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Issue 6, 2014
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Discovery of small molecule inhibitors targeting the SUMO–SIM interaction using a protein interface consensus approach

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Abstract

The SUMO–SIM is a challenging protein–protein interaction drug target. We present a virtual screening approach incorporating the consensus of protein interactions that led to the discovery of non-peptidic inhibitors. The most potent inhibitors have low micromolar potency and the binding affinity and interface was validated using multiple assays and HSQC-NMR.

Graphical abstract: Discovery of small molecule inhibitors targeting the SUMO–SIM interaction using a protein interface consensus approach

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Publication details

The article was received on 19 Dec 2013, accepted on 18 Mar 2014 and first published on 18 Mar 2014


Article type: Concise Article
DOI: 10.1039/C3MD00391D
Author version available: Download Author version (PDF)
Citation: Med. Chem. Commun., 2014,5, 783-786
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    Discovery of small molecule inhibitors targeting the SUMO–SIM interaction using a protein interface consensus approach

    A. R. D. Voet, A. Ito, M. Hirohama, S. Matsuoka, N. Tochio, T. Kigawa, M. Yoshida and K. Y. J. Zhang, Med. Chem. Commun., 2014, 5, 783
    DOI: 10.1039/C3MD00391D

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