Issue 42, 2010
From the journal:

Chemical Communications

Profiling small molecule inhibitors against helix–receptor interactions: the Bcl-2 family inhibitor BH3I-1 potently inhibits p53/hDM2†‡

Jason R. Porter,a   Mark R. Helmers,a   Ping Wang,a   Jennifer L. Furman,a   Stephen T. Joy,b   Paramjit S. Arora*b  and  Indraneel Ghosh*a  

* Corresponding authors

a Department of Chemistry and Biochemistry, University of Arizona, 1306 East University Blvd, Tucson, USA
E-mail: ghosh@u.arizona.edu
Fax: +1 520 621 8407
Tel: +1 520 621 6345

b Department of Chemistry, New York University, 100 Washington Square East New York, USA
E-mail: arora@nyu.edu
Tel: +1 212 998 8470

Abstract

We validate a practical methodology for the rapid profiling of small molecule inhibitors of protein–protein interactions. We find that a well known BH3 family inhibitor can potently inhibit the p53/hDM2 interaction.

Graphical abstract: Profiling small molecule inhibitors against helix–receptor interactions: the Bcl-2 family inhibitor BH3I-1 potently inhibits p53/hDM2

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Article information

DOI
https://doi.org/10.1039/C0CC02969F
Article type
Communication
Submitted
02 Aug. 2010
Accepted
21 Aug. 2010
First published
20 Sept. 2010

Chem. Commun., 2010,46, 8020-8022

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Profiling small molecule inhibitors against helix–receptor interactions: the Bcl-2 family inhibitor BH3I-1 potently inhibits p53/hDM2

J. R. Porter, M. R. Helmers, P. Wang, J. L. Furman, S. T. Joy, P. S. Arora and I. Ghosh, Chem. Commun., 2010, 46, 8020 DOI: 10.1039/C0CC02969F

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