scholarly journals Designing stapled peptides to inhibit protein‐protein interactions: An analysis of successes in a rapidly changing field

2020 ◽  
Author(s):  
Marie T. J. Bluntzer ◽  
James O'Connell ◽  
Terry S. Baker ◽  
Julien Michel ◽  
Alison N. Hulme
Keyword(s):  
Protein Interactions ◽  
Protein Protein Interactions ◽  
Stapled Peptides

CHAPTER 8. Double-click Stapled Peptides for Inhibiting Protein–Protein Interactions

2017 ◽  
pp. 164-187 ◽  
Author(s):  
K. Sharma ◽  
D. L. Kunciw ◽  
W. Xu ◽  
M. M. Wiedmann ◽  
Y. Wu ◽  
...  
Keyword(s):  
Protein Interactions ◽  
Protein Protein Interactions ◽  
Stapled Peptides ◽  
Inhibiting Protein

scholarly journals Stapled peptides as a new technology to investigate protein–protein interactions in human platelets

2018 ◽  
Vol 9 (20) ◽  
pp. 4638-4643 ◽  
Author(s):  
Jessica Iegre ◽  
Niaz S. Ahmed ◽  
Josephine S. Gaynord ◽  
Yuteng Wu ◽  
Kara M. Herlihy ◽  
...  
Keyword(s):  
Platelet Activation ◽  
Protein Interactions ◽  
New Technology ◽  
Human Platelets ◽  
Protein Protein Interactions ◽  
Stapled Peptides ◽  
Traditional Methods

We describe the first application of stapled peptides in human platelets. Bim BH3 stapled peptides are used to overcome the limitations of traditional methods and uncover a new role for Bim in platelet activation.

scholarly journals Titelbild: Light-Regulated Stapled Peptides to Inhibit Protein-Protein Interactions Involved in Clathrin-Mediated Endocytosis (Angew. Chem. 30/2013)

2013 ◽  
Vol 125 (30) ◽  
pp. 7759-7759
Author(s):  
Laura Nevola ◽  
Andrés Martín-Quirós ◽  
Kay Eckelt ◽  
Núria Camarero ◽  
Sébastien Tosi ◽  
...  
Keyword(s):  
Protein Interactions ◽  
Protein Protein Interactions ◽  
Stapled Peptides

scholarly journals Cover Picture: Light-Regulated Stapled Peptides to Inhibit Protein-Protein Interactions Involved in Clathrin-Mediated Endocytosis (Angew. Chem. Int. Ed. 30/2013)

2013 ◽  
Vol 52 (30) ◽  
pp. 7607-7607
Author(s):  
Laura Nevola ◽  
Andrés Martín-Quirós ◽  
Kay Eckelt ◽  
Núria Camarero ◽  
Sébastien Tosi ◽  
...  
Keyword(s):  
Protein Interactions ◽  
Protein Protein Interactions ◽  
Stapled Peptides

Light-Regulated Stapled Peptides to Inhibit Protein-Protein Interactions Involved in Clathrin-Mediated Endocytosis

2013 ◽  
Vol 125 (30) ◽  
pp. 7858-7862 ◽  
Author(s):  
Laura Nevola ◽  
Andrés Martín-Quirós ◽  
Kay Eckelt ◽  
Núria Camarero ◽  
Sébastien Tosi ◽  
...  
Keyword(s):  
Protein Interactions ◽  
Protein Protein Interactions ◽  
Stapled Peptides

scholarly journals Unprotected Peptide Macrocyclization and Stapling via A Fluorine-Thiol Displacement Reaction

2020 ◽  
Author(s):  
Md Shafiqul Islam ◽  
Samuel L. Junod ◽  
Si Zhang ◽  
Zakey Yusuf Buuh ◽  
Yifu Guan ◽  
...  
Keyword(s):  
Cellular Uptake ◽  
Protein Interactions ◽  
Cell Permeability ◽  
Displacement Reaction ◽  
Protein Protein Interactions ◽  
Cancer Cell Growth ◽  
Stapled Peptides ◽  
Peptide Substrates ◽  
New Approach ◽  
Dynamics Simulations

AbstractStapled peptides serve as a powerful tool for probing protein-protein interactions, but its application has been largely impeded by the limited cellular uptake. Here we report the discovery of a facile peptide macrocyclization and stapling strategy based on a fluorine thiol displacement reaction (FTDR), which renders a class of peptide analogues with enhanced stability, affinity, and cell permeability. This new approach enabled selective modification of the orthogonal fluoroacetamide side chains in unprotected peptides, with the identified 1,3-benzenedimethanethiol linker promoting alpha helicity of a variety of peptide substrates, as corroborated by molecular dynamics simulations. The cellular uptake of these stapled peptides was universally enhanced compared to the classic ring-closing metathesis (RCM) stapled peptides. Pilot mechanism studies suggested that the uptake of FTDR-stapled peptides may involve multiple endocytosis pathways. Consistent with the improved cell permeability, the FTDR-stapled lead Axin analogues demonstrated better inhibition of cancer cell growth than the RCM-stapled analogues.Graphical Abstract

An intramolecular tryptophan-condensation approach for peptide stapling

2018 ◽  
Vol 16 (3) ◽  
pp. 389-392 ◽  
Author(s):  
Eunice Y.-L. Hui ◽  
Bhimsen Rout ◽  
Yaw Sing Tan ◽  
Chandra S. Verma ◽  
Kok-Ping Chan ◽  
...  
Keyword(s):  
Protein Interactions ◽  
Therapeutic Agents ◽  
Target Protein ◽  
Next Generation ◽  
Protein Protein Interactions ◽  
Stapled Peptides ◽  
Tryptophan Residues ◽  
Peptide Stapling

Stapled peptides are gaining tremendous interest as next-generation therapeutic agents to target protein–protein interactions. Herein, we report an intramolecular peptide stapling method which links two tryptophan residues at C2 position of the indole moieties via acid-mediated condensation with an aldehyde.

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