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In Vitro Selection of Macrocyclic <scp>d</scp>/<scp>l</scp>-Hybrid Peptides against Human EGFR
- Source :
- Journal of the American Chemical Society. 143:5680-5684
- Publication Year :
- 2021
- Publisher :
- American Chemical Society (ACS), 2021.
-
Abstract
- d/l-Hybrid peptides are an attractive class of molecular modality because they are able to exhibit high proteolytic stability and unique structural diversity which cannot be accessed by those consisting of only proteinogenic l-amino acids. Despite such an expectation, it has not been possible to devise de novo d/l-hybrid peptides capable of disrupting the function of a protein target(s) due to the lack of an effective method that reliably constructs a highly diverse library and screens active species. Here we report for the first time construction of a library consisting of 1012 members of macrocyclic d/l-hybrid peptides containing five kinds of d-amino acids and performance of the RaPID selection against human EGFR as a showcase to uncover PPI (protein-protein interaction) inhibitors.
- Subjects :
- Protein Stability
Chemistry
Structural diversity
A protein
General Chemistry
Computational biology
010402 general chemistry
Peptides, Cyclic
01 natural sciences
Biochemistry
Catalysis
In vitro
0104 chemical sciences
ErbB Receptors
Kinetics
Colloid and Surface Chemistry
Humans
Amino Acid Sequence
Protein Interaction Maps
Amino Acids
Protein Kinase Inhibitors
Selection (genetic algorithm)
Function (biology)
Half-Life
Protein Binding
Subjects
Details
- ISSN :
- 15205126 and 00027863
- Volume :
- 143
- Database :
- OpenAIRE
- Journal :
- Journal of the American Chemical Society
- Accession number :
- edsair.doi.dedup.....8bd7d4696f8b0678335e6a8cd7cb8103