Molecular tweezers target a protein–protein interface and thereby modulate complex formation

F. Trusch; K. Kowski; K. Bravo-Rodriguez; C. Beuck; A. Sowislok; B. Wettig; A. Matena; E. Sanchez-Garcia; H. Meyer; T. Schrader; P. Bayer

doi:10.1039/C6CC08039A

Molecular tweezers target a protein–protein interface and thereby modulate complex formation†

F. Trusch,

‡^a K. Kowski,^b K. Bravo-Rodriguez,^c C. Beuck,^a A. Sowislok,^b B. Wettig,^b A. Matena,^a E. Sanchez-Garcia,^c H. Meyer,^d T. Schrader^b and P. Bayer

*^a

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* Corresponding authors

^a University of Duisburg-Essen, Research Group Structural and Medicinal Biochemistry, Centre for Medical Biotechnology (ZMB), 45117 Essen, Germany
E-mail: peter.bayer@uni-due.de

^b University of Duisburg-Essen, Research Group Organic Chemistry, 45117 Essen, Germany

^c Max-Planck-Institut für Kohlenforschung, Kaiser-Wilhelm-Platz 1, 45470 Mülheim an der Ruhr, Germany

^d University of Duisburg-Essen, Research Group Molecular Biology I, Centre for Medical Biotechnology (ZMB), 45117 Essen, Germany

Abstract

Molecular tweezers for lysine and arginine select a few residues on a protein surface and by their unique complexation mode disrupt a critical protein–protein interaction. Detailed structural information was gained by NMR experiments, strongly supported by QM/MM calculations and further substantiated by ITC, fluorescence anisotropy, ELISA and bio-layer-interference studies.

Chemical Communications

Molecular tweezers target a protein–protein interface and thereby modulate complex formation†

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Molecular tweezers target a protein–protein interface and thereby modulate complex formation

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