ArticleScientific reports2017
Identification of claudin-4 binder that attenuates tight junction barrier function by TR-FRET-based screening assay.
Article in Scientific reports, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed.
- Targeting claudins in cancer.Nature reviews. Drug discovery · 2026Review
- Structure-forward targeting of claudins with synthetic binders.FEBS letters · 2026Review
- The IQGAP1-Claudin4-JNK Signaling Axis as a Differential Biomarker in Renal Cell Carcinoma.Clinical and translational science · 2026Article
- The IQGAP1-claudin cell junction axis in cisplatin-induced epithelial damage.Cell communication and signaling : CCS · 2026Article
- Identification of amino acids essential for angulin-1/3 binding of the tricellular tight junction binder, angubindin-1.FEBS open bio · 2026Article
- Claudin-4 Modulates Autophagy via SLC1A5/LAT1 as a Mechanism to Regulate Micronuclei.Cancer research communications · 2024Article
- Characterization of an iPSC-based barrier model for blood-brain barrier investigations using the SBAD0201 stem cell line.Fluids and barriers of the CNS · 2023Article
- Storming the gate: New approaches for targeting the dynamic tight junction for improved drug delivery.Advanced drug delivery reviews · 2023Review
- Single-Cell Analysis Reveals Unexpected Cellular Changes and Transposon Expression Signatures in the Colonic Epithelium of Treatment-Naïve Adult Crohn's Disease Patients.Cellular and molecular gastroenterology and hepatology · 2022Article
- Host-Pathogen Interactions ofPathogens (Basel, Switzerland) · 2021Article
- Tight Junction Modulating Bioprobes for Drug Delivery System to the Brain: A Review.Pharmaceutics · 2020Review
- Evaluation of Sucrose Laurate as an Intestinal Permeation Enhancer for Macromolecules: Ex Vivo and In Vivo Studies.Pharmaceutics · 2019Article
- Potential for Tight Junction Protein-Directed Drug Development Using Claudin Binders and Angubindin-1.International journal of molecular sciences · 2019Review
Corrections and comments
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Authors and funding
12 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Claudins are key functional and structural components of tight junctions (TJs) in epithelial cell sheets. The C-terminal fragment of Clostridium perfringens enterotoxin (C-CPE) binds to claudin-4 and reversibly modulates intestinal TJ seals, thereby enhancing paracellular transport of solutes. However, the use of C-CPE as an absorption enhancer is limited by the molecule's immunogenicity and manufacturing cost. Here, we developed a high-throughput screening system based on the Time-Resolved Fluorescence Resonance Energy Transfer (TR-FRET) method to identify claudin-4 binders in a library collection of 32,560 compounds. Thiostrepton, identified from the screen, decreased transepithelial electrical resistance and increased flux of 4-kDa fluorescein isothiocyanate-labelled dextran (FD-4) in Caco-2 cell monolayers, a model of intestinal epithelium. Thiostrepton changed the expression, but not the localisation, of TJ components. Treatment of rat jejunum with thiostrepton increased the absorption of FD-4 without tissue toxicity, indicating that thiostrepton is a novel claudin-4 binder that enhances intestinal permeability. The screening system may therefore be a useful tool for identifying claudin-4 binders to enhance drug absorption in mucosa.
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