Issue 6, 2014
From the journal:

MedChemComm

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

Arnout R. D. Voet,‡a   Akihiro Ito,‡bc   Mikako Hirohama,be   Seiji Matsuoka,d   Naoya Tochio,§f   Takanori Kigawa,f   Minoru Yoshidabcde  and  Kam Y. J. Zhang*a  

* Corresponding authors

a Zhang Initiative Research Unit, RIKEN, 2-1 Hirosawa, Wako, Saitama 351-0198, Japan
E-mail: kamzhang@riken.jp

b Chemical Genetics Laboratory, RIKEN, 2-1 Hirosawa, Wako, Saitama 351-0198, Japan

c Chemical Genomics Research Group, RIKEN Center for Sustainable Resource Science, 2-1 Hirosawa, Wako, Saitama 351-0198, Japan

d Drug Discovery Platforms Cooperation Division, RIKEN Center for Sustainable Resource Science, 2-1 Hirosawa, Wako, Saitama 351-0198, Japan

e Japan Science and Technology Corporation, CREST Research Project, 4-1-8 Honcho, Kawaguchi, Saitama 332-0012, Japan

f Laboratory for Biomolecular Structure and Dynamics, Quantitative Biology Center, RIKEN, 1-7-22 Suehiro, Yokohama, Kanagawa 230-0045, Japan

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

About
Cited by
Related
Download options Please wait...

Supplementary files

Article information

DOI
https://doi.org/10.1039/C3MD00391D
Article type
Concise Article
Submitted
19 Dec 2013
Accepted
18 Mar 2014
First published
18 Mar 2014

Med. Chem. Commun., 2014,5, 783-786

Author version available

Download author version (PDF)

Permissions

Request permissions

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

To request permission to reproduce material from this article, please go to the Copyright Clearance Center request page.

If you are an author contributing to an RSC publication, you do not need to request permission provided correct acknowledgement is given.

If you are the author of this article, you do not need to request permission to reproduce figures and diagrams provided correct acknowledgement is given. If you want to reproduce the whole article in a third-party publication (excluding your thesis/dissertation for which permission is not required) please go to the Copyright Clearance Center request page.

Read more about how to correctly acknowledge RSC content.

Spotlight

Advertisements