC: a collaborative platform to discover & repurpose drugs to fight disease.Combinatorial chemistry & high throughput screening · 2014Article
- A 1536-well fluorescence polarization assay to screen for modulators of the MUSASHI family of RNA-binding proteins.Combinatorial chemistry & high throughput screening · 2014Article
- A novel high throughput 1536-well Notch1 γ -secretase AlphaLISA assay.Combinatorial chemistry & high throughput screening · 2013Article
- A synergetic screening approach with companion effector for combination therapy: application to retinoblastoma.PloS one · 2013Article
- Central VEGF-A pathway plays a key role in the development of trigeminal neuropathic pain in rats.Molecular painArticle
- A high-content assay strategy for the identification and profiling of ABCG2 modulators in live cells.Assay and drug development technologiesArticle
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
Early success of kinase inhibitors has validated their use as drugs. However, discovery efforts have also suffered from high attrition rates due to lack of cellular activity. We reasoned that screening for such candidates in live cells would identify novel cell-permeable modulators for development. For this purpose, we have used our recently optimized epidermal growth factor receptor (EGFR) biosensor assay to screen for modulators of EGFR activity. Here, we report on its validation under high-throughput screening (HTS) conditions displaying a signal-to-noise ratio of 21 and a Z' value of 0.56-attributes of a robust cell-based assay. We performed a pilot screen against a library of 6912 compounds demonstrating good reproducibility and identifying 82 inhibitors and 66 activators with initial hit rates of 1.2% and 0.95%, respectively. Follow-up dose-response studies revealed that 12 of the 13 known EGFR inhibitors in the library were confirmed as hits. ZM-306416, a vascular endothelial growth factor receptor (VEGFR) antagonist, was identified as a potent inhibitor of EGFR function. Flurandrenolide, beclomethasone, and ebastine were confirmed as activators of EGFR function. Taken together, our results validate this novel approach and demonstrate its utility in the discovery of novel kinase modulators with potential use in the clinic.
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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.