A Strategy for Discovering Heterochiral Bioactive Peptides by Using the OB2 n P Library and SPOTs Method
| Autor: | Takato H. Yoneda, Hinako Udagawa, Ryo Masuda, Takaki Koide |
|---|---|
| Rok vydání: | 2019 |
| Předmět: |
chemistry.chemical_classification
010405 organic chemistry Mimotope Chemistry Drug discovery Ligand binding assay High-throughput screening Organic Chemistry Peptide 010402 general chemistry Ligand (biochemistry) 01 natural sciences Biochemistry Combinatorial chemistry Chemical space 0104 chemical sciences Solid-phase synthesis Molecular Medicine Molecular Biology |
| Zdroj: | ChemBioChem. 20:2070-2073 |
| ISSN: | 1439-7633 1439-4227 |
| DOI: | 10.1002/cbic.201900237 |
| Popis: | d-Amino acid containing peptides are promising as drug lead compounds because of their expected higher stability in vivo. A heterochiral random peptide library called the one-bead-2n -peptide (OB2n P) library, which can display 2n peptide diastereomers per bead, has been developed. Through screening of the OB2n P library and subsequent binding assay among the peptide diastereomers synthesized in parallel by means of the SPOTs method, new heterochiral mimotopes for the anti-β-endorphin monoclonal antibody have been obtained. One mimotope was a new ligand for the μ-opioid receptor. The screening strategy enabled d-amino acid containing drug leads to be obtained efficiently by expanding searchable chemical space without increasing the experimental scale. |
| Databáze: | OpenAIRE |
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