Cyclobutane-bearing restricted anchoring residues enabled geometry-specific hydrocarbon peptide stapling

Chem. Sci., 2023, Advance Article
DOI: 10.1039/D3SC04279K, Edge Article
Open Access Open Access
Baobao Chen, Chao Liu, Wei Cong, Fei Gao, Yan Zou, Li Su, Lei Liu, Alexander Hillisch, Lutz Lehmann, Donald Bierer, Xiang Li, Hong-Gang Hu
Cyclobutane-based conformationally constrained amino acids, termed E7 and Z7, were rationally designed and efficiently synthesized, and were used for RCM-mediated peptide stapling to afford E7-E7 geometry-specific stapled peptides.
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