In Vitro Selection of Macrocyclic d /l -Hybrid Peptides against Human EGFR
| Autor: | Hiroaki Suga, Takayuki Katoh, Sayaka Imanishi, Marina Kawai, Yizhen Yin, Mituhiro Yamada |
|---|---|
| Rok vydání: | 2021 |
| Předmět: |
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 |
| Zdroj: | Journal of the American Chemical Society. 143:5680-5684 |
| ISSN: | 1520-5126 0002-7863 |
| DOI: | 10.1021/jacs.1c02593 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|