ArticleAngewandte Chemie (International ed. in English)2017
Enhancing the Cell Permeability and Metabolic Stability of Peptidyl Drugs by Reversible Bicyclization.
Article in Angewandte Chemie (International ed. in English), 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 48 papers.
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Who cites it
48 citing papers in PubMed.
- Linker Engineering in Stapled Peptides for Enhanced Membrane Permeability: Screening and Optimization Strategies.International journal of molecular sciences · 2026Review
- Fast Generation of Simulation-Quality Structural Ensembles of Mixed-Chirality Cyclic Peptides via Diffusion Models.Journal of chemical theory and computation · 2026Article
- Live-Cell Raman Imaging Elucidates Intracellular Distribution of Macrocyclic Peptides Designed as HIV Protease Inhibitors.Chemical & biomedical imaging · 2026Article
- CyclicMPNN: Stable Cyclic Peptide Sequence Generation.bioRxiv : the preprint server for biology · 2026Article
- Differential Self-Assembly Behaviors and Proteolytic Stability of Bicyclic Peptides Compared to Monocyclic Peptides.Chemistry, an Asian journal · 2026Article
- Advances in Peptidomimetics for Next-Generation Therapeutics: Strategies, Modifications, and Applications.Chemical reviews · 2025Review
- Dimeric copper peptide incorporated hydrogel for promoting diabetic wound healing.Nature communications · 2025Article
- End-to-End Backbone Cyclization Enhances Passive Permeability of bRo5 Oligomeric Depsipeptides with Nonlinear Size Dependence.ACS medicinal chemistry letters · 2025Article
- CYCLICCAE: A CONFORMATIONAL AUTOENCODER FOR EFFICIENT HETEROCHIRAL MACROCYCLIC BACKBONE SAMPLING.bioRxiv : the preprint server for biology · 2025Article
- Tackling Undruggable Targets with Designer Peptidomimetics and Synthetic Biologics.Chemical reviews · 2024Review
- Targeted delivery of extracellular vesicles: the mechanisms, techniques and therapeutic applications.Molecular biomedicine · 2024Review
- Peptide PET Imaging: A Review of Recent Developments and a Look at the Future of Radiometal-Labeled Peptides in Medicine.Chemical & biomedical imaging · 2024Review
- Recent Advances in Metal-Free Peptide Stapling Strategies.Chem & bio engineering · 2024Review
- Review
- Development and preclinical characterization of a novel radiotheranostic EphA2-targeting bicyclic peptide.Theranostics · 2024Article
- Research Progress on Cyclic-Peptide Functionalized Nanoparticles for Tumor-Penetrating Delivery.International journal of nanomedicine · 2024Review
- Intracellular Application of an Asparaginyl Endopeptidase for Producing Recombinant Head-to-Tail Cyclic Proteins.JACS Au · 2023Article
- Peptides Targeting HER2-Positive Breast Cancer Cells and Applications in Tumor Imaging and Delivery of Chemotherapeutics.Nanomaterials (Basel, Switzerland) · 2023Review
- Enhancing Cell Penetration Efficiency of Cyclic Oligoarginines Using Rigid Scaffolds.Pharmaceutics · 2023Article
- p-Chloropropynyl Phenylalanine, a Versatile Non-Canonical Amino Acid for Co-Translational Peptide Macrocyclization and Side Chain Diversification.Chembiochem : a European journal of chemical biology · 2023Article
Corrections and comments
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Authors and funding
8 authors.
Funding
Abstract
Therapeutic applications of peptides are currently limited by their proteolytic instability and impermeability to the cell membrane. A general, reversible bicyclization strategy is now reported to increase both the proteolytic stability and cell permeability of peptidyl drugs. A peptide drug is fused with a short cell-penetrating motif and converted into a conformationally constrained bicyclic structure through the formation of a pair of disulfide bonds. The resulting bicyclic peptide has greatly enhanced proteolytic stability as well as cell-permeability. Once inside the cell, the disulfide bonds are reduced to produce a linear, biologically active peptide. This strategy was applied to generate a cell-permeable bicyclic peptidyl inhibitor against the NEMO-IKK interaction.
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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.