ArticleJournal of biomolecular structure & dynamics2010
A conformationally constrained peptidomimetic binds to the extracellular region of HER2 protein.
Article in Journal of biomolecular structure & dynamics, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed, 44 citations in OpenAlex.
- The Dual Role of Nanomaterials in Ovarian Cancer and Female Fertility as Anti- and Prooxidants.Antioxidants (Basel, Switzerland) · 2025Review
- Peptides Targeting HER2-Positive Breast Cancer Cells and Applications in Tumor Imaging and Delivery of Chemotherapeutics.Nanomaterials (Basel, Switzerland) · 2023Review
- Peptidomimetics in cancer targeting.Molecular medicine (Cambridge, Mass.) · 2022Review
- Lipidated Peptidomimetic Ligand-Functionalized HER2 Targeted Liposome as Nano-Carrier Designed for Doxorubicin Delivery in Cancer Therapy.Pharmaceuticals (Basel, Switzerland) · 2021Article
- Computationally-guided design and affinity improvement of a protein binder targeting a specific site on HER2.Computational and structural biotechnology journal · 2021Article
- Article
- DISPOT: a simple knowledge-based protein domain interaction statistical potential.Bioinformatics (Oxford, England) · 2019Article
- Dynamical Rearrangement of Human Epidermal Growth Factor Receptor 2 upon Antibody Binding: Effects on the Dimerization.Biomolecules · 2019Article
- Design of novel lipidated peptidomimetic conjugates for targeting EGFR heterodimerization in HER2 + cancer.Bioorganic & medicinal chemistry letters · 2018Article
- Homo- and Heterodimerization of Proteins in Cell Signaling: Inhibition and Drug Design.Advances in protein chemistry and structural biology · 2018Review
- A peptidomimetic with a chiral switch is an inhibitor of epidermal growth factor receptor heterodimerization.Oncotarget · 2017Article
- Expression and purification of HER2 extracellular domain proteins in Schneider2 insect cells.Protein expression and purification · 2016Article
- Design and Synthesis of Near-Infrared Peptide for in Vivo Molecular Imaging of HER2.Bioconjugate chemistry · 2016Article
- Surfing the Protein-Protein Interaction Surface Using Docking Methods: Application to the Design of PPI Inhibitors.Molecules (Basel, Switzerland) · 2015Review
- Novel Peptidomimetics for Inhibition of HER2:HER3 Heterodimerization in HER2-Positive Breast Cancer.Chemical biology & drug design · 2015Article
- Current and future targeted therapies for non-small-cell lung cancers with aberrant EGF receptors.Future oncology (London, England) · 2015Review
- Structure-activity relationships of peptidomimetics that inhibit PPI of HER2-HER3.Biopolymers · 2014Article
- Design, synthesis and characterization of peptidomimetic conjugate of BODIPY targeting HER2 protein extracellular domain.European journal of medicinal chemistry · 2013Article
- Inhibition of protein-protein interaction of HER2-EGFR and HER2-HER3 by a rationally designed peptidomimetic.Journal of biomolecular structure & dynamics · 2012Article
- Structure-activity relationship of conformationally constrained peptidomimetics for antiproliferative activity in HER2-overexpressing breast cancer cell lines.MedChemComm · 2011Article
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
Human epidermal growth factor receptor 2 (HER2) is a member of the human epidermal growth factor receptor kinases (other members include EGFR or HER1, HER3, and HER4) that are involved in signaling cascades for cell growth and differentiation. It is well established that HER2-mediated heterodimerization has important implications in cancer. Deregulation of signaling pathways and overexpression of HER2 is known to occur in cancer cells, indicating a role of HER2 in tumorigenesis. Therefore, blocking HER2-mediated signaling has potential therapeutic value. We have designed several peptidomimetics to inhibit HER2-mediated signaling for cell growth. One of the compounds (HERP5, Arg-beta Naph-Phe) exhibited antiproliferative activity with IC(50) values in the micromolar-to-nanomolar range in breast cancer cell lines. Binding of fluorescently labeled HERP5 to HER2 protein was evaluated by fluorescence assay, microscopy, and circular dichroism spectroscopy. Results indicated that HERP5 binds to the extracellular region of the HER2 protein. Structure of the peptidomimetic HERP5 was studied by NMR and molecular dynamics simulations. Based on these results a model was proposed for HER2-EGFR dimerization and possible blocking by HERP5 peptidomimetic using a protein-protein docking method.
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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.