26. Fine Tuning the Properties of Stapled Peptides by Stereogenic α-Amino Acid Bridges
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作者:Qian Wang, Fengzhang Wang, Rui Li, Pushu Wang, Ruixin Yuan, Dangliang Liu, Yuan Liu, Prof. Yi Luan, Prof. Chu Wang*, Prof. Suwei Dong*
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发布时间: 2023-03-09
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chemistry-europechem.202203624
Qian Wang, Fengzhang Wang, Rui Li, Pushu Wang, Ruixin Yuan, Dangliang Liu, Yuan Liu, Prof. Yi Luan, Prof. Chu Wang*, Prof. Suwei Dong*

α-Amino Acids were used as bridges to construct side chain-stapled analogs library of an IL-17A-binding peptide (HAP) and evaluated the staples chirality (L/D) impacts on the peptide‘s properties. While all AA-derived peptidyl staples drastically increase the enzymatic stability of HAP, the L-AA-based staples generate more significant impacts in increasing the helicity and binding affinity of the modified peptide compared to the D-amino acid bridges.
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