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Cell-Permeable Bicyclic Peptide Inhibitors against Intracellular Proteins

Author:
Lian, Wenlong, Jiang, Bisheng, Qian, Ziqing, Pei, Dehua
Source:
Journal of the American Chemical Society 2014 v.136 no.28 pp. 9830-9833
ISSN:
1520-5126
Subject:
cell membranes, cyclic peptides, peptidylprolyl isomerase, protein-tyrosine-phosphatase, 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.
Agid:
5391872