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.

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 Elucidating the druggable interface of protein−protein interactions using fragment docking and coevolutionary analysis

2016 ◽  
Vol 113 (50) ◽  
pp. E8051-E8058 ◽  
Author(s):  
Fang Bai ◽  
Faruck Morcos ◽  
Ryan R. Cheng ◽  
Hualiang Jiang ◽  
José N. Onuchic
Keyword(s):  
Drug Design ◽  
Protein Interactions ◽  
Binding Sites ◽  
Hot Spots ◽  
Therapeutic Agents ◽  
Molecular Probes ◽  
Therapeutic Drug ◽  
Protein Protein Interactions ◽  
Protein Surface ◽  
Fragment Docking

Protein−protein interactions play a central role in cellular function. Improving the understanding of complex formation has many practical applications, including the rational design of new therapeutic agents and the mechanisms governing signal transduction networks. The generally large, flat, and relatively featureless binding sites of protein complexes pose many challenges for drug design. Fragment docking and direct coupling analysis are used in an integrated computational method to estimate druggable protein−protein interfaces. (i) This method explores the binding of fragment-sized molecular probes on the protein surface using a molecular docking-based screen. (ii) The energetically favorable binding sites of the probes, called hot spots, are spatially clustered to map out candidate binding sites on the protein surface. (iii) A coevolution-based interface interaction score is used to discriminate between different candidate binding sites, yielding potential interfacial targets for therapeutic drug design. This approach is validated for important, well-studied disease-related proteins with known pharmaceutical targets, and also identifies targets that have yet to be studied. Moreover, therapeutic agents are proposed by chemically connecting the fragments that are strongly bound to the hot spots.

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.

Interfering peptides targeting protein–protein interactions: the next generation of drugs?

2018 ◽  
Vol 23 (2) ◽  
pp. 272-285 ◽  
Author(s):  
Heriberto Bruzzoni-Giovanelli ◽  
Valerie Alezra ◽  
Nicolas Wolff ◽  
Chang-Zhi Dong ◽  
Pierre Tuffery ◽  
...  
Keyword(s):  
Protein Interactions ◽  
Next Generation ◽  
Protein Protein Interactions

scholarly journals Small-Molecule Inhibitors That Target Protein-Protein Interactions in the RAD51 Family of Recombinases

ChemMedChem ◽  
2014 ◽  
Vol 10 (2) ◽  
pp. 296-303 ◽  
Author(s):  
Duncan E. Scott ◽  
Anthony G. Coyne ◽  
Ashok Venkitaraman ◽  
Tom L. Blundell ◽  
Chris Abell ◽  
...  
Keyword(s):  
Small Molecule ◽  
Protein Interactions ◽  
Small Molecule Inhibitors ◽  
Target Protein ◽  
Protein Protein Interactions

scholarly journals Use of periplasmic target protein capture for phage display engineering of tight-binding protein–protein interactions

2011 ◽  
Vol 24 (11) ◽  
pp. 819-828 ◽  
Author(s):  
Bartlomiej G. Fryszczyn ◽  
Nicholas G. Brown ◽  
Wanzhi Huang ◽  
Miriam A. Balderas ◽  
Timothy Palzkill
Keyword(s):  
Phage Display ◽  
Protein Interactions ◽  
Binding Protein ◽  
Tight Binding ◽  
Target Protein ◽  
Protein Protein Interactions ◽  
Protein Capture

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 Next-Generation Sequencing for Binary Protein–Protein Interactions

2015 ◽  
Vol 6 ◽  
Author(s):  
Bernhard Suter ◽  
Xinmin Zhang ◽  
C. Gustavo Pesce ◽  
Andrew R. Mendelsohn ◽  
Savithramma P. Dinesh-Kumar ◽  
...  
Keyword(s):  
Next Generation Sequencing ◽  
Protein Interactions ◽  
Next Generation ◽  
Protein Protein Interactions ◽  
Generation Sequencing
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