功能高分子材料教育部重点实验室

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郭东升课题组 | ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

发布人:功能高分子材料教育部重点实验室    发布时间:2018/01/05   浏览次数: 693 次

Phosphorylation-Responsive Membrane Transport of Peptides

Peng, S (Peng, Shu)1,2 ] Barba-Bon, A (Barba-Bon, Andrea)1 ] Pan, YC (Pan, Yu-Chen)1,2 ] Nau, WM (Nau, Werner M.)1 ] Guo, DS (Guo, Dong-Sheng)2 ] Hennig, A (Hennig, Andreas)1 ]

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, 2017, 56(49): 15742-15745

DOI: 10.1002/anie.201707979

 WOS:000416244200046

Abstract

Phosphorylation and dephosphorylation of peptides by kinases and phosphatases is essential for signal transduction in biological systems, and many diseases involve abnormal activities of these enzymes. Herein, we introduce amphiphilic calixarenes as key components for supramolecular, phosphorylation-responsive membrane transport systems. Dye-efflux experiments with liposomes demonstrated that calixarenes are highly active counterion activators for established cell-penetrating peptides, with EC50 values in the low nanomolar range. We have now found that they can even activate membrane transport of short peptide substrates for kinases involved in signal transduction, whereas the respective phosphorylated products are much less efficiently transported. This allows regulation of membrane transport activity by protein kinaseA (PKA) and protein kinaseC (PKC), as well as monitoring of their activity in a label-free kinase assay.