title: Cell-permeable bicyclic peptide inhibitors against intracellular proteins.
abstract: 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.
authors: Department of Chemistry and Biochemistry, The Ohio State University , 484 West 12th Avenue, Columbus, Ohio 43210, United States.
authors: Wenlong
authors: W
authors: Lian
authors: Bisheng
authors: B
authors: Jiang
authors: Ziqing
authors: Z
authors: Qian
authors: Dehua
authors: D
authors: Pei
mesh_terms: D001643:Bridged Bicyclo Compounds / Q000138:chemical synthesis* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002463:Cell Membrane Permeability; D057846:Cell-Penetrating Peptides / Q000138:chemical synthesis* / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D006801:Humans; D010456:Peptides, Cyclic / Q000138:chemical synthesis* / Q000494:pharmacology*; D019696:Peptidylprolyl Isomerase / Q000037:antagonists & inhibitors / Q000737:chemistry; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1 / Q000037:antagonists & inhibitors; D013329:Structure-Activity Relationship
chemical_list: D001643:Bridged Bicyclo Compounds; D057846:Cell-Penetrating Peptides; D004791:Enzyme Inhibitors; D010456:Peptides, Cyclic; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1; D019696:Peptidylprolyl Isomerase