Cell-Permeable Bicyclic Peptide Inhibitors against Intracellular Proteins

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• 作者：Wenlong Lian ; Bisheng Jiang ; Ziqing Qian ; Dehua Pei
• 刊名：Journal of the American Chemical Society
• 出版年：2014
• 出版时间：July 16, 2014
• 年：2014
• 卷：136
• 期：28
• 页码：9830-9833
• 全文大小：281K
• ISSN：1520-5126

文摘

Cyclic peptides have great potential as therapeutic agents and research tools but are generally impermeable to the cell membrane. Fusion of cyclic peptides with a cyclic cell-penetrating peptide produces bicyclic peptides that are cell-permeable and retain the ability to recognize specific intracellular targets. Application of this strategy to protein tyrosine phosphatase 1B and a peptidyl-prolyl cis鈭抰rans isomerase (Pin1) isomerase resulted in potent, selective, proteolytically stable, and biologically active inhibitors against the enzymes.