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Generation of a cell-permeable cycloheptapeptidyl inhibitor against the peptidyl–prolyl isomerase Pin1

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Abstract

Cyclic peptides are capable of binding and modulating challenging drug targets including protein–protein interactions. However, their lack of membrane permeability prevents their application against intracellular targets. In this study, we show that it is possible to design a cell-permeable and biologically active cycloheptapeptide inhibitor against the intracellular enzyme peptidyl–prolyl isomerase Pin1 by integrating cell-penetrating and target-binding sequences.

Graphical abstract: Generation of a cell-permeable cycloheptapeptidyl inhibitor against the peptidyl–prolyl isomerase Pin1

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Publication details

The article was received on 21 Feb 2017, accepted on 23 Apr 2017 and first published on 18 May 2017


Article type: Communication
DOI: 10.1039/C7OB00430C
Citation: Org. Biomol. Chem., 2017, Advance Article
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    Generation of a cell-permeable cycloheptapeptidyl inhibitor against the peptidyl–prolyl isomerase Pin1

    W. Bedewy, H. Liao, N. A. Abou-Taleb, S. F. Hammad, T. Nasr and D. Pei, Org. Biomol. Chem., 2017, Advance Article , DOI: 10.1039/C7OB00430C

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