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Cell-Permeable Bicyclic Peptide Inhibitors against Intracellular Proteins
- Lian, Wenlong, Jiang, Bisheng, Qian, Ziqing, Pei, Dehua
- Journal of the American Chemical Society 2014 v.136 no.28 pp. 9830-9833
- cell membranes, cyclic peptides, peptidylprolyl isomerase, protein-tyrosine-phosphatase, proteins
- 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−trans isomerase (Pin1) isomerase resulted in potent, selective, proteolytically stable, and biologically active inhibitors against the enzymes.