ArticlePharmaceutical research2001
Improving the selectivity of HAV-peptides in modulating E-cadherin-E-cadherin interactions in the intercellular junction of MDCK cell monolayers.
Article in Pharmaceutical research, 2001. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
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Who cites it
23 citing papers in PubMed, 66 citations in OpenAlex.
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- Storming the gate: New approaches for targeting the dynamic tight junction for improved drug delivery.Advanced drug delivery reviews · 2023Review
- Roads to Stat3 Paved with Cadherins.Cells · 2022Review
- Improving In Vivo Brain Delivery of Monoclonal Antibody Using Novel Cyclic Peptides.Pharmaceutics · 2019Article
- Glioblastoma Chemoresistance: The Double Play by Microenvironment and Blood-Brain Barrier.International journal of molecular sciences · 2018Review
- Effect of long non-coding RNA AOC4P on gastrointestinal stromal tumor cells.OncoTargets and therapy · 2018Article
- Probing the interaction between cHAVc3 peptide and the EC1 domain of E-cadherin using NMR and molecular dynamics simulations.Journal of biomolecular structure & dynamics · 2017Article
- Improving Brain Delivery of Biomolecules via BBB Modulation in Mouse and Rat: Detection using MRI, NIRF, and Mass Spectrometry.Nanotheranostics · 2017Article
- Brain Delivery of Drug and MRI Contrast Agent: Detection and Quantitative Determination of Brain Deposition of CPT-Glu Using LC-MS/MS and Gd-DTPA Using Magnetic Resonance Imaging.Molecular pharmaceutics · 2016Article
- Comparison of Linear and Cyclic His-Ala-Val Peptides in Modulating the Blood-Brain Barrier Permeability: Impact on Delivery of Molecules to the Brain.Journal of pharmaceutical sciences · 2016Article
- Modulation of intercellular junctions by cyclic-ADT peptides as a method to reversibly increase blood-brain barrier permeability.Journal of pharmaceutical sciences · 2015Article
- Pathways and progress in improving drug delivery through the intestinal mucosa and blood-brain barriers.Therapeutic delivery · 2014Review
- Modulation of blood-brain barrier permeability in mice using synthetic E-cadherin peptide.Molecular pharmaceutics · 2014Article
- Cleavage of transmembrane junction proteins and their role in regulating epithelial homeostasis.Tissue barriers · 2013Review
- Improving the stability of the EC1 domain of E-cadherin by thiol alkylation of the cysteine residue.International journal of pharmaceutics · 2012Article
- Enhancement of drug absorption through the blood-brain barrier and inhibition of intercellular tight junction resealing by E-cadherin peptides.Molecular pharmaceutics · 2011Article
- The role of covalent dimerization on the physical and chemical stability of the EC1 domain of human E-cadherin.Journal of pharmaceutical sciences · 2009Article
- Characterization of multiple stable conformers of the EC5 domain of E-cadherin and the interaction of EC5 with E-cadherin peptides.Chemical biology & drug design · 2009Article
- Evaluation of the physical stability of the EC5 domain of E-cadherin: effects of pH, temperature, ionic strength, and disulfide bonds.Journal of pharmaceutical sciences · 2009Article
- Effects of an E-cadherin-derived peptide on the gene expression of Caco-2 cells.Pharmaceutical research · 2004Article
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
purposeThe objective of this work is to understand the sequence specificity of HAV peptides and to improve their selectivity in regulating E-cadherin-E-cadherin interactions in the intercellular junctions.
methodsPeptide 1 was modified using an alanine scanning method to give peptides 2-6. The ability of these peptides to modulate intercellular junctions was evaluated using Madin-Darby Canine Kidney (MDCK) cell monolayers on Transwell membranes from either the apical (AP) or the basolateral (BL) side. Modulation of the intercellular junctions was measured by the ability to lower the transepithelial electrical resistance (TEER) of MDCK monolayers and by the increase in mannitol flux. Molecular docking experiments were performed to model the binding properties of these peptides to the EC1 domain of E-cadherin.
resultsPeptides 5 (Ac-SHAVAS-NH2) and 6 (Ac-SHAVSA-NH2) were found to be more effective than the parent peptide 1 in decreasing the resistance of the cell monolayer. Furthermore, comparative studies with the control and the weak inhibitor peptide 2 indicate that peptide 5 displayed a significant increase in mannitol flux. Molecular docking of peptides 1, 2 and 5 to the EC1 domain suggests that peptide 5 has the lowest binding energy.
conclusionsHAV peptides have the ability to modulate E-cadherin-E-cadherin interactions in the intercellular junctions of the MDCK cell monolayer, thus indirectly increasing the permeability of the tight junctions. This observation indicates that residues flanking the HAV sequence are important in the binding selectivity of HAV peptides to E-cadherin. Molecular docking can further aid in the design of peptides with better selectivity to the EC1 domain of E-cadherin.
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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.