In Vitro Selection of Macrocyclic d/l-Hybrid Peptides against Human EGFR
Open Access
- 6 April 2021
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of the American Chemical Society
- Vol. 143 (15), 5680-5684
- https://doi.org/10.1021/jacs.1c02593
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.Funding Information
- Core Research for Evolutional Science and Technology (JPMJCR12L2)
- Precursory Research for Embryonic Science and Technology (JPMJPR14K3)
- Japan Agency for Medical Research and Development (JP20am0101090)
- Japan Society for the Promotion of Science (JP18H02080, JP20H05618)
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