Cell-permeable bicyclic peptide inhibitors against intracellular proteins.

Cell-permeable bicyclic peptide inhibitors against intracellular proteins.
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DOI:
10.1021/ja503710n
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发表时间:
2014-07-16
影响因子:
15
通讯作者:
Pei, Dehua
Pei, Dehua
中科院分区:
化学1区
文献类型:
--
作者:
Lian, Wenlong;Jiang, Bisheng;Qian, Ziqing;Pei, Dehua

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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.
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