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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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Supplementary files

Article information


Submitted
19 Dec 2013
Accepted
18 Mar 2014
First published
18 Mar 2014

Med. Chem. Commun., 2014,5, 783-786
Article type
Concise Article
Author version available

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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